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					Pharmacircle Results-Products & Pipeline : Therapeutic Category contains 'asthma'
Product_Pipeline     Therapeutic Categories (inc. partners)                 Phases (inc.         Molecules
Name                                                                        partners)


159797               ·COPD·Asthma                                           ·Phase2Ongoing·Phas -
                                                                            e2




159802               ·COPD·Asthma                                           ·Phase2Ongoing·Phas -
                                                                            e2




256066 Inhaled       ·Asthma·COPD                                           ·Phase2Ongoing·Phas -
                                                                            e2Ongoing

274150               ·RheumatoidArthritis·Migraine·Asthma                   ·Phase2Discontinued· -
                                                                            Phase2Discontinued·
                                                                            Phase2Discontinued




678007               ·COPD·Asthma                                           ·Phase2Ongoing·Phas -
                                                                            e2Ongoing
679586               ·Asthma                                                ·Phase2Ongoing      -


799943               ·Asthma·COPD                                           ·Phase2Discontinued· -
                                                                            Phase2Discontinued
870086    ·Asthma           ·Phase2Ongoing        -




ABN912    ·Asthma·COPD      ·Phase1Discontinued· -
                            Phase1Discontinued

ADC3322   ·Asthma·COPD      ·PreClinicalOngoing·P -
                            reClinicalOngoing

ADC3680   ·Asthma·Allergy   ·PreClinicalOngoing·P -
                            reClinicalOngoing

ADC4022   ·Asthma·COPD      ·Phase2Ongoing·Phas -
                            e2Ongoing
AEROSPAN Inhalation ·Asthma           ·Marketed           flunisolide
Aerosol




AFM19               ·Allergy·Asthma   ·ResearchOngoing·Re -
                                      searchOngoing

AG NCA805           ·Asthma           ·Research           -
AGI-Series for         ·Asthma   ·PreClinicalDiscontinu -
Respiratory Diseases             ed




AI-128                 ·Asthma   ·Phase1Finished        -
AIR Albuterol     ·Asthma           ·Phase2Discontinued albuterol sulfate




AIR GSK Program   ·Asthma           ·Phase1Discontinued -

AIR645            ·Asthma·Allergy   ·Phase1Finished·PreC -
                                    linical
AKELA CGRP   ·Asthma   ·Phase2   -
ALEGYSAL Dry syrup ·Asthma·Allergy   ·Marketed·Marketed   pemirolast potassium
ALEGYSAL Tablets     ·Allergy·Asthma   ·Marketed·Marketed   pemirolast potassium




ALK-Abello 2nd       ·Asthma           ·Research            -
Generation Tablets
AM-103    ·Asthma·Cardiovascular   ·Phase2Ongoing·Phas -
                                   e2Ongoing




AM211     ·Asthma·Allergy·COPD     ·Phase1Ongoing·Phas -
                                   e1Ongoing·Phase1On
                                   going




AMG 009   ·Asthma·Allergy          ·Phase1·Phase1      -

AMG 317   ·Asthma                  ·Phase2Ongoing      -




AMG 853   ·Asthma                  ·Phase1Ongoing      -
AP768                ·Asthma·AtopicDermatitis          ·Phase1·Phase1          -

APC-366              ·Asthma                           ·Phase2                 APC 366

ARD-1700             ·Asthma·COPD                      ·PreClinicalOngoing·P -
                                                       reClinicalOngoing




AT-1003              ·Asthma·COPD                      ·Research·Research      -

ATL 1102 Inhaled     ·Asthma                           ·PreClinical            -




ATL-844              ·Asthma·Diabetes,Type2            ·PreClinical·PreClinica -
                                                       l

ATL-907              ·Asthma                           ·PreClinical            -


AV 1101 Spray Form   ·Antiinflammatory/Immune·Asthma   ·Phase2·Undisclosed -

AVAC Asthma,         ·Asthma                           ·Phase1Discontinued -
Genesis/SR Pharma

AVE 0675             ·Asthma·Allergy                   ·Phase1Ongoing·Phas -
                                                       e1Ongoing
AVE 7279    ·Asthma·Allergy   ·Phase1Discontinued· -
                              Phase1Discontinued




AVE8923     ·Asthma           ·Phase1Ongoing     -
AVP-13358   ·Asthma·Allergy   ·Phase1OnHold·Phas -
                              e1OnHold
AVT-01                ·Asthma        ·Phase2Ongoing         -




AWD 12-281, Inhaled   ·COPD·Asthma   ·Phase2Discontinued· AWD 12-281
                                     Phase2Discontinued

AZD1419               ·Asthma·COPD   ·PreClinicalFinished·P -
                                     reClinical
AZD1678               ·Asthma        ·PreClinicalDiscontinu -
                                     ed
AZD1981   ·Asthma·COPD   ·Phase2Ongoing·Phas -
                         e2Ongoing




AZD2098   ·Asthma        ·PreClinicalDiscontinu -
                         ed
AZD2392   ·Asthma        ·PreClinicalDiscontinu -
                         ed
AZD3199   ·Asthma·COPD   ·Phase2·Phase2         -


AZD3778   ·Asthma        ·Phase1Discontinued -

AZD3825   ·Asthma        ·PreClinical        -
AZD5985   ·Asthma·COPD   ·Phase1Ongoing·Phas -
                         e1Ongoing


AZD8075   ·Asthma·COPD   ·Phase1Ongoing·Phas -
                         e1Ongoing
AZD8848   ·Asthma        ·Phase1             -




AZD9215   ·Asthma        ·PreClinicalDiscontinu -
                         ed
AZX100               ·WoundCare·Asthma·MuscleSpasm·IdiopathicPulmonaryFi ·Phase2Ongoing·PreC -
                     brosis                                              linicalOngoing·PreClini
                                                                         cal·PreClinicalOngoin
                                                                         g



Aarane N             ·Asthma                                              ·Marketed            triazolam· reproterol




Ablynx Respiratory   ·Asthma                                              ·Research            -
Program
Accolate Tablets   ·Asthma   ·Marketed   zafirlukast
AccuNeb Inhalation   ·Asthma                ·Marketed            albuterol sulfate
Solution




AccuNeb Inhalation   ·Bronchospasm·Asthma   ·Approved·Approved   albuterol sulfate
Solution, Generic
Watson
Actimis Respiratory   ·Asthma·Allergy   ·PreClinical·PreClinica -
and Inflammatory                        l
Disease Program




Acuair                ·Asthma           ·Phase2Discontinued fluticasone propionate
Advair Diskus   ·Asthma·COPD   ·Marketed·Marketed   fluticasone propionate·
                                                    salmeterol xinafoate
Advair HFA   ·Asthma   ·Marketed   fluticasone propionate·
                                   salmeterol xinafoate
AeRx HCQ   ·Asthma·COPD   ·Phase2Discontinued· hydroxychloroquine
                          Phase2Discontinued sulfate




Aeriva     ·Asthma        ·ResearchOngoing     -
AeroVant   ·Asthma   ·Phase2Ongoing   pitrakinra
Aerobid   ·Asthma   ·Marketed   flunisolide
Aerodose Albuterol   ·Asthma   ·Phase1Discontinued albuterol
Inhaler
Aerodose Budesonide ·Asthma   ·Phase1Discontinued budesonide
Inhaler
Aeron                 ·Asthma·Bronchitis   ·Marketed·Marketed   ipratropium bromide
                                                                anhydrous




AerovectRx            ·Asthma              ·Research            -
Respiratory Program
Afonilum Retard        ·Asthma·COPD   ·Marketed·Marketed   theophylline




Albuterol Inhalation   ·Asthma        ·Marketed            albuterol
Aerosol, GenPharm
Albuterol Inhalation   ·Asthma   ·Marketed   albuterol
Aerosol, Ivax
Albuterol Inhalation   ·Asthma   ·Marketed   albuterol sulfate
Aerosol, Martec
Albuterol Inhalation   ·Asthma   ·Marketed   albuterol
Aerosol, Pliva
Albuterol Mystic   ·Asthma   ·UndisclosedDiscontin albuterol
                             ued
Albuterol Sulfate      ·Asthma   ·Marketed   albuterol sulfate
Inhalation Solution,
Dey




Albuterol Sulfate      ·Asthma   ·Marketed   albuterol sulfate
Inhalation Solution,
Morton G.
Albuterol Sulfate      ·Asthma   ·Marketed   albuterol sulfate
Inhalation Solution,
Nephron
Albuterol Sulphate,   ·Asthma           ·PreClinical         albuterol sulfate
Chrysalis




Albuterol analog      ·Asthma           ·ResearchDiscontinue -
                                        d
Alesion Tablets       ·Allergy·Asthma   ·Marketed·Marketed epinastine
                                                             hydrochloride




Alexion IV Eculizumab ·Asthma           ·Phase1Finished      eculizumab




Alexion Nebulized     ·Asthma           ·Phase2              eculizumab
Eculizumab
Allegra Tablets   ·Allergy·SkinDisorders·Asthma·AtopicDermatitis   ·Marketed·Marketed·P fexofenadine
                                                                   hase3·Phase3         hydrochloride
Allergica Asthma     ·Asthma    ·Phase1               -
Program




Allergospas Novolizer ·Asthma   ·PreClinicalDiscontinu sodium cromoglycate·
                                ed                     reproterol
Allergospasmin   ·Asthma·COPD·Bronchitis   ·Marketed·Marketed·   sodium cromoglycate·
                                           Marketed              reproterol




Alluvant         ·Asthma                   ·PreClinical          -
Alphaprot   ·Emphysema·Asthma·CysticFibrosis   ·PreClinical·PreClinica alpha1-proteinase
                                               l·PreClinical           inhibitor, human
Alupent Inhalation   ·Asthma   ·Marketed   metaproterenol
Aerosol                                    sulphate
Alupent Inhalation   ·Asthma   ·Marketed   metaproterenol
Solution                                   sulphate
Alupent Inhalation    ·Asthma   ·Marketed   metaproterenol
Solution, Generic DEY                       sulphate
Alupent Inhalation   ·Asthma   ·Marketed   metaproterenol
Solution, Generic                          sulphate
Morton Grove
Alupent Inhalation   ·Asthma   ·Marketed   metaproterenol
Solution, Generic                          sulphate
Nephron
Alvesco 80 and 160    ·Asthma·Allergy·Asthma   ·Marketed·Phase1     ciclesonide
Inhalers




Alvesco Combination   ·Asthma                  ·Phase2              ciclesonide· formoterol




Ambrx FCER1 Ab        ·Asthma                  ·PreClinical         -
Program
Amsol-SR              ·Asthma·Bronchitis       ·Marketed·Marketed   ambroxol
                                                                    hydrochloride
Andolast              ·Asthma·Allergy·COPD                   ·Phase3·Phase1·Phas andolast
                                                             e2




Anti-Chitinase MAb,   ·Asthma·COPD·Antiinflammatory/Immune   ·PreClinicalDiscontinu -
Medimmune                                                    ed·PreClinicalDisconti
                                                             nued·PreClinical
Anti-IL13 program,    ·Asthma                                ·Phase2                -
Genentech


Antitope/NKT Antibody ·Asthma                                ·Research              -
Program
Aridol Test Kit   ·Asthma·COPD·Imaging&Diagnostics   ·Marketed·Phase2Fini mannitol
                                                     shed·Approved
Arzileuton Program,     ·Asthma·COPD·Atherosclerosis   ·Phase1·Phase1·Phas zileuton
Critical Therapeutics                                  e1
Asmabec Clickhaler   ·Asthma   ·Marketed   beclomethasone
                                           dipropionate




Asmacure Asthma      ·Asthma   ·Research   -
Program
Asmanex Twisthaler   ·Asthma   ·Marketed   mometasone furoate
Asmasal Clickhaler   ·Asthma   ·Marketed   albuterol
Assist/Asmair       ·Asthma·COPD   ·Research·Research     -
Actuated Inhaler
Programs




Asthma Program,     ·Asthma        ·PreClinicalDiscontinu -
Barr/Vectura                       ed
Asthma Program,     ·Asthma        ·UndisclosedDiscontin -
Eiffel/Meridica                    ued




Asthma Program,     ·Asthma        ·PreClinicalOngoing    -
Immune Control
Asthma Program,     ·Asthma        ·Undisclosed           -
Selecore
Asthma Vaccine,     ·Asthma        ·ResearchDiscontinue -
Genesis/SR Pharma                  d
Asthma/Allergy   ·Allergy·Asthma   ·PreClinical·PreClinica -
Program, 7TM                       l
Asthmolysin Tab.   ·Asthma   ·Marketed   proxyphylline·
                                         ephedrine
                                         hydrochloride·
                                         phenobarbital
Ataroc Syrup   ·Asthma·Bronchitis·Emphysema   ·Marketed·Marketed·   procaterol
                                              Marketed              hydrochloride
Ataroc Tablets   ·Asthma·Bronchitis·Emphysema   ·Marketed·Marketed·   procaterol
                                                Marketed              hydrochloride
Atrovent Aerocaps   ·COPD·Asthma·Bronchospasm   ·Marketed·Marketed·   ipratropium bromide
                                                Marketed              hydrate
Atrovent Inhalation   ·Asthma   ·MarketedDiscontinue ipratropium bromide
Aerosol-CFC                     d                    hydrate
Atrovent Inhalation   ·Asthma   ·Marketed   ipratropium bromide
Solution                                    hydrate
Avidia Asthma       ·Asthma                           ·PreClinical        -
Program




Avrina NF-κB   ·Asthma·RheumatoidArthritis·IBD   ·Research·Research· -
Decoy                                                 PreClinical

Axikin Asthma       ·Asthma                           ·PreClinical        -
Program
Azmacort HFA        ·Asthma                           ·Approvable         triamcinolone
                                                                          acetonide
Azmacort MDI   ·Asthma   ·Marketed   triamcinolone
                                     acetonide
BDP Modulite   ·Asthma   ·Marketed   beclomethasone
                                     dipropionate
BEA 2180 BR    ·COPD·Asthma              ·Phase2·Phase2        -




BFPT-2603      ·Asthma                   ·PreClinical          -

BI 1744 CL     ·COPD·Asthma              ·Phase3·Phase2        -




BIBW 2948 BS   ·COPD·Asthma·Bronchitis   ·Phase2·Phase2·Phas -
                                         e2

BIW-8405       ·Asthma                   ·Phase2Ongoing        -




BN83470        ·Asthma·COPD·Allergy      ·PreClinicalOngoing·P -
                                         reClinicalOngoing·Pre
                                         ClinicalOngoing
BT-061              ·RheumatoidArthritis·Psoriasis·Asthma·Allergy   ·Phase2Ongoing·Phas -
                                                                    e2Ongoing·PreClinical
                                                                    ·PreClinical

Bambec Tablets      ·Asthma·Bronchospasm                            ·Marketed·Marketed     bambuterol
                                                                                           hydrochloride




Battelle/Eiffel     ·Asthma                                         ·PreClinicalDiscontinu -
Technologies Asthma                                                 ed
Program
Beclazone Easi-        ·Asthma   ·Marketed           beclomethasone
Breathe 50, 100, 250                                 dipropionate
mcg Inhaler




Becloforte DiskHaler   ·Asthma   ·MarketedDiscontinue beclomethasone
                                 d                    dipropionate
Beclomet EasyHaler   ·Asthma   ·Marketed   beclomethasone
                                           dipropionate




Beclomethasone       ·Asthma   ·Marketed   beclomethasone
Cyclohaler                                 dipropionate
Becotide Aerosol   ·Asthma   ·Marketed   beclomethasone
                                         dipropionate
Berodual/Duovent   ·Asthma   ·Marketed   fenoterol
Respimat                                 hydrobromide·
                                         ipratropium bromide
                                         hydrate
Berotec Inhalation   ·Asthma    ·Marketed   fenoterol
Solution                                    hydrobromide




Berotec/Berotec Forte ·Asthma   ·Marketed   fenoterol
                                            hydrobromide
Betagen               ·Asthma·IBD                              ·PreClinical           -




Betaprot              ·Asthma·RheumatoidArthritis·IBD          ·PreClinical           -




Bionasal Amphoterin B ·Sinusitis·Asthma                        ·PreClinical·PreClinica amphotericin B
                                                               l




Bosatria              ·BloodCellDisorders·Esophagitis·Asthma   ·Registration·Phase2 mepolizumab
                                                               Ongoing·Phase2Ongo
                                                               ing
Brethine Injectable   ·Asthma   ·Marketed   terbutaline sulfate




Brethine Tablet       ·Asthma   ·Marketed   terbutaline sulfate
Bricanyl              ·Asthma          ·Marketed            terbutaline sulfate
Inhaler/Aerosol




Bricanyl Turbohaler   ·Asthma·Asthma   ·Marketed·Marketed   terbutaline sulfate




Bronica Tablets       ·Asthma          ·Marketed            seratrodast
Budesonid-ratiopharm ·Asthma   ·Marketed   budesonide
Auto-Jethaler




Budesonid-ratiopharm ·Asthma   ·Marketed   budesonide
Jethaler
Budesonide           ·Asthma    ·Marketed   budesonide
Airmax/Spiromax




Budesonide Clickhaler ·Asthma   ·Marketed   budesonide
Budesonide Cyclohaler ·Asthma   ·Marketed             budesonide




Budesonide HFA       ·Asthma    ·Discontinued/Inactive budesonide
SkyeFine
Budesonide Inhalation ·Asthma                                           ·Marketed           budesonide
Suspension, Ivax




Budesonide MMX       ·Asthma·Allergy·Crohn'sDisease·UlcerativeColitis   ·Phase3Ongoing·Phas budesonide
                                                                        e3Ongoing·Phase3On
                                                                        going·Phase3Ongoing
Budesonide Modulite   ·Asthma   ·Marketed   budesonide
Budesonide Mystic   ·Asthma·COPD   ·UndisclosedDiscontin budesonide
                                   ued·UndisclosedDisco
                                   ntinued




Budesonide          ·Asthma·COPD   ·Phase3·Phase3       budesonide
PowderWhirl
Butovent Pulvinal   ·Asthma   ·Marketed   albuterol
Buventol EasyHaler   ·Asthma   ·Marketed        albuterol




CAT-354              ·Asthma   ·Phase2Ongoing   -
CC-10004   ·PsoriaticArthritis·Psoriasis·Lupus·Behcet'sDisease·Asthm ·Phase2Ongoing·Phas apremilast
           a                                                         e2Ongoing·Phase1On
                                                                     going·Phase2Ongoing
                                                                     ·Undisclosed




CEP-1347   ·Asthma·Parkinson's·Asthma                              ·Phase2Finished·Phas -
                                                                   e2Discontinued·Phase
                                                                   2
CHF 4226   ·Asthma·COPD                                            ·Phase2·Phase2       carmoterol
CHF 5188          ·Asthma·COPD                         ·Phase2·Phase2      carmoterol·
                                                                           budesonide




CK-2018509        ·Asthma·PulmonaryHypertension·COPD   ·PreClinicalOngoing·P -
                                                       reClinicalOngoing·Pre
                                                       ClinicalOngoing
CLEANAL Tablets   ·Bronchitis·Asthma·Tuberculosis      ·Marketed·Marketed· fudosteine
                                                       Marketed
CP-141          ·Asthma                           ·UndisclosedDiscontin -
                                                  ued




CP-325366copd   ·Asthma·COPD                      ·Phase2Discontinued· tofimilast
                                                  Phase2Discontinued

CP-4112         ·Asthma·Antiinflammatory/Immune   ·ResearchOngoing·Re betamethasone
                                                  searchOngoing
CP-4114               ·Asthma·Antiinflammatory/Immune   ·Research·Research      prednisolone




CR 3465               ·Asthma·InterstitialCystitis      ·PreClinical·PreClinica -
                                                        l




CRTH2 Antagonist      ·Allergy·Asthma                   ·Phase2·Undisclosed -
Program, Actelion
CRTh2 Receptor        ·Asthma·Allergy                   ·Research·Research      -
Antagonist Program,
Argenta Discovery
CRx-170 MR Program ·ChronicPain·Asthma   ·Phase2OnHold·Phas prednisolone·
                                         e2                 nortriptyline
CRx-170   ·Asthma·ChronicPain   ·Phase2Finished·Phas prednisolone·
                                e2OnHold             nortriptyline
CTT Bromelain   ·Asthma   ·Research        bromelains




CVT-6883        ·Asthma   ·Phase1Ongoing   -
CYT003-QbG10   ·Allergy·AtopicDermatitis·Asthma   ·Phase2Finished·Phas -
                                                  e2·Phase2Ongoing
CYT005-AllQbG10   ·Allergy·Asthma   ·Phase2·Phase2   -
Vaccine
Calcort Tablets     ·RheumatoidArthritis·Asthma·Crohn'sDisease·Cancer,Leuk ·Marketed·Marketed· deflazacort
                    emia·Cancer,Lymphoid·OrganTransplantation              Marketed·Marketed·M
                                                                           arketed·Marketed




Captisol-Enabled      ·Asthma·COPD                                        ·Phase2·Phase2       budesonide
Budesonide Inhalation
Solution
Celera Allergy and   ·Asthma·Allergy   ·PreClinical·PreClinica -
Asthma Program                         l




Celltech/UCB/Merck   ·Asthma·COPD      ·Phase1·Phase1          -
PDE4 Inhibitor
Cellzome Itk Program   ·Allergy·Asthma·AtopicDermatitis   ·Research·Research· -
                                                          Research




Cellzome PI3K          ·RheumatoidArthritis·Asthma        ·PreClinical·PreClinica -
Gamma Program                                             l
Chiesi PDE-IV          ·Asthma·COPD                       ·Research·Research -
Inhibitors Program
Choledyl SA ER        ·Emphysema·Asthma·Bronchitis   ·Marketed·Marketed·   oxtriphylline
Tablets                                              Marketed




Choledyl SR Tablets   ·Asthma·PulmonaryEdema         ·Marketed·Marketed    choline theophylline




Ciclesonide Nebules   ·Asthma                        ·Phase1               ciclesonide
Cintredekin          ·Asthma·IdiopathicPulmonaryFibrosis   ·PreClinical·PreClinica cintredekin besudotox
Besudotox, Inhaled                                         l
Cipla/LTT         ·RheumatoidArthritis·Asthma   ·PreClinical·PreClinica -
Nanosteroids                                    l




Clenil Pulvinal   ·Asthma                       ·Marketed               beclomethasone
                                                                        dipropionate
Combivent   ·Asthma   ·Marketed   ipratropium bromide
                                  hydrate· albuterol
                                  sulfate
Concept1 Formoterol   ·Asthma   ·Phase2             formoterol




Contramid Xopenex     ·Asthma   ·Phase2Discontinued levalbuterol
                                                    hydrochloride
Corus 1030   ·Asthma   ·Phase2Discontinued lidocaine
Cromogen Easi-   ·Asthma   ·Marketed   cromolyn sodium
Breathe
Cromolyn Depot    ·Asthma        ·UndisclosedDiscontin cromolyn sodium
                                 ued




Cromolyn Mystic   ·Asthma·COPD   ·UndisclosedDiscontin cromolyn
                                 ued·UndisclosedDisco
                                 ntinued
Cue Astma Program   ·Asthma           ·Research              -

DMI 8393            ·Asthma           ·PreClinical           -

DRF-2546            ·COPD·Asthma      ·PreClinicalFinished·P -
                                      reClinicalFinished
DSP-3025            ·Allergy·Asthma   ·PreClinicalFinished·P -
                                      reClinicalFinished




Daxas               ·COPD·Asthma      ·Registration·Phase3   roflumilast




Diffumal 24         ·Asthma·COPD      ·Marketed·Marketed     theophylline
Dom0910   ·Asthma   ·Research   -
Domenan Tablets   ·Asthma   ·Marketed   ozagrel hydrochloride
Dual PI3K              ·RheumatoidArthritis·SLE·Asthma   ·ResearchFinished·Re -
gamma/delta inhibitors                                   searchFinished·Resea
                                                         rchFinished




DuoHaler Project #1   ·Asthma·COPD                       ·Phase2·Phase2         -


DuoHaler Project #2   ·Asthma·COPD                       ·Phase2·Phase2         -


Durason               ·Asthma                            ·Phase2                -




EP-012637             ·Asthma                            ·PreClinicalDiscontinu -
                                                         ed
EP-314         ·Asthma        ·PreClinicalDiscontinu -
                              ed




EPI-12323      ·Asthma·COPD   ·Phase1·Phase1         undisclosed small
Combinations                                         molecule· undisclosed
                                                     small molecule
ETX9101               ·Asthma   ·Phase2               -




Eiffel/Oriel Asthma   ·Asthma   ·UndisclosedDiscontin -
Program                         ued
Eligen Cromolyn   ·Allergy·Asthma   ·Phase1Discontinued· cromolyn sodium
Sodium                              Phase1Discontinued
Epinephrine Mist     ·Asthma   ·Marketed   epinephrine
Inhalation Aerosol
Euphyllin Retard   ·Asthma·COPD   ·Marketed·Marketed   theophylline
Euphylong             ·Asthma·COPD                                             ·Marketed·Marketed     theophylline




Euroscreen/Alchemia   ·Obesity·Asthma                                          ·ResearchOngoing·Re -
GPCR Program                                                                   searchOngoing




Excellair             ·Asthma·Allergy·ARDS·COPD·Infections,AvianFlu·Antiinfla ·PreClinical·PreClinica -
                      mmatory/Immune                                          l·PreClinical·PreClinic
                                                                              al·PreClinical·PreClini
                                                                              cal
FAR404             ·MS,RelapsingRemitting·Asthma·Crohn'sDisease·Ulcerativ ·RegistrationOngoing· -
                   eColitis·Lupus                                         Phase3Ongoing·Phas
                                                                          e2Ongoing·Phase2On
                                                                          going·Phase1Ongoing




FM-TP3000 Series   ·Asthma·COPD·Hypertension                              ·UndisclosedDiscontin -
                                                                          ued·UndisclosedDisco
                                                                          ntinued·UndisclosedDi
                                                                          scontinued
FOSTER Modulite   ·Asthma·COPD·COPD              ·Marketed·Phase3     beclomethasone
                                                                      dipropionate·
                                                                      formoterol fumarate




FP0522            ·Asthma·COPD·Cancer·Glaucoma   ·ResearchDiscontinue -
                                                 d·ResearchDiscontinu
                                                 ed·ResearchDiscontin
                                                 ued·ResearchDisconti
                                                 nued
Flixotide Diskhaler   ·Asthma                                   ·Marketed             fluticasone propionate




Flo-Pred Oral         ·Antiinflammatory/Immune·Asthma·Allergy   ·Approved·Approved·   prednisolone acetate
Suspension                                                      Approved
Flovent CFC Aerosol   ·Asthma   ·MarketedDiscontinue fluticasone propionate
                                d




Flovent Diskus        ·Asthma   ·Marketed             fluticasone propionate
Flovent-HFA/Flixotide   ·Asthma   ·Marketed   fluticasone propionate
EvoHaler
Fluasterone           ·LipidLowering·Diabetes,Type2·Psoriasis·Asthma·Rheumat ·PreClinical·Research· fluasterone
                      oidArthritis·MultipleSclerosis                         Research·Research·R
                                                                             esearch·Research




Fluticasone Miat-Haler ·Asthma                                                ·PreClinical          fluticasone propionate
Flutiform HFA       ·Asthma        ·RegistrationOngoing   formoterol· fluticasone
                                                          propionate




Foradil AeroLizer   ·Asthma·COPD   ·Marketed·Marketed     formoterol fumarate
Foradil AirMax   ·Asthma·COPD   ·PreClinicalDiscontinu formoterol fumarate
                                ed·PreClinicalDisconti
                                nued
Foradil Certihaler   ·Asthma·COPD   ·MarketedDiscontinue formoterol fumarate
                                    d·MarketedDiscontinu
                                    ed
Formatris        ·Asthma   ·Marketed            formoterol




Formoterol HFA   ·Asthma   ·Phase2Discontinued formoterol fumarate
Formoterol Modulite   ·Asthma    ·Marketed   formoterol fumarate




Formoterol            ·Asthma    ·Phase3     formoterol fumarate
PowderWhirl




Formoterol, Miat-Haler ·Asthma   ·Phase3     formoterol
Foster DPI   ·Asthma·COPD   ·Phase2·Phase2   beclomethasone
                                             dipropionate·
                                             formoterol fumarate
Frenolyn Budesonide   ·Asthma                  ·Marketed               budesonide
DPI




GOIL13s               ·Allergy·Asthma          ·UndisclosedDiscontin -
                                               ued·UndisclosedDisco
                                               ntinued
GRC 3886              ·Asthma·COPD             ·Phase2Ongoing·Phas oglemilast
                                               e2Ongoing


GRO0501               ·Asthma·Psoriasis        ·PreClinical·PreClinica -
                                               lDiscontinued




GSK/Sirna Respiratory ·Asthma·Infections,RSV   ·Research·Research      -
Program

GSK1160724            ·Asthma·COPD             ·Phase1Ongoing·Phas MABA
                                               e1Ongoing
GSK233705 Inhaled   ·COPD·Asthma   ·Phase2Ongoing·Phas darotropium bromide
                                   e1Discontinued




GW597901X           ·COPD·Asthma   ·Phase1Finished·Phas -
                                   e1Finished

GW685698X DPI       ·Asthma        ·Phase2Ongoing       fluticasone furoate
GW685698X/GW6424 ·Asthma·COPD                                               ·Phase2Ongoing·Phas fluticasone furoate
44M Combination                                                             e2Ongoing




Galapagos Drug      ·RheumatoidArthritis·Osteoarthritis·Osteoporosis·Alzheime ·Research·Research· -
Discovery Program   r's·Asthma                                                Research·Research·R
                                                                              esearch
Galileo 5-LO Program ·Asthma·Atherosclerosis                          ·PreClinical·PreClinica -
                                                                      l

Gen-Ipratropium      ·Bronchospasm·Asthma·COPD·Emphysema·Bronchitis   ·Marketed·Marketed· ipratropium bromide
Inhalation                                                            Marketed·Marketed·M hydrate
                                                                      arketed
Gen-Ipratropium   ·Bronchospasm·Asthma·COPD·Bronchitis·Emphysema   ·Marketed·Marketed· ipratropium bromide
Sterinebs                                                          Marketed·Marketed·M hydrate
                                                                   arketed
Gen-Salbutamol         ·Asthma·Bronchospasm   ·Marketed·Marketed   albuterol sulfate
Respirator Solution,
Genpharm




Gen-Salbutamol         ·Bronchospasm·Asthma   ·Marketed·Marketed   albuterol sulfate
Sterinebs




Generex/Stallergenes ·Asthma·Allergy          ·Research·Research   -
Drug Discovery
Program
Generic PULMICORT ·Asthma   ·Approved   budesonide
RESPULES, Apotex
Giona EasyHaler   ·Asthma   ·Marketed   budesonide
Giona                ·Asthma·COPD   ·Phase3·Phase3   budesonide· formoterol
EasyHaler/Formoterol
Combination
Glycopyrrolate   ·Asthma·COPD   ·PreClinicalDiscontinu glycopyrrolate bromide
Novolizer                       ed·PreClinicalDisconti
                                nued




HAE1             ·Asthma        ·Phase2Discontinued -
HF 1020           ·RheumatoidArthritis·IBD·Asthma   ·PreClinicalDiscontinu -
                                                    ed·PreClinicalDisconti
                                                    nued·PreClinicalDisco
                                                    ntinued




HFA Combination   ·Asthma                           ·PreClinicalDiscontinu undisclosed small
Product                                             ed                     molecule· undisclosed
                                                                           small molecule
HIV, Cardio, Asthma,   ·Infections,HIV/AIDS·Asthma·COPD   ·ResearchOngoing·Re -
COPD Program,                                             searchOngoing·Resea
Spring Bank                                               rchOngoing
HSP20 Hit Series       ·Asthma·COPD                       ·PreClinicalOngoing·P -
                                                          reClinicalOngoing
Hokunalin Tape       ·Asthma·COPD·Bronchitis   ·Marketed·Marketed·   tulobuterol
                                               Marketed




Hutchison             ·Asthma                  ·Research             -
Inflammation/pulmonar
y Program
IG-RD-001            ·Asthma                                   ·Phase3               -


IG-RD-002            ·Asthma                                   ·PreClinical          -


IG-RD-003            ·Asthma                                   ·Undisclosed          -


IG-RD-004            ·Asthma·COPD                              ·Undisclosed·Undisclo -
                                                               sed

IL-4 and IL-13       ·Asthma                                   ·Research             -
Blocking Peptide
Program, Synairgen



IL-4/13 Trap         ·Allergy·Asthma·Antiinflammatory/Immune   ·Phase1Discontinued· -
                                                               Phase1Discontinued·
                                                               Phase1Discontinued
IL13-PE38QQR          ·Cancer,Glioma/GlioblastomaMultiform·Asthma·IdiopathicP ·Phase3Finished·PreC cintredekin besudotox
                      ulmonaryFibrosis                                        linical·PreClinical




IL4 Target Program,   ·Asthma·Allergy                                        ·ResearchOngoing·Re -
Cosmix                                                                       searchOngoing
IL5Qb                 ·Asthma                                                ·PreClinicalFinished -
IMA-638        ·Asthma                            ·Phase1               anrukinzumab


INV102         ·Asthma                            ·Phase2Ongoing        nadolol




IPD Capsules   ·Allergy·Asthma·AtopicDermatitis   ·Marketed·Marketed·   suplatast tosilate
                                                  Marketed
IPD Dry Syrup          ·Asthma·Allergy·AtopicDermatitis   ·Marketed·Marketed·   suplatast tosilate
                                                          Marketed




IPL512,602             ·Asthma                            ·Phase2Discontinued -




IPL576,092             ·Asthma                            ·Phase2Discontinued -




Icatibant Inhalation   ·Asthma                            ·Phase2               icatibant




Inflammasome           ·RheumatoidArthritis·Gout·Asthma   ·ResearchOngoing·Re -
Program, Opsona                                           searchOngoing·Resea
                                                          rchOngoing
Inflammide Novolizer   ·Asthma    ·Marketed              budesonide




Inhale Interleukin-1    ·Asthma   ·UndisclosedDiscontin -
Receptor Program                  ued
Inhaled Albuterol, Next ·Asthma   ·PreClinical          albuterol sulfate
Safety




Inhaled ISS for        ·Asthma    ·Phase2                -
Asthma
Intal Aerosol A   ·Asthma   ·Marketed   cromolyn sodium
Intal Capsules 20mg   ·Asthma·Allergy   ·Marketed·Marketed   cromolyn sodium
Intal HFA   ·Asthma   ·UndisclosedDiscontin cromolyn sodium
                      ued
Intal Inhaler   ·Asthma   ·Marketed   cromolyn sodium
Intal Nebulizer Solution ·Asthma   ·Marketed   cromolyn sodium
Intal Nebulizer       ·Asthma   ·Marketed   cromolyn sodium
Solution, Generic Dey
Intal Nebulizer     ·Asthma   ·Marketed   cromolyn sodium
Solution, Generic
Morton Grove
Intal SpinCap   ·Asthma   ·Marketed   cromolyn sodium
Intal-Forte CFC Free   ·Asthma   ·Marketed   cromolyn sodium
Ipratropium Cyclohaler ·Asthma   ·Marketed   ipratropium bromide
                                             hydrate
Ipratropium           ·Asthma·COPD   ·MarketedDiscontinue ipratropium bromide
Steripoules Nebuliser                d·MarketedDiscontinu hydrate
Solution                             ed
IsoCrom   ·Asthma                        ·Phase2Ongoing        sodium cromoglycate




J51C      ·Asthma                        ·Research             -

KB002     ·RheumatoidArthritis·Asthma    ·Phase1·PreClinical   -




KCA-757   ·Asthma·InterstitialCystitis   ·Phase3Ongoing·Phas tipelukast
                                         e2
KI03219     ·Asthma·COPD             ·PreClinical·PreClinica undisclosed small
                                     l                       molecule· undisclosed
                                                             small molecule




KI04204     ·Asthma                  ·PreClinical            -

KM 278      ·Osteoarthritis·Asthma   ·PreClinical·PreClinica -
                                     l

KP-496DPI   ·Asthma                  ·Phase2Discontinued -
KPE06001   ·Asthma·Arthritis          ·Phase1Ongoing·Phas -
                                      e1Ongoing
KUR-1246   ·PregnancyRelated·Asthma   ·Phase1·Phase2      bedoradrine sulfate
KW-4490           ·Asthma                         ·Phase2                 -




Ketas Capsules    ·Asthma·CNS·MultipleSclerosis   ·Marketed·Marketed·P ibudilast
                                                  hase2Finished




L-97-1, Inhaled   ·Asthma                         ·PreClinical            -

L-97-1, Oral      ·Infections,Bacterial·Asthma    ·PreClinical·PreClinica -
                                                  l
LAS 101057        ·Asthma                         ·Phase1Discontinued -

LAS 186368        ·Asthma·COPD                    ·PreClinical·PreClinica -
                                                  l
LAS100977         ·Asthma·COPD                    ·Phase2Ongoing·Phas -
                                                  e2Ongoing




Laevo-Bambutero   ·Asthma                         ·Phase1                 -
Laonian Kechuan      ·Asthma                      ·Marketed               -
Tablets

Leech-derived        ·Asthma·AutoimmuneDiseases   ·PreClinical·PreClinica -
Tryptase Inhibitor                                l
Lodotra             ·RheumatoidArthritis·Asthma·PolymyalgiaRheumatica   ·Approved·Phase2On prednisone
                                                                        going·Phase1




Long-Acting Beta    ·Asthma·COPD                                        ·PreClinical·PreClinica -
Agonists Program,                                                       l
Sepracor
Loteprednol Etabonate ·Allergy·Asthma   ·Phase2·Phase2   loteprednol etabonate
Nasal Spray
Loteprednol Etabonate ·Asthma   ·PreClinicalDiscontinu loteprednol etabonate
Novolizer                       ed
Lufyllin Tablets   ·Asthma   ·Marketed   diphylline
Lumiliximab/Anti-CD23 ·Asthma·Allergy                                 ·Phase1Discontinued· lumiliximab
mAb                                                                   Phase1Discontinued




M40403                ·PostOperativeIleus·OralMucositis·Asthma·COPD   ·Phase1·Phase1·Phas -
                                                                      e1·Phase1


MAP Inhaled Steroids ·Asthma                                          ·PreClinical         -
MAP0005   ·Asthma·COPD      ·Phase2Ongoing·Phas budesonide· formoterol
                            e2Ongoing




MCC-847   ·Asthma·Allergy   ·Phase3·Phase2       -
MEDI-528   ·Asthma                                               ·Phase2              -




MEM 1414   ·Asthma·Depression·MildCognitiveImpairment·Dementia·Al ·Phase2Ongoing·Phas -
           zheimer's                                              e1·Phase1Finished·P
                                                                  hase1Finished·Phase
                                                                  1Finished
MEPTIN Air 10 ug   ·Asthma·Bronchitis   ·Marketed·Marketed   procaterol
                                                             hydrochloride
MEPTIN Drysyrup   ·Asthma·Bronchitis   ·Marketed·Marketed   procaterol
0.005%                                                      hydrochloride
MEPTIN Granules   ·Asthma·Bronchitis   ·Marketed·Marketed   procaterol
                                                            hydrochloride
MEPTIN Inhalation   ·Asthma·Bronchitis   ·Marketed·Marketed   procaterol
Solution                                                      hydrochloride
MEPTIN Kid Air 5 ug   ·Asthma·Bronchitis   ·Marketed·Marketed   procaterol
                                                                hydrochloride
MEPTIN Syrup   ·Asthma·Bronchitis   ·Marketed·Marketed   procaterol
                                                         hydrochloride
MEPTIN Tablets   ·Asthma·Bronchitis   ·Marketed·Marketed   procaterol
                                                           hydrochloride
MEPTIN-Mini Tablets   ·Asthma·Bronchitis   ·Marketed·Marketed   procaterol
                                                                hydrochloride
MK-0633             ·Asthma·Atherosclerosis·COPD                    ·Phase2Ongoing·Phas etoricoxib
                                                                    e2OnHold·Phase2On
                                                                    going




MK6105              ·Asthma                                         ·PreClinical            -




MLN6095             ·Asthma·Allergy                                 ·PreClinicalDiscontinu -
                                                                    ed·PreClinicalDisconti
                                                                    nued
MN-001 Once A Day   ·Asthma·InterstitialCystitis                    ·Undisclosed·Undisclo tipelukast
                                                                    sed

MORAb-022           ·RheumatoidArthritis·MultipleSclerosis·Asthma   ·PreClinical·PreClinica -
                                                                    l·PreClinical
MP41                ·Respiratory·Asthma                             ·PreClinical·PreClinica -
                                                                    l




MP8                 ·Sepsis·Asthma·MultipleSclerosis                ·PreClinical·PreClinica -
                                                                    l·PreClinical
MaxAir AutoHaler   ·Asthma   ·Marketed   pirbuterol acetate
Meptin Clickhaler    ·Asthma        ·Marketed               procaterol
                                                            hydrochloride




Miat-Haler           ·Asthma        ·PreClinical            -
Combinations

Microdose/Novartis   ·Asthma·COPD   ·PreClinical·PreClinica -
Program                             l
Miflonide AirMax   ·Asthma   ·UndisclosedDiscontin budesonide
                             ued
Mometasone/Formoter ·Asthma·COPD   ·Registration·Registrat mometasone furoate·
ol Combination MDI                 ion                     formoterol
Montelukast Injection   ·Asthma                                                ·Phase3              montelukast sodium




N115                    ·COPD·CysticFibrosis·InterstitialLungDisease·Emphysema· ·Phase2Finished·Phas sodium pyruvate
                        Asthma·Bronchitis                                       e1Ongoing·Undisclos
                                                                                ed·Undisclosed·Phase
                                                                                2Ongoing·Undisclose
                                                                                d
N30-201              ·CysticFibrosis·Asthma                                  ·Phase1·Phase1         -




NAL6266 3 Day Patch ·Asthma                                                  ·Undisclosed           -

NL6328 1 Day Patch   ·Asthma                                                 ·Undisclosed           tulobuterol




NM100100             ·Asthma                                                 ·PreClinicalDiscontinu -
                                                                             ed
NS-126               ·Allergy·Asthma                                         ·Phase3·Phase2         -


NT-702               ·IntermittentClaudication·PeripheralVascularDiseases·Asth ·Phase3Ongoing·Phas -
                     ma                                                        e2·Phase2
Naturasone   ·Asthma·COPD·Allergy   ·Phase2·Phase2·Phas -
                                    e1
Neophyllin Injection   ·Asthma·Bronchitis·HeartFailure·PulmonaryEdema·Angina ·Marketed·Marketed· aminophylline
                       Pectoris·CerebralPalsy                                Marketed·Marketed·M
                                                                             arketed·Marketed
Neophyllin Powder   ·Asthma·Bronchitis·Respiratory·HeartFailure   ·Marketed·Marketed·   aminophylline
                                                                  Marketed·Marketed
Neophyllin Tablets   ·Asthma·Bronchitis·Respiratory·HeartFailure   ·Marketed·Marketed·   aminophylline
                                                                   Marketed·Marketed
Nepadutant Injectable ·Asthma·IBD                                       ·Phase2·Phase2          nepadutant




Neu-105              ·Asthma·COPD·Alzheimer's                           ·PreClinical·PreClinica -
                                                                        l·PreClinical




Neutrazumab          ·RheumatoidArthritis·Stroke·Asthma·COPD·SLE·Rheumat ·Phase1·Phase1·Phas neutrazumab
                     oidArthritis                                        e1·Phase1·Phase1·Ph
                                                                         ase1
Neuzym Fine Granules ·Sinusitis·Periodontitis/Gingivitis·Bronchitis·Asthma·Bronchi ·Marketed·Marketed· lysozyme
                     ectasis                                                       Marketed·Marketed·M hydrochloride
                                                                                   arketed
Neuzym Granules   ·Sinusitis·Periodontitis/Gingivitis·Bronchitis·Asthma·Bronchi ·Marketed·Marketed· lysozyme
                  ectasis                                                       Marketed·Marketed·M hydrochloride
                                                                                arketed
Neuzym Tablets       ·Sinusitis·Periodontitis/Gingivitis·Bronchitis·Asthma·Bronchi ·Marketed·Marketed· lysozyme
                     ectasis                                                       Marketed·Marketed·M hydrochloride
                                                                                   arketed




Nitric Oxide-Enhancing ·Cancer·PainManagement·CNS·Asthma·ErectileDysfunctio ·Research·Research· -
PDE Inhibitors         n·PulmonaryHypertension                              Research·Research·R
                                                                            esearch·Research
Nitric Oxide-Enhancing ·Allergy·Asthma   ·Research·Research   -
Steroids




Novopulmon            ·Asthma·COPD       ·Marketed            budesonide
Nuelin SA Tablets   ·Bronchospasm·Asthma·COPD   ·Marketed·Marketed·     theophylline
                                                Marketed




ODC9101             ·Asthma                     ·Phase2                 -

OX-2477             ·Asthma·COPD                ·PreClinical·PreClinica -
                                                l

OX-914              ·Asthma·COPD·Allergy        ·Phase2Ongoing·Phas -
                                                e2Ongoing·Phase2On
                                                going



OX-CLI              ·Asthma·COPD·Allergy        ·PreClinical·PreClinica -
                                                l·PreClinical
OX-LSAID         ·Asthma                                        ·Phase2                 -




OX40             ·Cancer·Infections·AutoimmuneDiseases·Asthma   ·PreClinical·PreClinica -
                                                                l·PreClinical·PreClinic
                                                                al




OX40, La Jolla   ·Asthma                                        ·Research               -
OX914            ·COPD·Asthma·Allergy   ·Phase2·Phase2·Phas -
                                        e2




Omron MicroAir   ·Asthma·COPD           ·Marketed·Marketed   -
Nebulizer
Onon Capsules   ·Asthma·Allergy·COPD·Sinusitis   ·Marketed·Marketed·P pranlukast hydrate
                                                 hase2·Phase3Disconti
                                                 nued
Onon Dry Syrup   ·Asthma   ·Marketed      pranlukast hydrate




Optime Topical   ·Asthma   ·Undisclosed   -
Asthma
OraPred Oral Solution ·Asthma·Allergy·SkinAntiinflammatory·Cancer,Leukemia·E ·Marketed·Marketed· prednisolone sodium
                      yeAntiinflammatory·RheumatoidArthritis                 Marketed·Marketed·M phosphate
                                                                             arketed·Marketed
Orapred ODT           ·Asthma·Allergy·SkinAntiinflammatory·Cancer,Leukemia·E ·Marketed·Marketed· prednisolone sodium
                      yeAntiinflammatory·RheumatoidArthritis                 Marketed·Marketed·M phosphate
                                                                             arketed·Marketed




Osonide HFA Inhaler   ·Asthma                                               ·Marketed            ciclesonide
Oxagen GPCR       ·Antiinflammatory/Immune·IBD·RheumatoidArthritis·Psoria ·Undisclosed·Undisclo -
Program           sis·Asthma                                              sed·Undisclosed·Undi
                                                                          sclosed·Undisclosed

Oxis Turbohaler   ·Asthma·COPD                                            ·Marketed             formoterol fumarate




PAC-G31P          ·ARDS·Asthma·COPD                                       ·PreClinicalOngoing·P -
                                                                          reClinicalOngoing·Pre
                                                                          ClinicalOngoing



PF-3893787        ·Asthma                                                 ·Phase1Ongoing        -
PF-4191834         ·Asthma                                             ·Phase2Ongoing       -




PF-610355          ·Asthma·COPD                                        ·Phase2·Phase2       -

PI3 Kinase delta   ·RheumatoidArthritis·Asthma·Cancer,Haematological   ·PreClinicalOngoing·R -
inhibitor                                                              esearchOngoing·PreC
                                                                       linicalOngoing
PLA-695            ·Asthma·RheumatoidArthritis·Osteoarthritis          ·Phase1·Phase1·Phas giripladib
                                                                       e1




POL6014            ·COPD·Asthma                                        ·ResearchOngoing·Re -
                                                                       searchOngoing
PROAIR HFA   ·Asthma·Bronchospasm   ·Marketed·Marketed   albuterol sulfate
PRS-060    ·Asthma                                                  ·PreClinical           -




PS291822   ·COPD·Asthma·Psoriasis                                   ·Phase2·Phase2·Phas -
                                                                    e2




PS460644   ·Asthma·Allergy                                          ·Phase1·Phase1         -


PW3101     ·Asthma                                                  ·UndisclosedDiscontin -
                                                                    ued




PXS25      ·IdiopathicPulmonaryFibrosis·Asthma·MultipleSclerosis·Ac ·PreClinicalFinished·P -
           uteLungInjury                                            reClinicalOngoing·Pre
                                                                    ClinicalOngoing·PreCli
                                                                    nicalOngoing
PXS4159    ·Asthma                                                  ·PreClinicalOngoing    -
PXS64                   ·MultipleSclerosis·Asthma·AcuteLungInjury                ·PreClinical·PreClinica -
                                                                                 l·PreClinical




PXS74                   ·Asthma                                                 ·Research               -
Palau Pharma DP-1       ·Asthma·AtopicDermatitis·SLE·MultipleSclerosis·OrganTra ·PreClinical·PreClinica -
                        nsplantation                                            l·PreClinical·PreClinic
                                                                                al·PreClinical
Phyllocontin Continus   ·Asthma                                                 ·Marketed               aminophylline
                                                                                                        dihydrate
Phyllocontin Forte   ·Asthma   ·Marketed   aminophylline
Continus                                   dihydrate
Phyllocontin Pediatric   ·Asthma                                          ·Marketed               aminophylline
Continus                                                                                          dihydrate




Phylogica/Opsona    ·Asthma·AutoimmuneDiseases·AtopicDermatitis·Antiinflam ·ResearchOngoing·Re -
Discovery Programme matory/Immune                                          searchOngoing·Resea
                                                                           rchOngoing·Research
                                                                           Ongoing



Phytopharma Asthma       ·Asthma·COPD                                     ·PreClinical·PreClinica -
Program                                                                   l
Pleconaril   ·Infections,Viral·Asthma·CoughandCold   ·Phase2·Phase2·Phas pleconaril
                                                     e2
PreHistin Sublingual   ·Allergy·Migraine·Asthma·AtopicDermatitis   ·Phase3·Phase2·Undi cyanocobalamin
Lozenge                                                            sclosed·Undisclosed
Premaire Albuterol    ·Asthma   ·Phase2Discontinued albuterol sulfate




Premaire Budesonide   ·Asthma   ·Phase1Discontinued budesonide
Premaire Sodium   ·Asthma   ·PreClinicalDiscontinu sodium cromoglycate
Cromoglycate                ed
Primatene Mist   ·Asthma   ·Marketed   epinephrine
ProAir EasiBreathe   ·Asthma·Bronchospasm   ·Registration·Registrat albuterol sulfate
                                            ion




Profilar Tablets     ·Asthma                ·Marketed               ketotifen fumarate
Proteomics          ·Asthma   ·Research             -
Program,Synairgen




Proventil CFC       ·Asthma   ·MarketedDiscontinue albuterol sulfate
                              d
Proventil-HFA   ·Asthma   ·Marketed   albuterol sulfate
Pulmicort HFA       ·Asthma   ·Marketed   budesonide




Pulmicort Inhaler   ·Asthma   ·Marketed   budesonide
Pulmicort Respules    ·Asthma   ·Marketed   budesonide




Pulmicort Respules,   ·Asthma   ·Marketed   budesonide
Generic Par Pharma
Pulmicort TurboHaler   ·Asthma        ·Marketed             budesonide




PulmoSphere            ·Asthma        ·UndisclosedDiscontin albuterol
Albuterol                             ued




QAB149 CertiHaler      ·COPD·Asthma   ·Phase3Discontinued· indacaterol
                                      Phase3Discontinued




QAE397                 ·Asthma        ·Phase2             -
QAP642                 ·Asthma        ·Phase1Discontinued -
QAX935   ·Asthma·Allergy   ·Phase1·Phase1   -




QMF149   ·COPD·Asthma      ·Phase2·Phase2   indacaterol·
                                            mometasone furoate
Qvar 50 and 100 MDI   ·Asthma   ·Marketed   beclomethasone
                                            dipropionate




Qvar AutoHaler        ·Asthma   ·Marketed   beclomethasone
                                            dipropionate
Qvar Easi-Breathe   ·Asthma   ·Marketed   beclomethasone
                                          dipropionate




Qvar HFA            ·Asthma   ·Marketed   beclomethasone
                                          dipropionate
R1671         ·Asthma        ·Phase1Ongoing        -




R343, Rigel   ·Asthma·COPD   ·Phase1·PreClinical   -
R411      ·Asthma        ·Phase2               valategrast
                                               hydrochloride




R4930     ·Asthma        ·Phase1Ongoing        -




RESP001   ·Asthma·COPD   ·Phase1Finished·Phas albuterol sulfate
                         e1Finished
RIZABEN Dry syrup   ·Asthma·Allergy·AtopicDermatitis   ·Marketed·Marketed·   tranilast
                                                       Marketed
RIZABEN Fine   ·Asthma·Allergy·AtopicDermatitis                     ·Marketed·Marketed·     tranilast
granules                                                            Marketed




RPL554 Nasal   ·Antiinflammatory/Immune·Bronchitis·Allergy·Asthma   ·PreClinical·PreClinica -
                                                                    l·PreClinical·Phase1
RX-10001              ·Asthma·IBD·RheumatoidArthritis·Cardiovascular   ·PreClinical·PreClinica -
                                                                       l·PreClinical·PreClinic
                                                                       al




Racepinephrine        ·Asthma                                          ·Marketed               racepinephrine
Inhalation Solution
Reslizumab    ·Esophagitis·Asthma   ·Phase3Ongoing·Phas reslizumab
                                    e2Ongoing




Respicort     ·Asthma               ·Phase2              etiprednol dicloacetate




Respivert     ·Asthma·COPD          ·Research·Research   -
Asthma/COPD
Respontin Nebules   ·Asthma                                 ·Marketed           ipratropium bromide
                                                                                hydrate




Respriva            ·Emphysema·COPD·CysticFibrosis·Asthma   ·Phase2·Phase1·PreC -
                                                            linical·PreClinical
Rizaben Tablets       ·Allergy·Asthma   ·Marketed·Marketed   tranilast




Romet Fine Granules   ·Asthma           ·Marketed            repirinast
For Children


Romet Tablets         ·Asthma           ·Marketed            repirinast
S-5751       ·Asthma                               ·Phase2Discontinued S-5751


SAR 398171   ·Asthma                               ·PreClinicalDiscontinu   -
                                                   ed
SAR137272    ·Asthma·COPD                          ·PreClinicalOngoing·P    -
                                                   reClinicalOngoing
SAR21609     ·Asthma·Infections,RespiratoryTract   ·Phase1Ongoing·Phas      -
                                                   e1Ongoing
SAR389644    ·Asthma·Allergy                       ·Phase1Ongoing·Phas      -
                                                   e1Ongoing
SG003        ·Asthma                               ·Phase1                  interferon beta




SG004        ·Asthma·COPD                          ·Phase1Ongoing·Phas interferon beta
                                                   e1Ongoing




SG005        ·Asthma·COPD                          ·Phase1·Phase1      -
SG006        ·Asthma·COPD                          ·Phase1·Undisclosed -

SG007        ·Asthma                               ·Undisclosed             -
SG008        ·Asthma                               ·Undisclosed             -
SMP-028     ·Asthma        ·Phase1                -




SNG-1       ·Asthma        ·Phase1                interferon beta




SNG-3       ·Asthma        ·PreClinical           -




SRP312      ·Asthma        ·ResearchDiscontinue -
                           d




SSR161421   ·Asthma·COPD   ·PreClinicalDiscontinu -
                           ed·PreClinicalDisconti
                           nued
SUN-S 461   ·Asthma·COPD   ·PreClinicalOngoing·P -
                           reClinicalOngoing
Salamol Easi Breathe   ·Bronchospasm·Asthma   ·Marketed·Marketed    albuterol
CFC Free




Salamol Easi Breathe   ·Bronchospasm·Asthma   ·UndisclosedDiscontin albuterol
                                              ued·UndisclosedDisco
                                              ntinued
Salbunova HFA        ·Asthma    ·Marketed      albuterol




Salbutamol Cyclohaler ·Asthma   ·Marketed      albuterol




Salbutamol HFA, Inyx ·Asthma    ·PreClinical   albuterol
Salbutamol          ·Asthma·Bronchitis·Emphysema   ·Marketed·Marketed·   albuterol
Steripoules                                        Marketed




Salbutamol Taifun   ·Asthma                        ·Marketed             albuterol
Senicapoc        ·Asthma·Antiinflammatory/Immune·SickleCell   ·Phase2Ongoing·PreC senicapoc
                                                              linical·Phase3Disconti
                                                              nued




Sepracor/Arrow   ·Asthma                                      ·Research           ciclesonide
Ciclesonide
Seretide EvoHaler   ·Asthma   ·Marketed   salmeterol xinafoate·
                                          fluticasone propionate
Serevent Diskhaler   ·Asthma·COPD   ·Marketed·Marketed   salmeterol xinafoate
Serevent Diskus     ·Asthma·COPD   ·Marketed            salmeterol xinafoate




Serevent Evohaler   ·Asthma·COPD   ·Marketed·Marketed   salmeterol xinafoate
Serevent Inhalation   ·Asthma   ·MarketedDiscontinue salmeterol xinafoate
Aerosol - CFC                   d
Simponi   ·RheumatoidArthritis·AnkylosingSpondylitis·PsoriaticArthriti ·Approved·Approved· golimumab
          s·Asthma·UlcerativeColitis                                   Approved·Phase2·Pha
                                                                       se3
Singulair Chewable   ·Asthma·Allergy   ·Marketed·Marketed   montelukast sodium
Tablets
Singulair Granules   ·Asthma·Allergy   ·Marketed·Marketed   montelukast sodium
Singulair Tablets   ·Asthma·Allergy   ·Marketed·Marketed   montelukast sodium




Sirna Asthma Program ·Asthma          ·PreClinical         -
Solfa Tablets   ·Asthma·Allergy   ·Marketed·Marketed   amlexanox
Spiriva Respimat   ·Asthma·COPD   ·Marketed·Marketed   tiotropium bromide
                                                       monohydrate
Spiriva   ·Asthma·COPD·CysticFibrosis   ·Marketed·Marketed·U tiotropium bromide
                                        ndisclosed           monohydrate
Spiropent Tablets   ·Asthma·OveractiveBladder   ·Marketed·Marketed   clenbuterol
                                                                     hydrochloride
Symbicort SMART   ·Asthma·COPD   ·Marketed·Approved   budesonide· formoterol
MDI                                                   fumarate dihydrate
Symbicort Turbuhaler   ·Asthma·COPD   ·Marketed·Marketed   budesonide· formoterol
Synairgen Inhaled    ·Asthma                                                 ·Research               -
Growth Factor




Synta/Roche          ·Antiinflammatory/Immune·RheumatoidArthritis·Asthma·C   ·PreClinical·PreClinica -
Inflammatory Program OPD·Allergy                                             l·PreClinical·PreClinic
                                                                             al·PreClinical

TARG-ALLERG I-200 ·Asthma                                                    ·Undisclosed            -




TARG-ALLERG I-201 ·Asthma                                                    ·Undisclosed            -
TARG-ALLERG I-202 ·Asthma                            ·Undisclosed          -




TBC1269           ·COPD·Asthma·Psoriasis·ARDS        ·Phase2Ongoing·Phas bimosiamose
                                                     e2Ongoing·Phase2On
                                                     going·Phase1Finished

TBC4095           ·Asthma                            ·UndisclosedDiscontin -
                                                     ued
TBC4746           ·Asthma                            ·Phase1               -

TG100115          ·Cardiovascular·Asthma             ·Phase1·PreClinical   -




TJ-29             ·CoughandCold·Bronchitis·Asthma    ·Marketed·Marketed·   -
                                                     Marketed
TNX-650           ·Cancer,Hodgkin'sLymphoma·Asthma   ·Phase1·Phase1        -




TPI-1020          ·Asthma·COPD                       ·Phase2·Phase2Disco nitric oxide-donating
                                                     ntinued             derivative of
                                                                         budesonide
TPI-ASM8           ·Asthma   ·Phase2Ongoing   -




TRPA1 antagonist   ·Asthma   ·PreClinical     -
Program, Hydra
TUSSI-12D    ·CoughandCold·Asthma·Bronchitis   ·Marketed·Marketed·   carbetapentane
Suspension                                     Marketed              tannate· pyrilamine
                                                                     tannate· phenylephrine
                                                                     tannate
TUSSI-12D Tablet    ·CoughandCold·Asthma·Bronchitis   ·Marketed·Marketed·   carbetapentane
                                                      Marketed              tannate· pyrilamine
                                                                            tannate· phenylephrine
                                                                            tannate




Taifun Budesonide   ·Asthma                           ·Phase3               budesonide
Taifun Formoterol   ·Asthma   ·Phase1     formoterol




Taunus DPI          ·Asthma   ·Marketed   beclomethasone
                                          dipropionate




Tempo Fluticasone   ·Asthma   ·Phase1     fluticasone propionate
Teosona SOL   ·Asthma   ·Marketed   theophylline
Terbutaline Mystic   ·Asthma·COPD   ·UndisclosedDiscontin terbutaline sulfate
                                    ued·UndisclosedDisco
                                    ntinued
Theo-Dur Extended   ·Asthma·Bronchitis   ·MarketedDiscontinue theophylline
Release Tablets                          d·MarketedDiscontinu
                                         ed
Theo-Dur Sprinkle   ·Asthma   ·MarketedDiscontinue theophylline
Sustained Action              d
Capsules
TheoDur, Generic Able ·Asthma   ·MarketedDiscontinue theophylline
                                d




TheoDur, Generic URL ·Asthma    ·Marketed            theophylline
Theolin SR Capsules   ·Asthma   ·Marketed   theophylline
Theolong SR Granules ·Asthma·Bronchitis   ·Marketed·Marketed   theophylline
Theolong SR Tablets   ·Asthma·Bronchitis   ·Marketed·Marketed   theophylline
Theophyline LP     ·Asthma   ·PreClinical   theophylline




Theophylline CDT   ·Asthma   ·PreClinical   theophylline
Theophylline ER     ·Asthma   ·Marketed   theophylline
Capsules Generic,
Forest




Theophylline ER     ·Asthma   ·Marketed   theophylline
Tablets Generic,
Forest
Tilade CFC Free   ·Asthma   ·Marketed   nedocromil sodium
Inhaler
Tilade Inhalation   ·Asthma·Asthma   ·MarketedDiscontinue nedocromil sodium
Aerosol - CFC                        d·Marketed
Triamicinolone Mystic   ·Asthma·COPD   ·UndisclosedDiscontin triamcinolone
                                       ued·UndisclosedDisco acetonide
                                       ntinued




Tulobuterol Tape        ·Asthma        ·Marketed             tulobuterol
EMEC
Tulobuterol-TDS        ·Asthma        ·Phase1                 tulobuterol




Undisclosed Captisol   ·Asthma·COPD   ·PreClinical·PreClinica -
Inhalation                            l


Undisclosed            ·Asthma        ·PreClinicalDiscontinu -
compound, Ventaira                    ed


Undisclosed            ·Asthma        ·PreClinicalDiscontinu -
compound,                             ed
Ventaira/Abbott
Undisclosed            ·Asthma        ·PreClinicalDiscontinu -
compound,                             ed
Ventaira/Viasys
Uniphyl Tablets     ·Asthma·Bronchitis·Emphysema   ·Marketed·Marketed·   theophylline
                                                   Marketed




Unit Dose Budesonide ·Asthma                       ·Phase3Ongoing        budesonide




Uriach Asthma       ·Asthma                        ·Research             -
Program
VR315   ·Asthma        ·Phase2                undisclosed small
                                              molecule· undisclosed
                                              small molecule




VR632   ·Asthma·COPD   ·Phase2·Phase2         -




VR694   ·Asthma        ·PreClinicalDiscontinu -
                       ed
Vaccines Against       ·Asthma·Allergy                                         ·PreClinicalDiscontinu -
Allergy and Allergic                                                           ed·PreClinicalDisconti
Asthma                                                                         nued
Vagonixen              ·Asthma·COPD                                            ·PreClinical·PreClinica -
                                                                               l




Vantox                 ·Asthma·CysticFibrosis·ARDS·Antiinflammatory/Immune·E ·PreClinical·PreClinica -
                       mphysema·COPD                                         l·PreClinical·PreClinic
                                                                             al·PreClinical·PreClini
                                                                             cal
Vectura/BI DPI   ·Asthma·COPD   ·PreClinical·PreClinica -
Program                         l
Ventide Inhaler   ·Asthma   ·Marketed   albuterol·
                                        beclomethasone
                                        dipropionate
Ventide Rotocaps   ·Asthma   ·Marketed   albuterol sulfate·
                                         beclomethasone
                                         dipropionate
Ventilastin Novolizer   ·Asthma   ·Marketed   albuterol
Ventodisks   ·Asthma   ·Marketed   albuterol sulfate
Ventolin Accuhaler   ·Asthma·Bronchospasm   ·Marketed·Marketed   albuterol sulfate
Ventolin Inhalation   ·Asthma·Bronchospasm   ·MarketedDiscontinue albuterol
Aerosol - CFC                                d·MarketedDiscontinu
                                             ed
Ventolin Inhalation   ·Asthma                ·Marketed            albuterol
Aerosol - CFC,
Generic Armstrong




Ventolin Inhaled      ·Bronchospasm·Asthma   ·Marketed·Marketed   albuterol sulfate
Solution
Ventolin Nebules    ·Bronchospasm·Asthma   ·Marketed·Marketed   albuterol sulfate




Ventolin RotoCaps   ·Asthma·Bronchospasm   ·Marketed·Marketed   albuterol sulfate
Ventolin Syrup   ·Asthma   ·Marketed   albuterol sulfate
Ventolin-HFA   ·Asthma   ·Marketed   albuterol sulfate
Veramyst                ·Allergy·Asthma   ·Marketed·Phase2Ong fluticasone furoate
                                          oing




Verus Short-Acting      ·Asthma           ·Undisclosed         -
Beta Agonist Solution
Volare Easi-Breathe   ·Asthma   ·Phase3       albuterol




Volare MDI            ·Asthma   ·Approvable   albuterol
Volmax Tablets         ·Asthma·Bronchospasm   ·Marketed·Marketed   albuterol sulfate




Xcelovair Formoterol   ·Asthma                ·Phase1              formoterol
Xolair Injection       ·Asthma·Allergy   ·Marketed·Phase2   omalizumab




Xolair Prefilled Syringe ·Asthma         ·Phase2            omalizumab
Xopenex HFA   ·Asthma·COPD   ·Marketed·Marketed   levalbuterol tartrate
Xopenex Inhalation    ·Asthma   ·Approved   levalbuterol
Solution, Generic Dey                       hydrochloride
ZYFLO Tablets   ·Asthma·COPD   ·Marketed·Phase3   zileuton
Zenapax               ·OrganTransplantation·MultipleSclerosis·GVHD·Asthma·M ·Marketed·Phase2Ong daclizumab
                      S,RelapsingRemitting                                  oing·Undisclosed·Pha
                                                                            se2Discontinued·Phas
                                                                            e2




Zesulan Fine Granules ·Asthma·Allergy                                      ·Marketed·Marketed   -
0.6%
Zesulan Syrup       ·Asthma·Allergy                   ·Marketed·Marketed    mequitazine


Zesulan Tablet      ·Asthma·Allergy                   ·Marketed·Marketed    mequitazine


Zileuton I.V.       ·Asthma                           ·Phase2Ongoing        zileuton




Znomics/OHSU Drug   ·RheumatoidArthritis·Asthma·IBD   ·PreClinical·PreClinica -
Discovery Program                                     l·PreClinical
Zofac               ·Asthma                           ·Phase2                 pumactant
Zyflo CR   ·Asthma   ·Marketed   zileuton
aeroSRT           ·CysticFibrosis·AcuteLungInjury·COPD·Asthma   ·Phase2Ongoing·PreC -
                                                                linical·Research·Rese
                                                                arch




anti YKL40 MAb,   ·Asthma·COPD                                  ·PreClinical·PreClinica   -
Medimmune                                                       l
cgi1316           ·RheumatoidArthritis·SLE·Asthma               ·UndisclosedDiscontin     -
                                                                ued·UndisclosedDisco
                                                                ntinued·UndisclosedDi
                                                                scontinued
cgi1746           ·RheumatoidArthritis·SLE·Asthma               ·UndisclosedDiscontin     -
                                                                ued·UndisclosedDisco
                                                                ntinued·UndisclosedDi
                                                                scontinued
deCODE Asthma     ·Asthma                                       ·Phase2                   -
Program
rEV131   ·ARDS·DryEye·Asthma·EyeAntiinflammatory·Allergy   ·PreClinical·Phase2Di -
                                                           scontinued·Phase2Dis
                                                           continued·Phase2Disc
                                                           ontinued·Phase2Disco
                                                           ntinued




rhAAT    ·Emphysema·CysticFibrosis·COPD·Asthma·ARDS        ·PreClinicalOngoing·P alpha-1 antitrypsin,
                                                           reClinicalOngoing·Res recombinant human
                                                           earch·PreClinicalOngo
                                                           ing·PreClinicalOngoin
                                                           g
rhuMAb-OX40L            ·Asthma   ·Phase1        -




ß-Tryptase inhibitors   ·Asthma   ·Undisclosed   -
Product Type   Product Owner         Partners                Drug Delivery Route    Dosing                Mechanism Type




NCE            Theravance Inc.       · GlaxoSmithKline Plc   ·LiquidInhalers/Nebuliz Dosage Strengths :   Beta 2 Adrenergic
                                                             ers·DryPowderInhalers- 0.01, 0.015, 0.02     Agonists
                                                             DPI                     milligram ; Dosing
                                                                                     Frequency: Once a
                                                                                     day
NCE            Theravance Inc.       -                       ·DryPowderInhalers-    -                     Beta 2 Adrenergic
                                                             DPI                                          Agonists··Beta 2
                                                                                                          Adrenergic Agonists



NCE            GlaxoSmithKline Plc   -                       ·INHALATION            -                     PDE-4
                                                                                                          (Phosphodiesterase 4)
                                                                                                          Inhibitors
NCE            GlaxoSmithKline Plc   -                       ·ORALDRUGDELIVER Dosage Strength : 90        iNOS (Inducible Nitric
                                                             Y                milligram                   Oxide Synthase)
                                                                                                          Inhibitors




NCE            Theravance Inc.       -                       ·INHALATION            -                     Beta 2 Adrenergic
                                                                                                          Agonists
BLA            GlaxoSmithKline Plc   -                       ·INJECTABLES           -                     -


NCE            GlaxoSmithKline Plc   -                       ·INHALATION            -                     GR Agonists
NCE   GlaxoSmithKline Plc   -                   ·INHALATION        ; Dosing Frequency: 1 GR Agonists
                                                                   per day


BLA   Novartis AG           -                   ·INJECTABLES       -                     Anti-CCL2


NCE   Argenta Discovery     · Dr. Reddys        ·INHALATION        -                     -
                            Laboratories Ltd.

NCE   Argenta Discovery     -                   ·ORALDRUGDELIVER ; Dosing Frequency: 1 CRTH2 Antagonists
                                                Y                per day

NCE   Argenta Discovery     -                   ·INHALATION        ; Dosing Frequency: 2 -
                                                                   per day
new formulation   Forest Laboratories    -   ·Metered-DoseInhalers- Dosage                    Corticosteroids
                  Inc(USA)                   MDI                    Strength(flunisolide) :
                                                                    0.08 milligram ;
                                                                    Dosing Frequency: 2
                                                                    per day




BLA               Affimed Therapeutics   -   ·INJECTABLES            -                        -
                  AG

NCE               Ahn-Gook               -   -                       -                        -
                  Pharmaceutical
                  Co.,Ltd.
NCE               AtheroGenics, Inc.   -   -                     -                     -




new formulation   Acusphere Inc.       -   ·DryPowderInhalers-   ; Dosing Frequency: 1 -
                                           DPI                   per day
new formulation   Alkermes, Inc.           -   ·DryPowderInhalers-   -                      Beta 2 Adrenergic
                                               DPI                                          Agonists




NCE               GlaxoSmithKline Plc      -   ·DryPowderInhalers-   -                      -
                                               DPI
NCE               Altair Therapeutics Inc. -   ·INHALATION           Dosage Strengths : 20, Interleukin 4 Receptor
                                                                     30 milligram ; Dosing Antagonists
                                                                     Frequency: 1 a day
NCE   Akela Pharma Inc.   -   ·DryPowderInhalers-   Dosage Strength : 5    -
                              DPI                   milligram ; Dosing
                                                    Frequency: 2 per day
new formulation   Mitsubishi Tanabe    -   ·ORALDRUGDELIVER Dosage                 H1 (Histamine 1)
                  Pharma                   Y                Strength(pemirolast    Antagonists
                  Corporation(Japan)                        potassium) : 0.5
                                                            percent ; Dosing
                                                            Frequency: 2 per day
NCE   Mitsubishi Tanabe    -   ·ORALDRUGDELIVER Dosage                 H1 (Histamine 1)
      Pharma                   Y                Strengths(pemirolast   Antagonists
      Corporation(Japan)                        potassium) : 5, 10
                                                milligram ; Dosing
                                                Frequency: 2 per day




BLA   ALK-Abello           -   ·OralVaccineDelivery   -                -
NCE   Amira             · GlaxoSmithKline Plc   ·ORALDRUGDELIVER Dosage Strength :     FLAP Inhibitors
      Pharmaceuticals   (World)                 Y                1000 milligram ;
                                                                 Dosing Frequency: 1 a
                                                                 day




NCE   Amira             -                       ·ORALDRUGDELIVER -                        CRTH2 Antagonists
      Pharmaceuticals                           Y




NCE   Amgen Inc.        -                       ·ORALDRUGDELIVER -                      -
                                                Y
BLA   Amgen Inc.        · Takeda                ·INJECTABLES     Dosage Strengths : 75, Anti-IL-4·Anti-IL13
                        Pharmaceutical Co.                       150, 300 milligram ;
                        Ltd. (Japan)                             Dosing Frequency: 1
                                                                 per week




NCE   Amgen Inc.        -                       ·ORALDRUGDELIVER -                        Prostaglandin
                                                Y                                         (Prostanoid) Receptor
                                                                                          Antagonists
NCE               Boehringer Ingelheim   · Actimis              -                       ; Dosing Frequency: 1 CRTH2 Antagonists
                                         Pharmaceuticals                                per day
NCE               Celera Corp.(UK)       -                      ·DryPowderInhalers-     -                     Tryptase Inhibitors
                                                                DPI
new combination   Aradigm Corp.          · CyDex                ·LiquidInhalers/Nebuliz -                     mACh (Muscarinic
                                         Pharmaceuticals, Inc   ers·Cyclodextrins/Solu                        Acetylcholine)
                                                                bilizers-Inhalation                           Receptor
                                                                                                              Antagonists··Beta 2
                                                                                                              Adrenergic
                                                                                                              Agonists·Corticosteroi
                                                                                                              ds
NCE               Alba Therapeutics      -                      -                       -                     -
                  Corporation
new formulation   ISIS Pharmaceuticals   · Antisense            ·INHALATION             -                     alpha4beta1 (VLA-4)
                  Inc.                   Therapeutics Ltd.                                                    Integrin Antagonists


NCE               Clinical Data Inc.     · Novartis AG          ·ORALDRUGDELIVER -                            A2B Adenosine
                                                                Y                                             Receptor Antagonists

NCE               Clinical Data Inc.     -                      -                       -                     A2B Adenosine
                                                                                                              Receptor Antagonists

NCE               A-Viral                · Sanquin              ·INHALATION             -                     -

NCE               Genesis Research &     · Silence Therapeutics ·NasalDelivery          -                     -
                  Development Corp.      Plc

NCE               Pfizer Inc.            · Sanofi-Aventis (USA) ·INHALATION             -                     TLR9 (Toll-like
                                                                                                              receptors 9) Agonists
NCE   Pfizer Inc.       · Sanofi-Aventis   ·INHALATION         -                    TLR9 (Toll-like
                                                                                    receptors 9) Agonists




NCE   Sanofi-Aventis    -                  -                -                     Tryptase Inhibitors
NCE   Avanir            -                  ·ORALDRUGDELIVER Dosage Strengths : 1, Immunomodulators
      Pharmaceuticals                      Y                5 milligram ; Dosing
                                                            Frequency:
NCE   Avontec              · AnGes MG Inc.         ·LiquidInhalers/Nebuliz -   -
                           (Asia)                  ers·GeneDelivery




NCE   elbion NV            · GlaxoSmithKline Plc   ·INHALATION             -   PDE-4
                                                                               (Phosphodiesterase 4)
                                                                               Inhibitors
NCE   Dynavax Technologies · AstraZeneca Plc       -                       -   TLR9 (Toll-like
      Corp.                (World)                                             receptors 9) Agonists
NCE   AstraZeneca Plc      -                       -                       -   -
NCE   AstraZeneca Plc      -   ·ORALDRUGDELIVER Dosage Strengths : 50, CRTH2 Antagonists
                               Y                400, 1000 milligram ;
                                                Dosing Frequency: 2
                                                per day




NCE   AstraZeneca Plc(USA) -   -                      -                -

NCE   AstraZeneca Plc      -   -                      -                -

NCE   AstraZeneca Plc      -   ·InhalationFormulation -                -
                               s,DPI

NCE   AstraZeneca Plc      -   -                      -                Chemokine Receptor
                                                                       Antagonists
NCE   AstraZeneca Plc      -   -                -                      -
NCE   AstraZeneca Plc      -   ·ORALDRUGDELIVER -                      CRTH2 Antagonists
                               Y


NCE   AstraZeneca Plc      -   ·ORALDRUGDELIVER ; Dosing Frequency: 1 CRTH2 Antagonists
                               Y                   per day
NCE   AstraZeneca Plc      -   ·NasalSprayPumps/De -                  -
                               vices




NCE   AstraZeneca Plc      -   -                      -                -
NCE               Capstone              -   -                      -   -
                  Therapeutics(World)




new combination   Sanofi-               -   ·Metered-DoseInhalers- -   Benzodiazepines·Beta
                  Aventis(Germany)          MDI                        2 Adrenergic Agonists




BLA               Ablynx NV(World)      -   -                      -   -
NCE   AstraZeneca Plc(USA) · AstraZeneca Plc (UK) ·ORALDRUGDELIVER Dosage                   LT (Leukotriene)
                                                  Y                Strengths(zafirlukast) : Receptor Antagonists
                                                                   10, 20 milligram ;
                                                                   Dosing Frequency: 2
                                                                   per day
new formulation   DEY L.P.(USA)     -   ·LiquidInhalers/Nebuliz Dosage                 Beta 2 Adrenergic
                                        ers                     Strengths(albuterol    Agonists
                                                                sulfate) : 0.75, 1.5
                                                                milligram ; Dosing
                                                                Frequency: 3-4 a day




generic           Watson            -   ·LiquidInhalers/Nebuliz -                      Beta 2 Adrenergic
                  Pharmaceuticals       ers                                            Agonists
                  Inc.(USA)
NCE               Actimis           -   -                       -   -
                  Pharmaceuticals




new formulation   Ventaira          -   ·LiquidInhalers/Nebuliz -   Corticosteroids
                                        ers
new combination   GlaxoSmithKline     · Almirall (Spain)·   ·DryPowderInhalers-   Dosage                   Corticosteroids·Beta 2
                  Plc(USA,Europe,Japa Schwarz Pharma AG DPI                       Strengths(fluticasone Adrenergic Agonists
                  n)                  (Germany)· Mitsubishi                       propionate) : 0.1, 0.25,
                                      Tanabe Pharma                               0.5 milligram Dosage
                                      Corporation (Japan)                         Strengths(salmeterol
                                                                                  xinafoate) : 0.05, 0.05,
                                                                                  0.05 milligram ;
                                                                                  Dosing Frequency: 2 a
                                                                                  day
new formulation   GlaxoSmithKline   -   ·Metered-DoseInhalers- Dosage                 Corticosteroids·Beta 2
                  Plc(USA)              MDI                    Strengths(fluticasone Adrenergic Agonists
                                                               propionate) : 0.045,
                                                               0.115, 0.23 milligram
                                                               Dosage
                                                               Strengths(salmeterol
                                                               xinafoate) : 0.021,
                                                               0.021, 0.021 milligram
                                                               ; Dosing Frequency: 2
                                                               a day
new formulation   APT Pharmaceuticals -   ·LiquidInhalers/Nebuliz -   Antimalarial,
                                          ers                         Aminoquinolines




BLA               Arriva              -   -                       -   -
                  Pharmaceuticals
BLA   Aerovance, Inc.   -   ·DryPowderInhalers-   Dosage                    Interleukin 4 Receptor
                            DPI                   Strengths(pitrakinra) :   Antagonists·Interleukin
                                                  1, 3, 10, 25, 60          13 Receptor
                                                  milligram ; Dosing        Antagonists
                                                  Frequency: 1-2 a day
new formulation   Forest Laboratories   -   ·Metered-DoseInhalers- Dosage                    Corticosteroids
                  Inc(USA)                  MDI                    Strength(flunisolide) :
                                                                   0.25 milligram ;
                                                                   Dosing Frequency: 2
                                                                   per day
new formulation   Nektar Therapeutics   -   ·LiquidInhalers/Nebuliz -   Beta 2 Adrenergic
                                            ers                         Agonists
new formulation   Nektar Therapeutics   -   ·LiquidInhalers/Nebuliz -   Corticosteroids
                                            ers
NCE               Arrow              -   ·LiquidInhalers/Nebuliz Dosage                  mACh (Muscarinic
                  Pharmaceuticals        ers                     Strengths(ipratropium   Acetylcholine)
                  Ltd.(Australia)                                bromide anhydrous) :    Receptor Antagonists
                                                                 0.25, 0.5 milligram




new formulation   AerovectRx Corp.   -   ·NasalDelivery         -                        -
generic   Eurand N.V.(Europe)   -   ·OralBarrierFilmTablet Dosage                  Xanthines
                                    &Microcaps             Strengths(theophylline)
                                                           : 125, 250, 375, 500
                                                           milligram




generic   GenPharm(USA)         -   ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
                                    MDI                    Strength(albuterol) :   Agonists
                                                           0.09 milligram
generic   Teva Pharmaceutical    -   ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
          Industries Ltd.(USA)       MDI                    Strength(albuterol) :   Agonists
                                                            0.09 milligram
generic   Martec Pharmaceutical -   ·Metered-DoseInhalers- -   Beta 2 Adrenergic
          Inc.(USA)                 MDI                        Agonists
generic   Barr Pharmaceuticals   · Pliva (USA)   ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
          Inc.(USA)                              MDI                    Strength(albuterol) :   Agonists
                                                                        0.09 milligram
new formulation   Ventaira(USA)   -   ·LiquidInhalers/Nebuliz -   Beta 2 Adrenergic
                                      ers                         Agonists
generic   DEY L.P.(USA)         -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                                    ers                     Strength(albuterol       Agonists
                                                            sulfate) : 0.083 percent
                                                            ; Dosing Frequency: 3-
                                                            4 a day




generic   Wockhardt Ltd.(USA)   -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                                    ers                     Strength(albuterol       Agonists
                                                            sulfate) : 0.083 percent
generic   Nephron           -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
          Pharmaceuticals       ers                     Strengths(albuterol      Agonists
          Corp.(USA)                                    sulfate) : 0.042, 0.083,
                                                        0.5 percent
new formulation   Chrysalis              -                   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                  Technologies                               ers                     Strength(albuterol       Agonists
                                                                                     sulfate) : 0.5 percent




NCE               ARYx Therapeutics      -                   -                       -                        Beta 2 Adrenergic
                                                                                                              Agonists
new formulation   Boehringer           · Daiichi Sankyo Co   ·ORALDRUGDELIVER Dosage                          H1 (Histamine 1)
                  Ingelheim(Japan,Kore Ltd. (Japan)          Y                Strengths(epinastine            Antagonists
                  a)                                                          hydrochloride) : 10, 20
                                                                              milligram

new formulation   Alexion                -                   ·INJECTABLES            -                        Anti-C5 Complement
                  Pharmaceuticals Inc.




new formulation   Alexion                -                   ·LiquidInhalers/Nebuliz -                        Anti-C5 Complement
                  Pharmaceuticals Inc.                       ers
new formulation   Sepracor Inc.   · Sanofi-Aventis   ·ORALDRUGDELIVER Dosage                 H1 (Histamine 1)
                                  (USA,Europe)       Y                Strengths(fexofenadin Antagonists
                                                                      e hydrochloride) : 30,
                                                                      60, 120, 180 milligram
                                                                      ; Dosing Frequency: 1-
                                                                      2 per day
NCE               Allergica   -   ·INHALATION·CellPen -     Mast Cell Stabilizers
                                  etratingPeptides(CPPs
                                  )




new combination   Meda AB     -   ·DryPowderInhalers-   -   Mast Cell
                                  DPI                       Stabilizers·Beta 2
                                                            Adrenergic Agonists
new combination   Meda AB(Germany)   -   ·Metered-DoseInhalers- Dosage                 Mast Cell
                                         MDI                    Strength(sodium        Stabilizers·Beta 2
                                                                cromoglycate) : 0.914 Adrenergic Agonists
                                                                milligram Dosage
                                                                Strength(reproterol) :
                                                                0.5 milligram ; Dosing
                                                                Frequency: 4 a day




new formulation   AirPharma          -   ·DryPowderInhalers-   -                      -
                                         DPI
new formulation   geneRx+ Inc.   -   ·INJECTABLES   -   Elastase Inhibitors
NCE   Boehringer       -   ·Metered-DoseInhalers- Dosage                Beta 2 Adrenergic
      Ingelheim(USA)       MDI                    Strength(metaproteren Agonists
                                                  ol sulphate) : 0.65
                                                  milligram ; Dosing
                                                  Frequency: 4-6 a day
new formulation   Boehringer       -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                  Ingelheim(USA)       ers                     Strengths(metaprotere Agonists
                                                               nol sulphate) : 0.4, 0.6
                                                               percent ; Dosing
                                                               Frequency: 4-6 a day
generic   DEY L.P.(USA)   -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                              ers                     Strengths(metaprotere Agonists
                                                      nol sulphate) : 0.4, 0.6
                                                      percent ; Dosing
                                                      Frequency: 4-6 a day
generic   Wockhardt Ltd.(USA)   -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                                    ers                     Strengths(metaprotere Agonists
                                                            nol sulphate) : 0.4, 0.6
                                                            percent
generic   Nephron           -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
          Pharmaceuticals       ers                     Strengths(metaprotere Agonists
          Corp.(USA)                                    nol sulphate) : 0.4, 0.6
                                                        percent
NCE               Nycomed(USA)          · Nycomed             ·Metered-DoseInhalers- Dosage                   Corticosteroids
                                        (Europe,Brazil,Canada MDI                    Strengths(ciclesonide)
                                        ,Mexico,UK)· Teijin                          : 0.08, 0.16 milligram ;
                                        Pharma Ltd. (Japan)·                         Dosing Frequency:
                                        Sepracor Inc. (USA)·                         Once a day
                                        Trudell Medical
                                        International



new combination   Nycomed(ex-US)        · Sepracor Inc. (USA)   ·DryPowderInhalers-    -                      Corticosteroids·Beta 2
                                                                DPI                                           Adrenergic Agonists




BLA               Ambrx, Inc.           -                       -                      -                      -

generic           Themis Laboratories   -                       ·OralBarrierFilmTablet Dosage                 -
                  Private Ltd.(ex-US)                           &Microcaps             Strengths(ambroxol
                                                                                       hydrochloride) : 75,
                                                                                       120 milligram ; Dosing
                                                                                       Frequency: 1 per day
NCE   Rottapharm       -                     ·DryPowderInhalers-   Dosage                  BK (Ca2+-activated
                                             DPI                   Strengths(andolast) :   K+) Channel Openers
                                                                   2, 4, 8 milligram




BLA   Medimmune Inc.   -                     ·INJECTABLES          -                       Anti-Chitinase


NCE   Genentech Inc.   -                     -                     -                       Anti-IL13




NCE   Antitope Ltd.    · NKT Therapeutics,   -                     -                       -
                       Inc.
NCE   Pharmaxis                · Pharmaxis Ltd.       ·DryPowderInhalers-   -   Osmotic Diuretics
      Ltd.(Asia,Europe,Austr   (USA)· Trimedal AG     DPI
      alia,Germany,Korea,U     (Switzerland)· Nigaard
      K)                       Pharma AS
                               (Denmark,Finland,Icel
                               and,Norway,Sweden)·
                               Allertec Hellas A.E.
                               (Greece)
new formulation   Cornerstone         -   ·ORALDRUGDELIVER -   5-lipoxygenase
                  Therapeutics Inc.       Y                    Inhibitors
new formulation   Vectura Group Plc   · UCB Pharma          ·DryPowderInhalers-   Dosage               Corticosteroids
                                      (France,Ireland,UK)   DPI                   Strengths(beclometha
                                                                                  sone dipropionate) :
                                                                                  0.2, 0.4 milligram ;
                                                                                  Dosing Frequency: 2
                                                                                  per day




NCE               Asmacure, Inc.      -                     -                     -                     -
new formulation   Schering-Plough      -   ·DryPowderInhalers-   Dosage                 Corticosteroids
                  Corp.(USA,Europe,Jap     DPI                   Strengths(mometason
                  an)                                            e furoate) : 1.1, 0.2,
                                                                 0.4 milligram ; Dosing
                                                                 Frequency: 1-2 per
                                                                 day
new formulation   Vectura Group Plc   · UCB Pharma          ·DryPowderInhalers-   Dosage                Beta 2 Adrenergic
                                      (Europe,France,Irelan DPI                   Strength(albuterol) : Agonists
                                      d,UK)                                       0.114 milligram ;
                                                                                  Dosing Frequency: 3-4
                                                                                  per day
new formulation   Bang and Olufsen       · Bespak             ·Metered-DoseInhalers- -   -
                  Medicom AS                                  MDI




NCE               Barr Pharmaceuticals   -                    ·DryPowderInhalers-   -    -
                  Inc.                                        DPI
new formulation   Pfizer Inc.            -                    ·SCF,Inhalation·DryPo -    -
                                                              wderInhalers-DPI




NCE               Immune Control Inc.    -                    ·ORALDRUGDELIVER -         -
                                                              Y
NCE               NascaCell              -                    -                -         Tryptase Inhibitors
                  Technologies AG
BLA               Genesis Research &     · Silence Therapeutics ·INJECTABLES         -   -
                  Development Corp.      Plc
NCE   7TM Pharma A/S   · Ortho-McNeil    ·ORALDRUGDELIVER -   CRTH2 Antagonists
                       Pharmaceuticals   Y
                       (World)
new combination   Maruho            -   ·ORALDRUGDELIVER -   Alpha Adrenergic
                  Co.,Ltd.(Japan)       Y                    Agonists·Beta
                                                             Adrenergic
                                                             Agonists·Anticonvulsa
                                                             nts, Barbiturates
generic   Novell Pharmaceutical -   ·ORALDRUGDELIVER -   Beta 2 Adrenergic
          Laboratories              Y                    Agonists
generic   Novell Pharmaceutical -   ·ORALDRUGDELIVER Dosage                  Beta 2 Adrenergic
          Laboratories              Y                Strengths(procaterol    Agonists
                                                     hydrochloride) : 0.025,
                                                     0.05 milligram
new formulation   Boehringer          -   ·DryPowderInhalers-   Dosage                mACh (Muscarinic
                  Ingelheim(Europe)       DPI                   Strength(ipratropium  Acetylcholine)
                                                                bromide hydrate) :    Receptor Antagonists
                                                                0.04 milligram ;
                                                                Dosing Frequency: 3-4
                                                                a day
NCE   Boehringer       -   ·Metered-DoseInhalers- Dosage                 mACh (Muscarinic
      Ingelheim(USA)       MDI                    Strength(ipratropium   Acetylcholine)
                                                  bromide hydrate) :     Receptor Antagonists
                                                  0.018 milligram ;
                                                  Dosing Frequency: 4
                                                  per day
new formulation   Boehringer         · Boehringer Ingelheim ·LiquidInhalers/Nebuliz Dosage                mACh (Muscarinic
                  Ingelheim(ex-US)   (USA)                  ers                     Strength(ipratropium  Acetylcholine)
                                                                                    bromide hydrate) :    Receptor Antagonists
                                                                                    0.02 percent ; Dosing
                                                                                    Frequency: 3-4 per
                                                                                    day
BLA               Amgen Inc.            -                        ·INJECTABLES           -                      -




NCE               Anesiva, Inc.         · Transcription Factor   -                      -                      -
                                        Therapeutics, LLC
                                        (World)
NCE               Axikin                -                        -                      -                      -
                  Pharmaceuticals
new formulation   Abbott Laboratories   -                        ·Metered-DoseInhalers- Dosage                 Corticosteroids
                  Inc.(USA)                                      MDI                    Strengths(triamcinolon
                                                                                        e acetonide) : 0.075,
                                                                                        0.225 milligram ;
                                                                                        Dosing Frequency: 2-4
                                                                                        a day
new formulation   Abbott Laboratories   -   ·Metered-DoseInhalers- Dosage                 Corticosteroids
                  Inc.(USA)                 MDI                    Strength(triamcinolone
                                                                   acetonide) : 0.1
                                                                   milligram ; Dosing
                                                                   Frequency: 2-4 a day
new formulation   Chiesi Farmaceutici   · GlaxoSmithKline Plc   ·Metered-DoseInhalers- Dosage               Corticosteroids
                  SpA(Europe)           (France,UK)             MDI                    Strengths(beclometha
                                                                                       sone dipropionate) :
                                                                                       0.05, 0.1, 0.2, 0.25
                                                                                       milligram
NCE   Boehringer Ingelheim   -                   ·LiquidInhalers/Nebuliz Dosage Strengths :       -
                                                 ers                     0.05, 0.1, 0.2 milligram
                                                                         ; Dosing Frequency: 1
                                                                         per day




BLA   Barofold               -                   ·INJECTABLES            -                        -

NCE   Boehringer Ingelheim   -                   ·LiquidInhalers/Nebuliz Dosage Strengths :      -
                                                 ers                     0.005, 0.01 milligram ;
                                                                         Dosing Frequency: 1
                                                                         per day



NCE   Boehringer Ingelheim   -                   ·DryPowderInhalers-     -                        -
                                                 DPI

BLA   Kyowa Hakko Kirin      · AstraZeneca Plc   ·INJECTABLES            -                        Anti-IL-5R
      Co., Ltd.(USA)         (USA)




NCE   Funxional              -                   ·ORALDRUGDELIVER -                               Chemokine Receptor
      Therapeutics, Ltd.                         Y                                                Antagonists
BLA               Biotest AG            · Boehringer Ingelheim ·INJECTABLES          -                 -




NCE               AstraZeneca Plc(ex-   -                    ·ORALDRUGDELIVER Dosage                  Beta 2 Adrenergic
                  US)                                        Y                Strengths(bambuterol Agonists
                                                                              hydrochloride) : 10, 20
                                                                              milligram ; Dosing
                                                                              Frequency: 1 per day




new formulation   Ventaira              · Telesso            ·SCF,Inhalation·LiquidI -                 -
                                        Technologies         nhalers/Nebulizers
new formulation   Teva Pharmaceutical -     ·Metered-DoseInhalers- Dosage               Corticosteroids
                  Industries Ltd.(Europe)   MDI                    Strengths(beclometha
                                                                   sone dipropionate) :
                                                                   0.05, 0.1, 0.25
                                                                   milligram




new formulation   GlaxoSmithKline       -   ·DryPowderInhalers-   Dosage                  Corticosteroids
                  Plc(UK)                   DPI                   Strength(beclomethas
                                                                  one dipropionate) : 0.4
                                                                  milligram ; Dosing
                                                                  Frequency: 2 a day
new formulation   Orion Corp.(Europe)   · HRA Pharma   ·DryPowderInhalers-   Dosage               Corticosteroids
                                        (France)       DPI                   Strengths(beclometha
                                                                             sone dipropionate) :
                                                                             0.1, 0.2 milligram




new formulation   Teva Pharmaceutical -                ·DryPowderInhalers-   Dosage                  Corticosteroids
                  Industries Ltd.(Europe)              DPI                   Strengths(beclometha
                                                                             sone dipropionate) :
                                                                             0.1, 0.2, 0.4 milligram
new formulation   Orion Corp.(USA)   -   ·Metered-DoseInhalers- Dosage                   Corticosteroids
                                         MDI                    Strengths(beclometha
                                                                sone dipropionate) :
                                                                0.05, 0.1, 0.2 milligram
                                                                ; Dosing Frequency: 2
                                                                per day
new combination   Boehringer           -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                  Ingelheim(Germany)       ers                     Strength(fenoterol       Agonists·mACh
                                                                   hydrobromide) : 1.25     (Muscarinic
                                                                   milligram Dosage         Acetylcholine)
                                                                   Strength(ipratropium     Receptor Antagonists
                                                                   bromide hydrate) : 0.5
                                                                   milligram
new formulation   Boehringer Ingelheim   -   ·LiquidInhalers/Nebuliz Dosage                  Beta 2 Adrenergic
                                             ers                     Strengths(fenoterol     Agonists
                                                                     hydrobromide) : 0.25,
                                                                     0.625 milligram




new formulation   Boehringer             -   ·Metered-DoseInhalers- Dosage                   Beta 2 Adrenergic
                  Ingelheim(USA)             MDI                    Strengths(fenoterol      Agonists
                                                                    hydrobromide) : 0.1,
                                                                    0.2 milligram
NCE               geneRx+ Inc.           -                       ·Liposomes,Inhalation· -   Transcription factor
                                                                 Lipid(Cationic)Vectors     inhibitor




BLA               geneRx+ Inc.           -                       ·INJECTABLES           -   Transcription factor
                                                                                            inhibitor




new formulation   BioDelivery Sciences   · Accentia              ·NasalDelivery         -   Antifungals, Polyene
                  International Inc.     Biopharmaceuticals
                                         Inc. (USA)




BLA               GlaxoSmithKline        · GlaxoSmithKline Plc   ·INJECTABLES           -   Anti-IL-5R
                  Plc(Europe)            (USA)
new formulation   Novartis AG(USA)   · AAIPharma (USA)   ·INJECTABLES        Dosage                 Beta 2 Adrenergic
                                                                             Strength(terbutaline   Agonists
                                                                             sulfate) : 0.25
                                                                             milligram




NCE               Novartis AG(USA)   · AAIPharma (USA)   ·ORALDRUGDELIVER Dosage                    Beta 2 Adrenergic
                                                         Y                Strengths(terbutaline     Agonists
                                                                          sulfate) : 2.5, 5
                                                                          milligram ; Dosing
                                                                          Frequency: 3 per day
new formulation   AstraZeneca Plc(ex-   -                     ·Metered-DoseInhalers- Dosage                 Beta 2 Adrenergic
                  US)                                         MDI                    Strength(terbutaline   Agonists
                                                                                     sulfate) : 0.25
                                                                                     milligram ; Dosing
                                                                                     Frequency: 4 per day




new formulation   Sanofi-               · Sanofi-Aventis (USA) ·DryPowderInhalers-   Dosage                   Beta 2 Adrenergic
                  Aventis(Europe)                              DPI                   Strength(terbutaline     Agonists
                                                                                     sulfate) : 0.5 milligram
                                                                                     ; Dosing Frequency: 1-
                                                                                     4 per day




NCE               Takeda                -                     ·ORALDRUGDELIVER Dosage                 TXA2 (Thromboxane
                  Pharmaceutical Co.                          Y                Strengths(seratrodast) A2) Receptor
                  Ltd.(Japan)                                                  : 40, 80 milligram ;   Antagonists
                                                                               Dosing Frequency: 1
                                                                               per day
new formulation   RatioPharm      -   ·DryPowderInhalers-   -   Corticosteroids
                  GmbH(Germany)       DPI




new formulation   RatioPharm      -   ·DryPowderInhalers-   -   Corticosteroids
                  GmbH(Germany)       DPI
new formulation   Teva Pharmaceutical -                      ·DryPowderInhalers-   -   Corticosteroids
                  Industries                                 DPI
                  Ltd.(Denmark,German
                  y)




generic           Vectura Group Plc   · Merck KGaA           ·DryPowderInhalers-   -   Corticosteroids
                                      (Europe)· Mylan Inc.   DPI
                                      (Europe)
new formulation   Teva Pharmaceutical -     ·DryPowderInhalers-    Dosage                Corticosteroids
                  Industries Ltd.(Europe)   DPI                    Strengths(budesonide)
                                                                   : 0.2, 0.4 milligram




new formulation   SkyePharma Plc        -   ·Metered-DoseInhalers- Dosage                 Corticosteroids
                                            MDI                    Strength(budesonide) :
                                                                   0.2 milligram
generic           Teva Pharmaceutical    -                     ·LiquidInhalers/Nebuliz ; Dosing Frequency: 2 Corticosteroids
                  Industries Ltd.(USA)                         ers                     per day




new formulation   Cosmo                  · Ferring              ·ColonicRelease       Dosage                Corticosteroids
                  Pharmaceuticals        Pharmaceuticals                              Strengths(budesonide)
                  S.p.A.(USA,Canada)     (Asia,Latin                                  : 6, 9 milligram
                                         America,Europe,ex-
                                         Japan)· Santarus, Inc.
                                         (USA)
new formulation   Chiesi Farmaceutici   -   ·Metered-DoseInhalers- Dosage                 Corticosteroids
                  SpA(Germany)              MDI                    Strength(budesonide) :
                                                                   0.2 milligram ; Dosing
                                                                   Frequency: 1 per day
new formulation   Ventaira           -   ·LiquidInhalers/Nebuliz -   Corticosteroids
                                         ers




new formulation   Direct-Haler A/S   -   ·DryPowderInhalers-     -   Corticosteroids
                                         DPI
new formulation   Chiesi Farmaceutici   · Trinity Biotech Plc   ·DryPowderInhalers-   Dosage                 Beta 2 Adrenergic
                  SpA(Europe)                                   DPI                   Strength(albuterol) :  Agonists
                                                                                      0.2 milligram ; Dosing
                                                                                      Frequency: 1-4 per
                                                                                      day
new formulation   Orion Corp.(Europe)   · HRA Pharma     ·DryPowderInhalers-   Dosage                   Beta 2 Adrenergic
                                        (France)         DPI                   Strengths(albuterol) :   Agonists
                                                                               0.1, 0.2 milligram




BLA               AstraZeneca Plc       · Synairgen·     ·INJECTABLES          ; Dosing Frequency: 1 Anti-IL13
                                        Medimmune Inc.                         per month
NCE   Celgene Corp.(USA)    -                   ·ORALDRUGDELIVER Dosage                       PDE-4
                                                Y                Strengths(apremilast) :      (Phosphodiesterase 4)
                                                                 10, 20, 30, 40               Inhibitors·TNF-alpha
                                                                 milligram ; Dosing           Inhibitors
                                                                 Frequency: 1-2 per
                                                                 day




NCE   Kyowa Hakko Kirin     · deCODE Genetics   ·ORALDRUGDELIVER -                            MAP3K9 Inhibitors
      Co., Ltd.             Inc.                Y

NCE   Chiesi Farmaceutici   · 3M Health Care    ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
      SpA(Europe)           (USA)· Mitsubishi   MDI                    Strengths(carmoterol) : Agonists
                            Tanabe Pharma                              0.001, 0.002, 0.004
                            Corporation                                milligram ; Dosing
                            (Asia,Japan)                               Frequency: 1 per day
new combination   Chiesi Farmaceutici   -   ·Metered-DoseInhalers- -                 Beta 2 Adrenergic
                  SpA                       MDI                                      Agonists·Corticosteroi
                                                                                     ds




NCE               Cytokinetics, Inc.    -   ·INHALATION            -                 muscle myosin
                                                                                     inhibitors

NCE               Mitsubishi            -   ·ORALDRUGDELIVER Dosage                 Mucolytic Agents
                  Pharmaceutical            Y                Strength(fudosteine) :
                  Corp.(Japan)                               200 milligram ; Dosing
                                                             Frequency: 3 per day
new formulation   BTG International   -   ·OralLiquidMR       -   -
                  Limited




NCE               Pfizer Inc.         -   ·NasalDelivery      -   PDE-4
                                                                  (Phosphodiesterase 4)
                                                                  Inhibitors
NCE               Clavis Pharma ASA   -   ·Prodrugs,LowMWAtta -   Corticosteroids
                                          chments
new formulation   Clavis Pharma ASA   -   ·Prodrugs,LowMWAtta -   Corticosteroids
                                          chments




NCE               Rottapharm          -   ·ORALDRUGDELIVER -      LT (Leukotriene)
                                          Y                       Receptor Antagonists




NCE               Actelion Ltd.       -   -                   -   CRTH2 Antagonists

NCE               Argenta Discovery   -   ·ORALDRUGDELIVER -      CRTH2 Antagonists
                                          Y
new combination   CombinatoRx Inc.   -   ·OralModifiedRel.(MR) ; Dosing Frequency: 1 Corticosteroids·Tricycli
                                                               per day               c Antidepressants
new combination   CombinatoRx Inc.   -   ·ORALDRUGDELIVER -   Corticosteroids·Tricycli
                                         Y                    c Antidepressants
new indication   Competitive          -   -                   -                   -
                 Technologies, Inc.




NCE              Gilead Sciences      -   ·ORALDRUGDELIVER ; Dosing Frequency: 1 A2B Adenosine
                 Inc.(World)              Y                per day               Receptor Antagonists
BLA   Cytos Biotechnology   -   ·INJECTABLES   Dosage Strength : 0.3 -
      AG                                       milligram
new combination   Cytos Biotechnology   -   ·INJECTABLES   Dosage Strength : 0.3 -
                  AG(USA)                                  milligram
NCE               Shire Pharmaceuticals -                   ·ORALDRUGDELIVER Dosage                 Corticosteroids
                  Group PLC(UK)                             Y                Strengths(deflazacort)
                                                                             : 1, 6, 30 milligram




new formulation   Verus                 · AstraZeneca Plc   ·Cyclodextrins/Solubiliz -               Corticosteroids
                  Pharmaceuticals       (North America)     ers-
                                                            Inhalation·LiquidInhale
                                                            rs/Nebulizers
NCE   Celera Corp.   -                     -   -   Tryptase Inhibitors




NCE   UCB Pharma     · Merck and Co Inc.   -   -   PDE-4
                                                   (Phosphodiesterase 4)
                                                   Inhibitors
NCE   Cellzome AG           -   -   -   Itk Inhibitors




NCE   Cellzome AG           -   -   -   PI3K-gamma Inhibitors

NCE   Chiesi Farmaceutici   -   -   -   PDE-4
      SpA                               (Phosphodiesterase 4)
                                        Inhibitors
generic           Pfizer Inc.           · Warner Chilcott Ltd.   ·OralMatrixMR           Dosage                   Xanthines·PDE
                                        (USA)                                            Strengths(oxtriphylline) (phosphodiesterase)
                                                                                         : 400, 600 milligram ; Inhibitors
                                                                                         Dosing Frequency: 2
                                                                                         per day




OTC               Galenica S.A.(Greece) -                        ·OralMatrixMR           Dosage                 -
                                                                                         Strengths(choline
                                                                                         theophylline) : 400,
                                                                                         600 milligram
new formulation   Nycomed               -                        ·LiquidInhalers/Nebuliz -                      Corticosteroids
                                                                 ers
BLA   NeoPharm Inc.   · National Institute of   ·LiquidInhalers/Nebuliz -   Antibiotics,
                      Health (NIH)              ers                         Antineoplastic
new formulation   LTT Bio-Pharma Co     · Cipla Ltd.   ·NanoparticlesOther,Inj -                      Corticosteroids
                  Ltd                                  ectable




new formulation   Chiesi Farmaceutici   -              ·DryPowderInhalers-     Dosage                  Corticosteroids
                  SpA(Europe)                          DPI                     Strengths(beclometha
                                                                               sone dipropionate) :
                                                                               0.1, 0.2, 0.4 milligram
                                                                               ; Dosing Frequency: 2-
                                                                               4 per day
new combination   Boehringer       -   ·Metered-DoseInhalers- Dosage                 mACh (Muscarinic
                  Ingelheim(USA)       MDI                    Strength(ipratropium   Acetylcholine)
                                                              bromide hydrate) :     Receptor
                                                              0.018 milligram        Antagonists·Beta 2
                                                              Dosage                 Adrenergic Agonists
                                                              Strength(albuterol
                                                              sulfate) : 0.09
                                                              milligram ; Dosing
                                                              Frequency: 4 per day
new formulation   Novartis AG     -   ·INHALATION     -   Beta 2 Adrenergic
                                                          Agonists




new formulation   Sepracor Inc.   -   ·OralMatrixMR   -   Beta 2 Adrenergic
                                                          Agonists
new formulation   Gilead Sciences Inc.   -   ·LiquidInhalers/Nebuliz -   Sodium Channel
                                             ers                         Blockers·Local
                                                                         Anesthetics, Amides
new formulation   Teva Pharmaceutical    -   ·Metered-DoseInhalers- Dosage                  NSAIDs (Non Steroidal
                  Industries Ltd.(USA)       MDI                    Strength(cromolyn       Antiinflammatory
                                                                    sodium) : 5 milligram   Drugs)
new formulation   Durect Corporation   -   ·Biodeg(PLGA)Microca -      NSAIDs (Non Steroidal
                                           ps/Rods                     Antiinflammatory
                                                                       Drugs)




NCE               Ventaira             -   ·LiquidInhalers/Nebuliz -   -
                                           ers
NCE       Caden Biosciences     -                   -                    -                      -
          Inc.
NCE       DMI BioSciences, Inc. -                   -                    -                      -

NCE       Dr. Reddys           · Argenta Discovery  ·INHALATION          -                      -
          Laboratories Ltd.
-         Dainippon Sumitomo · AstraZeneca Plc (ex- -                    -                      TLR7 Agonists
          Pharmaceutical(Japan Asia,Europe)
          )



NCE       Nycomed(USA,Switzer · Mitsubishi Tanabe   ·ORALDRUGDELIVER Dosage                   PDE-4
          land)               Pharma Corporation    Y                Strengths(roflumilast) : (Phosphodiesterase 4)
                              (Japan)                                0.25, 0.5 milligram ;    Inhibitors
                                                                     Dosing Frequency: 1
                                                                     per day



generic   Eurand N.V.(Europe)   -                   ·OralMatrixMR        Dosage                  Xanthines
                                                                         Strengths(theophylline)
                                                                         : 100, 200, 350
                                                                         milligram ; Dosing
                                                                         Frequency: Once a
                                                                         day
BLA   Domantis Limited   -   ·INJECTABLES   -   Anti-IL-4·Anti-IL13
NCE   Kissei Pharmaceutical -   ·ORALDRUGDELIVER Dosage                  Thromboxane
      Company(Japan)            Y                Strengths(ozagrel       Synthetase Inhibitors
                                                 hydrochloride) : 100,
                                                 200 milligram
NCE               Cellzome AG            -                       -                      -   PI3K-delta
                                                                                            Inhibitors·PI3K-gamma
                                                                                            Inhibitors




new formulation   Vectura Group Plc      -                       ·DryPowderInhalers-    -   -
                                                                 DPI

new formulation   Vectura Group Plc      -                       ·DryPowderInhalers-    -   -
                                                                 DPI

NCE               Epigenesis             · Chiesi Farmaceutici   ·Metered-DoseInhalers- -   A1A Adenosin
                  Pharmaceuticals Inc.   SpA                     MDI                        Receptor Related




NCE               Enanta                 -                       ·Topical               -   CN (Calcineurin)
                  Pharmaceuticals                                                           Inhibitors
NCE               Enanta                 -   ·Topical               -   CN (Calcineurin)
                  Pharmaceuticals                                       Inhibitors




new combination   Epigenesis             -   ·Metered-DoseInhalers- -   -
                  Pharmaceuticals Inc.       MDI
new indication    e-Therapeutics plc      -   ·ORALDRUGDELIVER -        -
                                              Y




new formulation   Oriel Therapeutics Inc. -   ·DryPowderInhalers-   -   -
                                              DPI·SCF,Inhalation
new formulation   Emisphere            -   ·OralSolubleDrugsIncr -   NSAIDs (Non Steroidal
                  Technologies, Inc.       easedAbsorption           Antiinflammatory
                                                                     Drugs)
OTC   Amphastar         -   ·Metered-DoseInhalers- Dosage                  Alpha Adrenergic
      Pharmaceuticals       MDI                    Strength(epinephrine) : Agonists·Beta
      Inc.(USA)                                    0.22 milligram          Adrenergic Agonists
generic   Nycomed(ex-US)   -   ·OralEnteric/DelayedR Dosage                 Xanthines
                               el.                   Strength(theophylline)
                                                     : 250 milligram ;
                                                     Dosing Frequency: 2-3
                                                     per day
new formulation   Nycomed              -                 ·INJECTABLES   ; Dosing Frequency: 1 Xanthines
                                                                        per day




NCE               Euroscreen S.A.      · Alchemia Ltd.   -              -                    P2Y2 Receptor
                                       (Australia)                                           Agonists




NCE               ZaBeCor              -                 -              -                    Anti-inflammatory
                  Pharmaceuticals, LLC
NCE   Farmacija          -   ·INJECTABLES   -   -




NCE   Forbes Medi-Tech   -   -              -   VPAC2 Agonists
new combination   Chiesi Farmaceutici   · Chiesi Farmaceutici ·Metered-DoseInhalers- Dosage                  Corticosteroids·Beta 2
                  SpA(Europe,Russia)    SpA (USA)· Orient     MDI                    Strength(beclomethas Adrenergic Agonists
                                        Europharma Co. Ltd.                          one dipropionate) : 0.1
                                        (Taiwan)· Novartis AG                        milligram Dosage
                                        (Europe)                                     Strength(formoterol
                                                                                     fumarate) : 0.006
                                                                                     milligram ; Dosing
                                                                                     Frequency: 1-2 a day




NCE               Domain Therapeutics   -                      -                      -                      A3A Adenosine
                                                                                                             Receptor Antagonists
new formulation   GlaxoSmithKline        -   ·DryPowderInhalers-   Dosage                   Corticosteroids
                  Plc(UK)                    DPI                   Strengths(fluticasone
                                                                   propionate) : 0.05, 0.1,
                                                                   0.25, 0.5 milligram ;
                                                                   Dosing Frequency: 2 a
                                                                   day




new formulation   Taro Pharmaceutical    -   ·TasteMasking         -                       Corticosteroids
                  Industries Ltd.(USA)
new formulation   GlaxoSmithKline   -                    ·Metered-DoseInhalers- Dosage                   Corticosteroids
                  Plc(World)                             MDI                    Strengths(fluticasone
                                                                                propionate) : 0.044,
                                                                                0.11, 0.22 milligram ;
                                                                                Dosing Frequency: 2
                                                                                per day




new formulation   GlaxoSmithKline   · Almirall (Spain)   ·DryPowderInhalers-    Dosage                   Corticosteroids
                  Plc(USA)                               DPI                    Strengths(fluticasone
                                                                                propionate) : 0.05, 0.1,
                                                                                0.25 milligram ;
                                                                                Dosing Frequency: 2
                                                                                for 2 days
new formulation   GlaxoSmithKline   -   ·Metered-DoseInhalers- Dosage                 Corticosteroids
                  Plc(USA,UK)           MDI                    Strengths(fluticasone
                                                               propionate) : 0.044,
                                                               0.11, 0.22 milligram ;
                                                               Dosing Frequency: 2 a
                                                               day
NCE               Hollis-Eden            -   -                     -   Androgens
                  Pharmaceuticals Inc.




new formulation   Miat Spa               -   ·DryPowderInhalers-   -   Corticosteroids
                                             DPI
new combination   SkyePharma Plc     · Abbott Laboratories   ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
                                     Inc. (USA)·             MDI                    Strengths(formoterol) : Agonists·Corticosteroi
                                     Mundipharma AG                                 0.01, 0.01 milligram    ds
                                     (Europe)· Kyorin                               Dosage
                                     Pharmaceutical                                 Strengths(fluticasone
                                     (Japan)                                        propionate) : 0.1, 0.25
                                                                                    milligram ; Dosing
                                                                                    Frequency: 2 per day




NCE               Novartis AG(USA)   · Novartis AG (UK)·   ·DryPowderInhalers-      Dosage                  Beta 2 Adrenergic
                                     Schering-Plough Corp. DPI                      Strength(formoterol     Agonists
                                     (USA)                                          fumarate) : 0.012
                                                                                    milligram ; Dosing
                                                                                    Frequency: 2 per day
new formulation   Novartis AG   · Astellas Pharma Inc. ·DryPowderInhalers-   -   Beta 2 Adrenergic
                                                       DPI                       Agonists
new formulation   Novartis AG   · Novartis AG        ·DryPowderInhalers-   ; Dosing Frequency: 2 Beta 2 Adrenergic
                                (Europe,Germany,Swit DPI                   per day               Agonists
                                zerland)· SkyePharma
                                Plc (USA)
NCE               Meda AB(Europe)   -   ·DryPowderInhalers-    Dosage                  Beta 2 Adrenergic
                                        DPI                    Strengths(formoterol) : Agonists
                                                               0.006, 0.012 milligram




new formulation   SkyePharma Plc    -   ·Metered-DoseInhalers- -                      Beta 2 Adrenergic
                                        MDI                                           Agonists
new formulation   Chiesi Farmaceutici · Novartis AG       ·Metered-DoseInhalers- Dosage                Beta 2 Adrenergic
                  SpA(France,Germany, (Europe)· Nycomed   MDI                    Strength(formoterol   Agonists
                  Greece,Italy,UK)    (Canada)                                   fumarate) : 0.012
                                                                                 milligram




new formulation   Direct-Haler A/S    -                   ·DryPowderInhalers-    -                     Beta 2 Adrenergic
                                                          DPI                                          Agonists




new formulation   Miat Spa            -                   ·DryPowderInhalers-    -                     Beta 2 Adrenergic
                                                          DPI                                          Agonists
new formulation   Chiesi Farmaceutici   -   ·DryPowderInhalers-   -   Corticosteroids·Beta 2
                  SpA                       DPI                       Adrenergic Agonists
new formulation   Miat Spa(ex-US)     -                       ·DryPowderInhalers-   -                 Corticosteroids
                                                              DPI




BLA               GenOdyssee          -                       -                     -                 -


NCE               Glenmark            · Forest Laboratories   ·ORALDRUGDELIVER ; Dosing Frequency: 1 PDE-4
                  Pharmaceuticals     Inc (North America)·    Y                per day               (Phosphodiesterase 4)
                                      Teijin Pharma Ltd.                                             Inhibitors
                                      (Japan)
NCE               Novozymes GroPep    -                       -                     -                 -
                  Ltd.




NCE               Merck and Co Inc.   -                       ·INHALATION           -                 -


NCE               Theravance Inc.     · GlaxoSmithKline Plc   ·INHALATION           -                 mACh (Muscarinic
                                                                                                      Acetylcholine)
                                                                                                      Receptor
                                                                                                      Antagonists·Beta 2
                                                                                                      Adrenergic Agonists
NCE               GlaxoSmithKline Plc   -                   ·DryPowderInhalers-   ; Dosing Frequency: 1 mACh (Muscarinic
                                                            DPI                   per day               Acetylcholine)
                                                                                                        Receptor Antagonists




NCE               Theravance Inc.       -                   ·INHALATION           -                       Beta 2 Adrenergic
                                                                                                          Agonists··Beta 2
                                                                                                          Adrenergic Agonists
new formulation   GlaxoSmithKline Plc   · Theravance Inc.   ·DryPowderInhalers-   Dosage                  Corticosteroids
                                                            DPI                   Strengths(fluticasone
                                                                                  furoate) : 0.025, 0.8
                                                                                  milligram ; Dosing
                                                                                  Frequency: 2 a day
NCE,new combination GlaxoSmithKline Plc   · Theravance Inc.   ·DryPowderInhalers-   -   Corticosteroids··Cortic
                                                              DPI                       osteroids·Beta 2
                                                                                        Adrenergic Agonists




NCE                  Galapagos NV         -                   -                     -   -
NCE       Galileo                 -   -                      -                       5-lipoxygenase
          Pharmaceuticals, Inc.                                                      Inhibitors

generic   GenPharm(ex-US)         -   ·LiquidInhalers/Nebuliz Dosage                 mACh (Muscarinic
                                      ers                     Strength(ipratropium   Acetylcholine)
                                                              bromide hydrate) :     Receptor Antagonists
                                                              0.025 percent
generic   GenPharm(ex-US)   -   ·LiquidInhalers/Nebuliz Dosage                 mACh (Muscarinic
                                ers                     Strength(ipratropium   Acetylcholine)
                                                        bromide hydrate) :     Receptor Antagonists
                                                        0.025 percent
generic   GenPharm(ex-US)       -                    ·LiquidInhalers/Nebuliz -   Beta 2 Adrenergic
                                                     ers                         Agonists




generic   GenPharm(ex-US)       -                    ·LiquidInhalers/Nebuliz -   Beta 2 Adrenergic
                                                     ers                         Agonists




NCE       Generex               · Antigen Express,   ·INJECTABLES            -   -
          Biotechnology Corp.   Inc.· Stallergenes
generic   Apotex   -   ·LiquidInhalers/Nebuliz -   Corticosteroids
                       ers
new formulation   Orion Corp.(USA)   -   ·DryPowderInhalers-   Dosage                 Corticosteroids
                                         DPI                   Strength(budesonide) :
                                                               0.1 milligram ; Dosing
                                                               Frequency: 2 per day
new formulation   Orion Corp.   -   ·DryPowderInhalers-   -   Corticosteroids·Beta 2
                                    DPI                       Adrenergic Agonists
new formulation   Almirall         -   ·DryPowderInhalers-   -   mACh (Muscarinic
                                       DPI                       Acetylcholine)
                                                                 Receptor Antagonists




BLA               Genentech Inc.   -   ·GeneDelivery         -   Anti-IgE
BLA       Hunter-Fleming   -   -                      -   -




generic   Inyx Inc.        -   ·Metered-DoseInhalers- -   -
                               MDI
NCE   Spring Bank         -   -   -   -
      Technologies, Inc

NCE   Prolexys            -   -   -   HSP20 signal
                                      modulators
NCE   Abbott Laboratories   · Maruho Co.,Ltd.     ·PatchesDrug-in-   Dosage                   Beta 2 Adrenergic
      Inc.(Japan)           (Japan)· Aveva Drug   Adhesive           Strengths(tulobuterol) : Agonists
                            Delivery Systems                         0.5, 1, 2 milligram ;
                                                                     Dosing Frequency:
                                                                     Once a day




NCE   Hutchison China       -                     -                  -                      -
      Meditech
NCE   Indigene                -   -              -   -
      Pharmaceuticals, Inc.

NCE   Indigene                -   -              -   -
      Pharmaceuticals, Inc.

NCE   Indigene                -   -              -   -
      Pharmaceuticals, Inc.

NCE   Indigene                -   -              -   -
      Pharmaceuticals, Inc.

NCE   Synairgen               -   -              -   Interleukin 4 Receptor
                                                     Antagonists·Interleukin
                                                     13 Receptor
                                                     Antagonists

BLA   Regeneron               -   ·INJECTABLES   -   Anti-IL-4·Anti-IL13
      Pharmaceuticals Inc.
BLA   NeoPharm Inc.         · Nippon Kayaku Co.,     ·ConvectionEnhanced -    Antibiotics,
                            Ltd. (Japan)· National   Delivery·Prodrugs,High   Antineoplastic
                            Institute of Health      MWAttach.(PEGetc.)
                            (NIH)




NCE   Cosmix                -                        ·INJECTABLES         -   -

BLA   Cytos Biotechnology   -                        ·INJECTABLES         -   -
      AG
BLA                  Wyeth                -   ·INJECTABLES          -                Anti-IL13


new indication,new   Inverseon, Inc.      -   ·OralModifiedRel.(MR) -                Beta Blockers, Non-
formulation                                                                          selective




NCE                  Taiho Pharmaceutical -   ·ORALDRUGDELIVER Dosage                Interleukin 4 Receptor
                     Co., Ltd.(Japan)         Y                Strengths(suplatast   Antagonists
                                                               tosilate) : 50, 100
                                                               milligram
NCE               Taiho Pharmaceutical -                   ·ORALDRUGDELIVER Dosage                  Interleukin 4 Receptor
                  Co., Ltd.(Japan)                         Y                Strength(suplatast      Antagonists
                                                                            tosilate) : 5 percent




NCE               Orexo AB              · Helicon (USA)·   ·ORALDRUGDELIVER Dosage Strength : 20    LSAID (Leukocyte
                                        Sanofi-Aventis     Y                milligram ; Dosing      Selective Anti-
                                                                            Frequency: 1 per day    Inflammatory Drug)




NCE               Orexo AB              -                  ·ORALDRUGDELIVER -                       -
                                                           Y


new formulation   Shire Pharmaceuticals -                  ·INHALATION          -                   BDKRB2 (Bradykinin
                  Group PLC                                                                         Receptor B2)
                                                                                                    Antagonists




NCE               Opsona Therapeutics   -                  -                    -                   Interleukin-1 beta
                  Ltd.                                                                              inhibitor
OTC               Boehringer Ingelheim   -   ·DryPowderInhalers-     Dosage                 Corticosteroids
                                             DPI                     Strength(budesonide) :
                                                                     0.4 milligram




NCE               Nektar Therapeutics    -   ·DryPowderInhalers-     -                      -
                                             DPI
new formulation   Next Safety, Inc.      -   ·LiquidInhalers/Nebuliz -                      Beta 2 Adrenergic
                                             ers                                            Agonists




BLA               Dynavax Technologies -     ·INHALATION             -                      -
                  Corp.
new formulation   Astellas Pharma   -   ·Metered-DoseInhalers- Dosage                  NSAIDs (Non Steroidal
                  Inc.(Japan)           MDI                    Strength(cromolyn       Antiinflammatory
                                                               sodium) : 2 milligram ; Drugs)
                                                               Dosing Frequency: 4
                                                               per day
NCE   Astellas Pharma   -   ·DryPowderInhalers-   Dosage                 NSAIDs (Non Steroidal
      Inc.(Japan)           DPI                   Strength(cromolyn      Antiinflammatory
                                                  sodium) : 20 milligram Drugs)
                                                  ; Dosing Frequency: 3-
                                                  4 per day
new formulation   King Pharmaceuticals -   ·Metered-DoseInhalers- -   NSAIDs (Non Steroidal
                  Inc.                     MDI                        Antiinflammatory
                                                                      Drugs)
new formulation   Sanofi-Aventis   · King Pharmaceuticals ·Metered-DoseInhalers- Dosage                  NSAIDs (Non Steroidal
                                   Inc.                   MDI                    Strength(cromolyn       Antiinflammatory
                                   (USA,Canada,Puerto                            sodium) : 5 milligram ; Drugs)
                                   Rico)· Astellas Pharma                        Dosing Frequency: 4
                                   Inc. (Japan)                                  per day
new formulation   Sanofi-           · King Pharmaceuticals ·LiquidInhalers/Nebuliz Dosage                 NSAIDs (Non Steroidal
                  Aventis(Europe)   Inc. (USA)· Catalent   ers                     Strength(cromolyn      Antiinflammatory
                                    Pharma Solutions,                              sodium) : 20 milligram Drugs)
                                    Inc.· Astellas Pharma                          ; Dosing Frequency: 4
                                    Inc. (Japan)                                   per day
generic   DEY L.P.(USA)   -   ·LiquidInhalers/Nebuliz Dosage                NSAIDs (Non Steroidal
                              ers                     Strength(cromolyn     Antiinflammatory
                                                      sodium) : 1 percent ; Drugs)
                                                      Dosing Frequency: 4 a
                                                      day
generic   Morton Grove      -   ·LiquidInhalers/Nebuliz Dosage                NSAIDs (Non Steroidal
          Pharmaceuticals       ers                     Strength(cromolyn     Antiinflammatory
          Inc.(USA)                                     sodium) : 1 percent   Drugs)
new formulation   Sanofi-           · Sanofi-Aventis (USA) ·DryPowderInhalers-   Dosage                 NSAIDs (Non Steroidal
                  Aventis(Europe)                          DPI                   Strength(cromolyn      Antiinflammatory
                                                                                 sodium) : 20 milligram Drugs)
                                                                                 ; Dosing Frequency: 4
                                                                                 per day
new formulation   Sanofi-              · King Pharmaceuticals ·Metered-DoseInhalers- Dosage                  NSAIDs (Non Steroidal
                  Aventis(Australia)   Inc. (USA)             MDI                    Strength(cromolyn       Antiinflammatory
                                                                                     sodium) : 5 milligram ; Drugs)
                                                                                     Dosing Frequency: 4
                                                                                     per day
new formulation   Teva Pharmaceutical -     ·DryPowderInhalers-   -   mACh (Muscarinic
                  Industries Ltd.(Europe)   DPI                       Acetylcholine)
                                                                      Receptor Antagonists
new formulation   Galen Limited(UK)   -   ·LiquidInhalers/Nebuliz -   mACh (Muscarinic
                                          ers                         Acetylcholine)
                                                                      Receptor Antagonists
new formulation   Pari Pharma GmbH     -                     ·LiquidInhalers/Nebuliz Dosage              Mast Cell Stabilizers
                                                             ers                     Strength(sodium
                                                                                     cromoglycate) : 1
                                                                                     percent




NCE               Jado Technologies    -                     -                      -                    -
                  GmbH
BLA               KaloBios             -                     ·INJECTABLES           -                    -
                  Pharmaceuticals




NCE               Kyorin               · MediciNova, Inc. (ex- ·ORALDRUGDELIVER Dosage                  LT (Leukotriene)
                  Pharmaceutical(Japan Asia)                   Y                Strengths(tipelukast) : Receptor Antagonists
                  )                                                             500, 750 milligram ;
                                                                                Dosing Frequency: 1-2
                                                                                per day
NCE   Abbott Laboratories     -   ·Metered-DoseInhalers- -   Corticosteroids·Beta 2
      Inc.                        MDI                        Adrenergic Agonists




NCE   Abbott Laboratories     -   ·Metered-DoseInhalers- -   -
      Inc.                        MDI
NCE   Cellceutix              -   -                      -   -
      Pharmaceuticals, Inc.

NCE   Kaken Pharmaceutical -      -                      -   LTD4 Receptor
      Co                                                     Antagonists·TXA2
                                                             (Thromboxane A2)
                                                             Receptor Antagonists
NCE   Kemin Pharma         -                     -                 -   -

NCE   Kissei Pharmaceutical · MediciNova, Inc. (ex- ·INJECTABLES   -   Beta 2 Adrenergic
      Company(Asia,Japan) Japan)                                       Agonists
NCE   Kyowa Hakko Kirin      -                     -                     -                     PDE-4
      Co., Ltd.(France,UK)                                                                     (Phosphodiesterase 4)
                                                                                               Inhibitors




NCE   Kyorin                · MediciNova, Inc.     ·ORALDRUGDELIVER Dosage                   PDE
      Pharmaceutical(Japan, (USA)· Handok          Y                Strength(ibudilast) : 10 (phosphodiesterase)
      South Korea)          Pharmaceuticals Co.,                    milligram ; Dosing       Inhibitors
                            Ltd (Korea)                             Frequency: 2-3 per
                                                                    day




NCE   Endacea, Inc.          -                     ·INHALATION           -                     A1A Adenosine
                                                                                               Receptor Antagonists
NCE   Endacea, Inc.          -                     ·ORALDRUGDELIVER -                          A1A Adenosine
                                                   Y                                           Receptor Antagonists
NCE   Almirall               -                     -                -                          A2B Adenosine
                                                                                               Receptor Antagonists
NCE   Almirall               -                     ·DryPowderInhalers-   -                     -
                                                   DPI
NCE   Almirall               -                     ·DryPowderInhalers-   ; Dosing Frequency: 1 -
                                                   DPI                   per day




NCE   Lotus Pharmaceuticals -                      -                     -                     -
      Inc.(China)
NCE   Tianyin               -   ·ORALDRUGDELIVER Dosage Strength : 250 -
      Pharmaceutical Co.,       Y                milligram
      Inc.(China)
NCE   Proteo Biotech AG     -   -                  -                   Tryptase Inhibitors
new formulation   Nitec Pharma    · Merck KGaA       ·ColonicRelease·OralP Dosage                Corticosteroids
                  AG(Europe)      (Austria)· Nitec   ulsedMR               Strengths(prednisone)
                                  Pharma AG (USA)·                         : 1, 2, 5 milligram
                                  Mundipharma AG·
                                  Merck KGaA
                                  (Germany)




NCE               Sepracor Inc.   -                  -                     -                     Beta Agonists
new formulation   Meda AB   -   ·NasalDelivery   Dosage                   Corticosteroids
                                                 Strengths(loteprednol
                                                 etabonate) : 0.1, 0.2,
                                                 0.4 milligram
new formulation   Almirall   -   ·DryPowderInhalers-   -   Corticosteroids
                                 DPI
NCE   Meda AB(USA)   -   ·ORALDRUGDELIVER Dosage                  Xanthines·PDE
                         Y                Strengths(diphylline) : (phosphodiesterase)
                                          200, 400 milligram ;    Inhibitors
                                          Dosing Frequency: 4 a
                                          day
BLA               Biogen Idec Inc.(USA) -   ·INJECTABLES      -   Anti-CD23




NCE               ActivBiotics          -   -                 -   -




new formulation   MAP Pharmaceuticals -     ·SCF,Inhalation   -   -
                  Inc.
new formulation   MAP Pharmaceuticals -                       ·SCF,Inhalation·Metere Dosage                  Corticosteroids·Beta 2
                  Inc.                                        d-DoseInhalers-MDI     Strengths(budesonide) Adrenergic Agonists
                                                                                     : 0.104, 0.312
                                                                                     milligram Dosage
                                                                                     Strengths(formoterol) :
                                                                                     0.0054, 0.0162
                                                                                     milligram




NCE               AstraZeneca Plc(UK)   · Mitsubishi Tanabe   -                      -                       LTD4 Receptor
                                        Pharma Corporation                                                   Antagonists
                                        (Japan)
BLA   Medimmune Inc.        · Genaera Corp.   ·INJECTABLES        Dosage Strengths :   Anti-IL-9
                                                                  0.3, 1, 3, 9
                                                                  milligram/kg




NCE   Memory                -                 ·ORALDRUGDELIVER Dosage Strength : 600 PDE-4
      Pharmaceuticals Corp.                   Y                milligram             (Phosphodiesterase 4)
                                                                                     Inhibitors
new formulation   Otsuka                -   ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
                  Pharmaceutical Co.,       MDI                    Strength(procaterol     Agonists
                  Ltd.(Japan)                                      hydrochloride) : 0.01
                                                                   milligram ; Dosing
                                                                   Frequency: 1-2 a day
new formulation   Otsuka                -   ·ORALDRUGDELIVER Dosage                  Beta 2 Adrenergic
                  Pharmaceutical Co.,       Y                Strength(procaterol     Agonists
                  Ltd.(Japan)                                hydrochloride) : 0.05
                                                             milligram
new formulation   Otsuka                -   ·ORALDRUGDELIVER Dosage                 Beta 2 Adrenergic
                  Pharmaceutical Co.,       Y                Strength(procaterol    Agonists
                  Ltd.(Japan)                                hydrochloride) : 0.1
                                                             milligram
new formulation   Otsuka                -   ·INHALATION   Dosage                   Beta 2 Adrenergic
                  Pharmaceutical Co.,                     Strengths(procaterol     Agonists
                  Ltd.(Japan)                             hydrochloride) : 0.03,
                                                          0.05 milligram
new formulation   Otsuka                -   ·Metered-DoseInhalers- Dosage                 Beta 2 Adrenergic
                  Pharmaceutical Co.,       MDI                    Strength(procaterol    Agonists
                  Ltd.(Japan)                                      hydrochloride) : 0.005
                                                                   milligram
new formulation   Otsuka                -   ·ORALDRUGDELIVER Dosage                  Beta 2 Adrenergic
                  Pharmaceutical Co.,       Y                Strength(procaterol     Agonists
                  Ltd.(Japan)                                hydrochloride) : 0.05
                                                             milligram
NCE   Otsuka                -   ·ORALDRUGDELIVER Dosage                  Beta 2 Adrenergic
      Pharmaceutical Co.,       Y                Strength(procaterol     Agonists
      Ltd.(Japan)                                hydrochloride) : 0.05
                                                 milligram ; Dosing
                                                 Frequency: 1-2 per
                                                 day
new formulation   Otsuka                -   ·ORALDRUGDELIVER Dosage                 Beta 2 Adrenergic
                  Pharmaceutical Co.,       Y                Strength(procaterol    Agonists
                  Ltd.(Japan)                                hydrochloride) : 0.025
                                                             milligram ; Dosing
                                                             Frequency: 1-2 per
                                                             day
new formulation   Merck and Co Inc.      -                     ·ORALDRUGDELIVER Dosage                  COX-2
                                                               Y                Strengths(etoricoxib) : (Cyclooxygenase-2)
                                                                                5, 100 milligram        Inhibitors




BLA               CSL Ltd.               · Merck and Co Inc.   ·INJECTABLES            -                    Anti-IL13




NCE               Millennium             · Sanofi-Aventis      -                       -                    Anti-CRTH2
                  Pharmaceuticals        (World)
                  Inc.(North America)
NCE               Kyorin                 · MediciNova, Inc. (ex- ·OralModifiedRel.(MR) ; Dosing Frequency: 1 LT (Leukotriene)
                  Pharmaceutical(Japan   Asia)                                         per day               Receptor Antagonists
                  )
BLA               Eisai Co. Ltd          · Morphotek Inc.      ·INJECTABLES            -                    -

NCE               AnGes MG Inc.          · Meyer               ·LiquidInhalers/Nebuliz -                    NF-kB Inhibitors
                                         Pharmaceuticals       ers
                                         (North
                                         America,Europe)




NCE               Meyer                  -                     ·INJECTABLES            -                    -
                  Pharmaceuticals
NCE   Graceway              · Meda AB (Europe)   ·Metered-DoseInhalers- Dosage                   Beta 2 Adrenergic
      Pharmaceuticals LLC                        MDI                    Strength(pirbuterol      Agonists
                                                                        acetate) : 0.2 milligram
                                                                        ; Dosing Frequency: 4-
                                                                        6 per day
new formulation   Otsuka                -   ·DryPowderInhalers-   -   Beta 2 Adrenergic
                  Pharmaceutical Co.,       DPI                       Agonists
                  Ltd.(Japan)




new formulation   Miat Spa              -   ·DryPowderInhalers-   -   -
                                            DPI

new formulation   Novartis AG           -   ·DryPowderInhalers-   -   -
                                            DPI
new formulation   Novartis AG   -   ·DryPowderInhalers-   -   Corticosteroids
                                    DPI
new combination   Novartis AG   -   ·Metered-DoseInhalers- Dosage                  Corticosteroids·Beta 2
                                    MDI                    Strengths(mometason Adrenergic Agonists
                                                           e furoate) : 0.2, 0.4
                                                           milligram Dosage
                                                           Strengths(formoterol) :
                                                           0.01, 0.01 milligram ;
                                                           Dosing Frequency: 2 a
                                                           day
new formulation   Merck and Co      · Kyorin         ·INJECTABLES            -   LT (Leukotriene)
                  Inc.(USA)         Pharmaceutical                               Receptor Antagonists




NCE               EmphyCorp, Inc.   -                ·LiquidInhalers/Nebuliz -   -
                                                     ers
NCE               N30 Pharma            -                     ·LiquidInhalers/Nebuliz -                     -
                                                              ers




new formulation   NAL Pharmaceuticals   -                     ·Transdermal            ; Dosing Frequency:   -
                  Ltd.                                                                Once a day
generic           NAL Pharmaceuticals   -                     ·Transdermal            ; Dosing Frequency:   Beta 2 Adrenergic
                  Ltd.                                                                Once a day            Agonists




new formulation   NexMed, Inc.          -                      ·TransdermalEnhancer -                       -
                                                               s/Gels
NCE               Hisamitsu             · Nippon-Shinyaku Co., ·NasalDelivery       -                       -
                  Pharmaceutical Co.    LTD. (Japan)
                  Inc.
NCE               Taisho Pharmaceutical · Nissan Chemical     ·ORALDRUGDELIVER Dosage Strengths : 4, PDE
                  Co., Ltd.(Japan)      Industries (USA)·     Y                8 milligram ; Dosing  (phosphodiesterase)
                                        Indigo                                 Frequency: 2 per day Inhibitors·Thromboxan
                                        Pharmaceuticals                                              e Synthetase Inhibitors
                                        (World)· Nissan
                                        Chemical Industries
                                        (Japan)
NCE   Epigenesis             -   ·Metered-DoseInhalers- ; Dosing Frequency: 1 -
      Pharmaceuticals Inc.       MDI                    per day
NCE   Eisai Co. Ltd(Japan)   -   ·INJECTABLES   Dosage                 Xanthines
                                                Strength(aminophylline
                                                ) : 250 milligram ;
                                                Dosing Frequency: 1-2
                                                per day
NCE   Eisai Co. Ltd(Japan)   -   ·INJECTABLES   Dosage                 Xanthines
                                                Strength(aminophylline
                                                ) : 100 milligram ;
                                                Dosing Frequency: 3-4
                                                per day
NCE   Eisai Co. Ltd(Japan)   -   ·ORALDRUGDELIVER Dosage                 Xanthines
                                 Y                Strength(aminophylline
                                                  ) : 100 milligram ;
                                                  Dosing Frequency: 3-4
                                                  per day
NCE   A. Menarini Pharma    -                    ·INJECTABLES   -   NK2 (Neurokinin-2)
                                                                    Antagonists




NCE   Neurim                -                    -              -   5HT2 [5-
      Pharmaceuticals                                               hydroxytryptamine2
                                                                    (serotonin)]
                                                                    Antagonists·LT
                                                                    (Leukotriene) Receptor
                                                                    Antagonists
BLA   G2 Therapies Pty Ltd. · Novo Nordisk A/S   ·INJECTABLES   -   C5a Receptor
                                                                    Antagonists
new formulation   Eisai Co. Ltd(Japan)   -   ·ORALDRUGDELIVER Dosage                 -
                                             Y                Strength(lysozyme
                                                              hydrochloride) : 200
                                                              milligram ; Dosing
                                                              Frequency: 3 per day
new formulation   Eisai Co. Ltd(Japan)   -   ·ORALDRUGDELIVER Dosage                 -
                                             Y                Strength(lysozyme
                                                              hydrochloride) : 100
                                                              milligram ; Dosing
                                                              Frequency: 3 per day
new formulation   Eisai Co. Ltd(Japan)   -   ·ORALDRUGDELIVER Dosage                  -
                                             Y                Strengths(lysozyme
                                                              hydrochloride) : 30, 90
                                                              milligram ; Dosing
                                                              Frequency: 3 per day




NCE               Nitromed Inc.          -   -                   -                    PDE
                                                                                      (phosphodiesterase)
                                                                                      Inhibitors
NCE               Nitromed Inc.     -   -                     -                      -




new formulation   Meda AB(Europe)   -   ·DryPowderInhalers-   Dosage                 Corticosteroids
                                        DPI                   Strengths(budesonide)
                                                              : 0.2, 0.4 milligram ;
                                                              Dosing Frequency: 1-2
                                                              per day
new formulation   Meda AB(ex-US)   -   ·OralModifiedRel.(MR) Dosage                  Xanthines
                                                             Strengths(theophylline)
                                                             : 175, 250 milligram ;
                                                             Dosing Frequency: 2
                                                             per day




NCE               Oxagen Ltd       -   ·ORALDRUGDELIVER -                           CRTH2 Antagonists
                                       Y
NCE               Orexo AB         -   ·ORALDRUGDELIVER -                           Eoxin Inhibitor
                                       Y

NCE               Orexo AB         -   ·ORALDRUGDELIVER Dosage Strengths : 15, PDE-4
                                       Y                50 milligram           (Phosphodiesterase 4)
                                                                               Inhibitors



NCE               Orexo AB         -   ·ORALDRUGDELIVER -                           PDE-4
                                       Y                                            (Phosphodiesterase 4)
                                                                                    Inhibitors
new formulation   Orexo AB             -                  -              -   -




BLA               Celtic Pharma        -                  ·INJECTABLES   -   -
                  Management L.P.




NCE               La Jolla             · Medimmune Inc.   ·INJECTABLES   -   -
                  Pharmaceutical Co.
NCE               Orexo AB           -   ·ORALDRUGDELIVER Dosage Strengths : 15, PDE-4
                                         Y                50 milligram           (Phosphodiesterase 4)
                                                                                 Inhibitors




new formulation   Omron HealthCare   -   ·LiquidInhalers/Nebuliz -                -
                                         ers
NCE   Ono Pharmaceutical   · Schering-Plough   ·ORALDRUGDELIVER Dosage                 LT (Leukotriene)
      Co., Ltd.(Japan)     Corp. (Latin        Y                Strength(pranlukast    Receptor Antagonists
                           America,Mexico)                      hydrate) : 112.5
                                                                milligram ; Dosing
                                                                Frequency: 2 per day
new formulation   Ono Pharmaceutical   · Schering-Plough   ·ORALDRUGDELIVER Dosage                  LT (Leukotriene)
                  Co., Ltd.(Japan)     Corp. (Latin        Y                Strength(pranlukast     Receptor Antagonists
                                       America,Mexico)                      hydrate) : 70
                                                                            milligram/kg ; Dosing
                                                                            Frequency: 2 per day




new formulation   OPTIME Therapeutics, -                   ·Topical           -                     -
                  Inc.
NCE   Biomarin              · Shionogi and Co.,    ·TasteMasking   Dosage                Corticosteroids
      Pharmaceutical Inc.   Ltd. (North America)                   Strength(prednisolone
                                                                   sodium phosphate) :
                                                                   20.2 milligram
new formulation   Biomarin              · Sciele Pharma, Inc.   ·ConventionalMeltTabl Dosage                Corticosteroids
                  Pharmaceutical Inc.   (North America)         ets·TasteMasking      Strengths(prednisolon
                                                                                      e sodium phosphate) :
                                                                                      10, 15, 30 milligram




generic           Ranbaxy Laboratories -                        ·Metered-DoseInhalers- Dosage                 Corticosteroids
                  Ltd.(India)                                   MDI                    Strengths(ciclesonide)
                                                                                       : 0.08, 0.16 milligram
NCE   Oxagen Ltd           -   -                     -                     -




NCE   AstraZeneca          -   ·DryPowderInhalers-   Dosage                Beta 2 Adrenergic
      Plc(Europe)              DPI                   Strength(formoterol   Agonists
                                                     fumarate) : 0.009
                                                     milligram ; Dosing
                                                     Frequency: 1-2 per
                                                     day




NCE   Pacgen               -   -                     -                     CXCR1
      Biopharmaceuticals                                                   Antagonists·CXCR2
      Corp.                                                                Antagonists



NCE   Pfizer Inc.          -   ·ORALDRUGDELIVER ; Dosing Frequency: 2 -
                               Y                per day
NCE   Pfizer Inc.          -   ·ORALDRUGDELIVER -                       -
                               Y




NCE   Pfizer Inc.(World)   -   ·INHALATION         ; Dosing Frequency: 1 Beta 2 Adrenergic
                                                   per day               Agonists
NCE   Roche                -   -                   -                     PI3K-gamma Inhibitors


NCE   Wyeth                -   ·ORALDRUGDELIVER Dosage                  Cytosolic
                               Y                Strengths(giripladib) : Phospholipase A2
                                                50, 200, 400 milligram Inhibitors
                                                ; Dosing Frequency: 1-
                                                2 per day




NCE   Polyphor Ltd         -   -                   -                    Serine Protease
                                                                        Inhibitors
generic   Teva Pharmaceutical    · UCB Pharma (USA)   ·Metered-DoseInhalers- Dosage               Beta 2 Adrenergic
          Industries Ltd.(USA)                        MDI                    Strength(albuterol   Agonists
                                                                             sulfate) : 0.09
                                                                             milligram ; Dosing
                                                                             Frequency: 4-6 per
                                                                             day
BLA               Pieris AG              -                    ·INHALATION        -                   -




NCE               Ligand                 · Schering-Plough    ·ORALDRUGDELIVER Dosage Strengths : 1, CXCR2 Antagonists
                  Pharmaceuticals Inc.   Corp. (USA)          Y                30 milligram




NCE               Ligand                 · Daiichi             -                 -                   VCAM Antagonists
                  Pharmaceuticals Inc.   Pharmaceutical
                                         Corporation (USA)
new formulation   Penwest                · Teva Pharmaceutical ·OralMatrixMR     -                   -
                  Pharmaceuticals Co.    Industries Ltd. (USA)




NCE               Pharmaxis Ltd.         -                    -                  -                   -




NCE               Pharmaxis Ltd.         -                    -                  -                   -
new formulation   Pharmaxis Ltd.       -                  ·OralModifiedRel.(MR) -                     -




NCE               Pharmaxis Ltd.       -                  -                     -                     -
NCE               Palau Pharma         -                  -                     -                     H4 (Histamine 4)
                                                                                                      Antagonists

generic           Napp Pharmaceuticals · United           ·OralMatrixMR         Dosage                 Xanthines
                  Ltd.(UK)             Pharmaceuticals·                         Strength(aminophylline
                                       Mundipharma AG                           dihydrate) : 225
                                       (Switzerland)                            milligram ; Dosing
                                                                                Frequency: 2 per day
generic   Napp Pharmaceuticals · United           ·OralMatrixMR   Dosage                 Xanthines
          Ltd.(UK)             Pharmaceuticals·                   Strength(aminophylline
                               Mundipharma AG                     dihydrate) : 350
                               (Switzerland)                      milligram ; Dosing
                                                                  Frequency: 2 per day
generic   United                -                     ·OralMatrixMR   Dosage                 Xanthines
          Pharmaceuticals(Middl                                       Strength(aminophylline
          e East)                                                     dihydrate) : 100
                                                                      milligram




NCE       Phylogica Ltd.        · Opsona Therapeutics -               -                     -
                                Ltd.




NCE       Phytopharm Plc        -                     -               -                     -
NCE   Schering-Plough Corp. -   ·ORALDRUGDELIVER Dosage                  -
                                Y                Strengths(pleconaril) :
                                                 200, 400 milligram ;
                                                 Dosing Frequency: 2-3
                                                 per day
OTC   Cobalis Corp.   -   ·OralLozenge   Dosage                 -
                                         Strength(cyanocobala
                                         min) : 3.3 milligram ;
                                         Dosing Frequency: 2 a
                                         day
new formulation   Sheffield             -   ·LiquidInhalers/Nebuliz -   Beta 2 Adrenergic
                  Pharmaceuticals           ers                         Agonists
                  Inc(USA)




new formulation   Sheffield             -   ·LiquidInhalers/Nebuliz -   Corticosteroids
                  Pharmaceuticals Inc       ers
new formulation   Sheffield             -   ·LiquidInhalers/Nebuliz -   Mast Cell Stabilizers
                  Pharmaceuticals Inc       ers
OTC   Wyeth(USA)   -   ·Metered-DoseInhalers- Dosage                  Alpha Adrenergic
                       MDI                    Strength(epinephrine) : Agonists·Beta
                                              0.22 milligram          Adrenergic Agonists
-         Teva Pharmaceutical    -   ·Metered-DoseInhalers- -                  Beta 2 Adrenergic
          Industries Ltd.(USA)       MDI                                       Agonists




generic   United                -    ·ORALDRUGDELIVER Dosage                  H1 (Histamine 1)
          Pharmaceuticals(Middl      Y                Strength(ketotifen      Antagonists
          e East)                                     fumarate) : 1 milligram
                                                      ; Dosing Frequency: 2
                                                      per day
NCE   Synairgen             -   -                      -   -




NCE   Schering-Plough Corp. -   ·Metered-DoseInhalers- -   Beta 2 Adrenergic
                                MDI                        Agonists
new formulation   Schering-Plough   -   ·Metered-DoseInhalers- Dosage               Beta 2 Adrenergic
                  Corp.(USA)            MDI                    Strength(albuterol   Agonists
                                                               sulfate) : 0.12
                                                               milligram ; Dosing
                                                               Frequency: 4-6 per
                                                               day
new formulation   AstraZeneca Plc(ex-   -   ·Metered-DoseInhalers- Dosage                Corticosteroids
                  US,Europe,Denmark,F       MDI                    Strengths(budesonide)
                  inland,Hungary,Portug                            : 0.1, 0.2 milligram
                  al,Spain)




new formulation   AstraZeneca Plc(USA) -    ·Metered-DoseInhalers- Dosage                 Corticosteroids
                                            MDI                    Strength(budesonide) :
                                                                   0.2 milligram ; Dosing
                                                                   Frequency: 2 per day
new formulation   AstraZeneca         -   ·LiquidInhalers/Nebuliz Dosage                Corticosteroids
                  Plc(USA,UK)             ers                     Strengths(budesonide)
                                                                  : 1, 2 milligram ;
                                                                  Dosing Frequency: 2
                                                                  per day




generic           Par Pharmaceutical  -   ·LiquidInhalers/Nebuliz ; Dosing Frequency: 2 Corticosteroids
                  Companies Inc.(USA)     ers                     per day
new formulation   AstraZeneca           -   ·DryPowderInhalers-    Dosage                    Corticosteroids
                  Plc(USA,UK)               DPI                    Strengths(budesonide)
                                                                   : 0.1, 0.2, 0.4 milligram
                                                                   ; Dosing Frequency: 2
                                                                   per day




new formulation   Nektar Therapeutics   -   ·InhalationFormulation -                        Beta 2 Adrenergic
                                            s                                               Agonists




NCE               Novartis AG           -   ·DryPowderInhalers-    Dosage                  Beta 2 Adrenergic
                                            DPI                    Strengths(indacaterol) Agonists
                                                                   : 0.075, 0.15, 0.3, 0.6
                                                                   milligram ; Dosing
                                                                   Frequency: 1 per day

NCE               Novartis AG           -   ·INHALATION            -                        -
NCE               Novartis AG           -   -                      -                        CCR3 Antagonists
NCE               Idera Pharmaceuticals · Novartis AG (USA)   -                     -                     TLR9 (Toll-like
                  Inc.                                                                                    receptors 9) Agonists




new combination   Novartis AG(World)    -                     ·DryPowderInhalers-   ; Dosing Frequency: 1 Beta 2 Adrenergic
                                                              DPI                   a day                 Agonists·Corticosteroi
                                                                                                          ds
generic           Teva Pharmaceutical -     ·Metered-DoseInhalers- Dosage               Corticosteroids
                  Industries Ltd.(Europe)   MDI                    Strengths(beclometha
                                                                   sone dipropionate) :
                                                                   0.5, 0.1 milligram ;
                                                                   Dosing Frequency: 2
                                                                   per day




new formulation   Teva Pharmaceutical -     ·Metered-DoseInhalers- Dosage                Corticosteroids
                  Industries Ltd.(Europe)   MDI                    Strengths(beclometha
                                                                   sone dipropionate) :
                                                                   0.05, 0.1 milligram ;
                                                                   Dosing Frequency: 2
                                                                   per day
new formulation   Teva Pharmaceutical   · 3M Health Care      ·Metered-DoseInhalers- Dosage                Corticosteroids
                  Industries Ltd.(UK)                         MDI                    Strengths(beclometha
                                                                                     sone dipropionate) :
                                                                                     0.05, 0.1 milligram ;
                                                                                     Dosing Frequency: 2 a
                                                                                     day




new formulation   3M Health Care        · Teva Pharmaceutical ·Metered-DoseInhalers- Dosage                 Corticosteroids
                                        Industries Ltd. (USA)· MDI                   Strengths(beclometha
                                        Lavipharm SA·                                sone dipropionate) :
                                        Dainippon Sumitomo                           0.04, 0.08 milligram ;
                                        Pharmaceutical                               Dosing Frequency: 2
                                        (Japan)· Schering-                           per day
                                        Plough Corp. (Japan)
BLA   Genmab(World)           · Roche                ·INJECTABLES          Dosage Strength :   -
                                                                           0.0015 milligram




NCE   Rigel Pharmaceuticals, · Pfizer Inc. (World)   ·DryPowderInhalers-   -                   SYK (Spleen Tyrosine
      Inc.                                           DPI                                       Kinase) Inhibitors
NCE               Roche            -         ·ORALDRUGDELIVER Dosage                 alpha4beta1 (VLA-4)
                                             Y                Strength(valategrast   Integrin Antagonists
                                                              hydrochloride) : 200
                                                              milligram




BLA               Genmab           · Roche   ·INJECTABLES          -                 Anti-CD134




new formulation   Respirics Inc.   -         ·DryPowderInhalers-   -                 Beta 2 Adrenergic
                                             DPI                                     Agonists
new formulation   Kissei Pharmaceutical -   ·ORALDRUGDELIVER Dosage                    -
                  Company(Japan)            Y                Strength(tranilast) : 5
                                                             milligram/kg
NCE   Kissei Pharmaceutical -   ·ORALDRUGDELIVER Dosage                 -
      Company(Japan)            Y                Strength(tranilast) :
                                                 100 milligram ; Dosing
                                                 Frequency: 3 per day




NCE   Verona Pharma Plc     -   ·NasalDelivery      -                   PDE-4
                                                                        (Phosphodiesterase 4)
                                                                        Inhibitors
NCE       Resolvyx               -   ·ORALDRUGDELIVER -                            -
          Pharmaceuticals Inc.       Y




generic   Nephron                -   ·LiquidInhalers/Nebuliz Dosage                 Beta Adrenergic
          Pharmaceuticals            ers                     Strength(racepinephrin Agonists·Alpha
          Corp.(USA)                                         e) : 2.25 percent      Adrenergic Agonists
BLA   Ception Therapeutics   -   ·INJECTABLES          Dosage                   Anti-IL-5R··Anti-IL-5R
                                                       Strengths(reslizumab)
                                                       : 1, 2, 3 milligram/kg ;
                                                       Dosing Frequency: 1
                                                       per month




NCE   Teva Pharmaceutical    -   ·DryPowderInhalers-   -                       Corticosteroids
      Industries Ltd.(USA)       DPI


NCE   Respivert, Inc         -   -                     -                       -
new formulation   GlaxoSmithKline   -                        ·LiquidInhalers/Nebuliz Dosage                  mACh (Muscarinic
                  Plc(UK)                                    ers                     Strengths(ipratropium Acetylcholine)
                                                                                     bromide hydrate) : 0.1, Receptor Antagonists
                                                                                     0.5 milligram ; Dosing
                                                                                     Frequency: 1-4 per
                                                                                     day




BLA               Arriva            · Baxter International   ·LiquidInhalers/Nebuliz Dosage Strengths : 10, -
                  Pharmaceuticals   Inc.                     ers                     50, 100, 200 milligram
new formulation   Kissei Pharmaceutical -   ·ORALDRUGDELIVER Dosage                 -
                  Company(Japan)            Y                Strength(tranilast) :
                                                             100 milligram ; Dosing
                                                             Frequency: 3 per day




NCE               Mitsubishi            -   ·ORALDRUGDELIVER Dosage                   -
                  Pharmaceutical            Y                Strength(repirinast) :
                  Corp.(Japan)                               10 percent

NCE               Mitsubishi            -   ·ORALDRUGDELIVER Dosage                   -
                  Pharmaceutical            Y                Strength(repirinast) :
                  Corp.(Japan)                               150 milligram
NCE               Shionogi and Co., Ltd. -             ·ORALDRUGDELIVER -   DP Antagonists
                                                       Y

NCE               Sanofi-Aventis         -             -                -   CRTH2 Antagonists

NCE               Sanofi-Aventis         -             -                -   A3A Adenosine
                                                                            Receptor Antagonists
NCE               Sanofi-Aventis(USA)    -             -                -   TRL9 Agonist

NCE               Sanofi-Aventis(USA)    -             -                -   DP1 Antagonist

new formulation   Dr. Rentschler Holding · Synairgen   ·INHALATION      -   Interferons
                  GmbH & Co. KG




new formulation   Dr. Rentschler Holding · Synairgen   ·INHALATION      -   Interferons
                  GmbH & Co. KG




NCE               Synairgen              -             -                -   -
NCE               Synairgen              -             -                -   -

NCE               Synairgen              -             -                -   -
NCE               Synairgen              -             -                -   -
NCE               Dainippon Sumitomo     -   ·ORALDRUGDELIVER -                            -
                  Pharmaceutical(USA)        Y


new formulation   Synairgen              -   ·LiquidInhalers/Nebuliz -                     Interferons
                                             ers




BLA               Synairgen              -   -                       -                     -




NCE               Silence Therapeutics   -   -                       -                     -
                  Plc




NCE               Sanofi-Aventis         -   -                       -                     A3A Adenosine
                                                                                           Receptor Antagonists

new formulation   Sun Pharmaceutical     -   ·DryPowderInhalers-     ; Dosing Frequency: 1 Corticosteroids
                  Industries                 DPI                     a day
new formulation   Teva Pharmaceutical   -   ·Metered-DoseInhalers- Dosage                 Beta 2 Adrenergic
                  Industries                MDI                    Strength(albuterol) :  Agonists
                  Ltd.(Europe,Mexico)                              0.1 milligram ; Dosing
                                                                   Frequency: 1-4 a day




new formulation   Teva Pharmaceutical   -   ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
                  Industries                MDI                    Strength(albuterol) :   Agonists
                  Ltd.(Europe,Mexico)                              0.1 milligram
new formulation   Lavipharm SA(ex-US) -      ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
                                             MDI                    Strength(albuterol) :   Agonists
                                                                    0.1 milligram




new formulation   Teva Pharmaceutical -      ·DryPowderInhalers-     -                      Beta 2 Adrenergic
                  Industries Ltd.(Europe)    DPI                                            Agonists




new formulation   Phares Drug Delivery   -   ·Metered-DoseInhalers- -                       Beta 2 Adrenergic
                  AG                         MDI·InhalationFormula                          Agonists
                                             tions
new formulation   Galen Limited   -   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                                      ers                     Strengths(albuterol) :   Agonists
                                                              2.5, 5 milligram ;
                                                              Dosing Frequency: 4
                                                              per day




new formulation   Akela Pharma    -   ·DryPowderInhalers-     Dosage                 Beta 2 Adrenergic
                  Inc.(Europe)        DPI                     Strengths(albuterol) : Agonists
                                                              0.05, 0.1 milligram ;
                                                              Dosing Frequency: 1-4
                                                              a day
NCE               ICAgen Inc.(World)   -                      ·ORALDRUGDELIVER ; Dosing Frequency: 1 Potassium Channel
                                                              Y                per day               Blockers




new formulation   Sepracor Inc.        · Arrow                ·LiquidInhalers/Nebuliz -              Corticosteroids
                                       Pharmaceuticals Ltd.   ers
new formulation   GlaxoSmithKline   -   ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
                  Plc(Europe)           MDI                    Strength(salmeterol     Agonists·Corticosteroi
                                                               xinafoate) : 0.025      ds
                                                               milligram Dosage
                                                               Strengths(fluticasone
                                                               propionate) : 0.05,
                                                               0.125, 0.25 milligram ;
                                                               Dosing Frequency: 2
                                                               per day
new formulation   GlaxoSmithKline   -   ·DryPowderInhalers-   Dosage                Beta 2 Adrenergic
                  Plc(UK)               DPI                   Strength(salmeterol   Agonists
                                                              xinafoate) : 0.05
                                                              milligram ; Dosing
                                                              Frequency: 2 for 2
                                                              days
new formulation   GlaxoSmithKline   · Almirall (Spain)   ·DryPowderInhalers-    Dosage                Beta 2 Adrenergic
                  Plc(USA,UK)                            DPI                    Strength(salmeterol   Agonists
                                                                                xinafoate) : 0.05
                                                                                milligram ; Dosing
                                                                                Frequency: Once a
                                                                                day




new formulation   GlaxoSmithKline   -                    ·Metered-DoseInhalers- Dosage                Beta 2 Adrenergic
                  Plc(Europe)                            MDI                    Strength(salmeterol   Agonists
                                                                                xinafoate) : 0.025
                                                                                milligram ; Dosing
                                                                                Frequency: 2 a day
NCE   GlaxoSmithKline   -   ·Metered-DoseInhalers- Dosage                 Beta 2 Adrenergic
      Plc(USA,Europe)       MDI                    Strength(salmeterol    Agonists
                                                   xinafoate) : 0.021
                                                   milligram ; Dosing
                                                   Frequency: 2 per day
BLA   Centocor   · Medarex Inc.        ·DisposableAutoinjecto Dosage                 Anti-TNF
                 (USA,Canada)·         rs·PrefillableSyringes/ Strength(golimumab) :
                 Schering-Plough Corp. Cartridges              50 milligram ; Dosing
                 (Europe)· Janssen                             Frequency: 1 a month
                 Pharmaceutica
                 Products, LP (Japan)·
                 Mitsubishi Tanabe
                 Pharma Corporation
                 (Japan)
new formulation   Merck and Co   -   ·ChewableTablets/Gu   Dosage                LT (Leukotriene)
                  Inc.(USA,UK)       m                     Strengths(montelukast Receptor Antagonists
                                                           sodium) : 4, 5
                                                           milligram ; Dosing
                                                           Frequency: 1 per day
new formulation   Merck and Co   · Merck and Co Inc.   ·ORALDRUGDELIVER Dosage                  LT (Leukotriene)
                  Inc.(USA)      (UK)· Kyorin          Y                Strength(montelukast Receptor Antagonists
                                 Pharmaceutical                         sodium) : 4 milligram ;
                                 (Japan)                                Dosing Frequency: 1
                                                                        per day
NCE   Merck and Co        · Merck and Co Inc.   ·ORALDRUGDELIVER Dosage                LT (Leukotriene)
      Inc.(USA)           (UK)· Kyorin          Y                Strengths(montelukast Receptor Antagonists
                          Pharmaceutical                         sodium) : 10, 5
                          (Japan)                                milligram ; Dosing
                                                                 Frequency: 1 per day




NCE   Merck and Co Inc.   -                     ·INHALATION         -                   -
new formulation   Takeda               -   ·ORALDRUGDELIVER Dosage               Interleukins
                  Pharmaceutical Co.       Y                Strengths(amlexanox)
                  Ltd.(Japan)                               : 25, 50 milligram ;
                                                            Dosing Frequency: 3
                                                            per day
new formulation   Boehringer          · Pfizer Inc.   ·LiquidInhalers/Nebuliz Dosage               mACh (Muscarinic
                  Ingelheim(Europe)                   ers                     Strength(tiotropium  Acetylcholine)
                                                                              bromide monohydrate) Receptor Antagonists
                                                                              : 0.025 milligram ;
                                                                              Dosing Frequency: 1
                                                                              per day
NCE   Boehringer          · Pfizer Inc. (World)   ·DryPowderInhalers-   Dosage               mACh (Muscarinic
      Ingelheim(Europe)                           DPI                   Strength(tiotropium  Acetylcholine)
                                                                        bromide monohydrate) Receptor Antagonists
                                                                        : 0.018 milligram ;
                                                                        Dosing Frequency: 1
                                                                        per day
NCE   Boehringer Ingelheim   · Teijin Pharma Ltd.   ·ORALDRUGDELIVER Dosage                   Beta 2 Adrenergic
                             (Japan)                Y                Strengths(clenbuterol    Agonists
                                                                     hydrochloride) : 0.01,
                                                                     0.02 milligram ;
                                                                     Dosing Frequency: 2
                                                                     per day
new combination   AstraZeneca Plc(USA) -   ·Metered-DoseInhalers- Dosage                 Corticosteroids·Beta 2
                                           MDI                    Strengths(budesonide) Adrenergic Agonists
                                                                  : 0.08, 0.16 milligram
                                                                  Dosage
                                                                  Strengths(formoterol
                                                                  fumarate dihydrate) :
                                                                  0.0045, 0.0045
                                                                  milligram ; Dosing
                                                                  Frequency: 2 per day
new combination   AstraZeneca Plc(ex-   -   ·DryPowderInhalers-   Dosage                  Corticosteroids·Beta 2
                  US)                       DPI                   Strengths(budesonide) Adrenergic Agonists
                                                                  : 0.08, 0.16, 0.32
                                                                  milligram Dosage
                                                                  Strengths(formoterol) :
                                                                  0.0045, 0.0045, 0.009
                                                                  milligram ; Dosing
                                                                  Frequency: 1-2 per
                                                                  day
BLA   Synairgen            -          ·INHALATION   -   Growth Factors




NCE   Synta Pharmaceuticals · Roche   -             -   CRAC Channel
      Corp.                                             Inhibitors


NCE   Targepeutics, Inc.   -          ·INHALATION   -   Interleukin 13
                                                        Receptor Antagonists




NCE   Targepeutics, Inc.   -          ·INHALATION   -   Interleukin 13
                                                        Receptor Antagonists
NCE   Targepeutics, Inc.     -                      ·INHALATION              -                      Interleukin 13
                                                                                                    Receptor Antagonists




NCE   Revotar                -                      ·INHALATION              -                      Selectin Antagonists
      Biopharmaceuticals
      AG

NCE   Encysive               -                      -                        -                      CCR3 Antagonists
      Pharmaceuticals Inc.
NCE   Pfizer Inc.            · Schering-Plough      ·ORALDRUGDELIVER -                              alpha4beta1 (VLA-4)
                             Corp. (World)          Y                                               Integrin Antagonists
NCE   TargeGen Inc.          -                      ·Cyclodextrins/Solubiliz -                      Selective PI3
                                                    ers-Injectable                                  (Phosphoinositide 3)
                                                                                                    kinase



NCE   Tsumura & Co.(Japan) -                        ·ORALDRUGDELIVER -                              -
                                                    Y
BLA   Tanox, Inc.            -                      ·INJECTABLES     -                              Anti-IL13




NCE   Nicox SA               · Topigen              ·INHALATION              Dosage Strength(nitric -
                             Pharmaceuticals Inc.                            oxide-donating
                             (North America)                                 derivative of
                                                                             budesonide) : 0.6
                                                                             milligram ; Dosing
                                                                             Frequency: 2 per day
NCE   Topigen                -   ·LiquidInhalers/Nebuliz Dosage Strengths :      -
      Pharmaceuticals Inc.       ers                     0.25, 0.5 milligram ;
                                                         Dosing Frequency: 1
                                                         per day




NCE   Hydra Biosciences      -   -                       -                       TRPA1 Antagonists
new combination   Meda AB(USA)   -   ·ORALDRUGDELIVER Dosage                   H1 (Histamine 1)
                                     Y                Strength(carbetapenta Antagonists·Alpha
                                                      ne tannate) : 30         Adrenergic Agonists
                                                      milligram Dosage
                                                      Strength(pyrilamine
                                                      tannate) : 30 milligram
                                                      Dosage
                                                      Strength(phenylephrin
                                                      e tannate) : 5 milligram
                                                      ; Dosing Frequency: 2
                                                      per day
new combination   Meda AB(USA)        -   ·ORALDRUGDELIVER Dosage                  H1 (Histamine 1)
                                          Y                Strength(carbetapenta Antagonists·Alpha
                                                           ne tannate) : 60        Adrenergic Agonists
                                                           milligram Dosage
                                                           Strength(pyrilamine
                                                           tannate) : 40 milligram
                                                           Dosage
                                                           Strength(phenylephrin
                                                           e tannate) : 10
                                                           milligram ; Dosing
                                                           Frequency: 2 per day




generic           Akela Pharma Inc.   -   ·DryPowderInhalers-   -                   Corticosteroids
                                          DPI
generic           Akela Pharma Inc.   -   ·DryPowderInhalers-    -   Beta 2 Adrenergic
                                          DPI                        Agonists




new formulation   Kyowa Hakko Kirin   -   ·DryPowderInhalers-    -   Corticosteroids
                  Co., Ltd.(Japan)        DPI




new formulation   MAP Pharmaceuticals -   ·Metered-DoseInhalers- -   Corticosteroids
                  Inc.                    MDI
generic   Osmotica         · Laboratorios Phoenix ·OralOsmoticMR   Dosage                 Xanthines
          Pharmaceutical   (Argentina)                             Strength(theophylline)
                                                                   : 300 milligram ;
                                                                   Dosing Frequency: 1
                                                                   per day
new formulation   Ventaira(USA)   -   ·LiquidInhalers/Nebuliz -   Beta 2 Adrenergic
                                      ers                         Agonists
new formulation   Schering-Plough   · Mitsubishi Tanabe   ·OralBarrierFilmTablet Dosage                  Xanthines
                  Corp.(USA)        Pharma Corporation    &Microcaps             Strengths(theophylline)
                                    (Japan)                                      : 100, 200, 300, 450
                                                                                 milligram ; Dosing
                                                                                 Frequency: 127 for 2
                                                                                 days
new formulation   Schering-Plough Corp. · Mitsubishi         ·OralBarrierFilmTablet Dosage                  Xanthines
                                        Pharmaceutical Corp. &Microcaps             Strengths(theophylline)
                                        (Japan)                                     : 50, 75, 125, 200
                                                                                    milligram ; Dosing
                                                                                    Frequency: 2-3 per
                                                                                    day
generic   Sun Pharmaceutical   -                ·OralModifiedRel.(MR) Dosage                  Xanthines
          Industries(USA)                                             Strengths(theophylline)
                                                                      : 300, 400, 450, 600
                                                                      milligram




generic   URL Pharma, Inc.     · Lavipharm SA   ·OralBarrierFilmTablet Dosage                  Xanthines
                                                &Microcaps             Strengths(theophylline)
                                                                       : 200, 300 milligram
generic   United                -   ·OralBarrierFilmTablet Dosage                  Xanthines
          Pharmaceuticals(Middl     &Microcaps             Strengths(theophylline)
          e East)                                          : 200, 300 milligram
new formulation   Eisai Co. Ltd(Japan)   -   ·OralMatrixMR   Dosage                 Xanthines
                                                             Strength(theophylline)
                                                             : 50 percent ; Dosing
                                                             Frequency: 2 per day
new formulation   Eisai Co. Ltd(Japan)   -   ·OralMatrixMR   Dosage                  Xanthines
                                                             Strengths(theophylline)
                                                             : 50, 100, 200
                                                             milligram ; Dosing
                                                             Frequency: 2 per day
generic   Galenix             -   ·OralMatrixMR   Dosage                 Xanthines
                                                  Strength(theophylline)
                                                  : 300 milligram




generic   SCOLR Pharma Inc.   -   ·OralMatrixMR   -                     Xanthines
generic   Forest Laboratories   -   ·OralBarrierFilmTablet Dosage                  Xanthines
          Inc(USA)                  &Microcaps             Strengths(theophylline)
                                                           : 100, 125, 200, 300
                                                           milligram ; Dosing
                                                           Frequency: 2 per day




generic   Forest Laboratories   -   ·OralModifiedRel.(MR) Dosage                  Xanthines
          Inc(USA)                                        Strengths(theophylline)
                                                          : 100, 200, 300, 450
                                                          milligram ; Dosing
                                                          Frequency: 2 per day
new formulation   Sanofi-                -   ·Metered-DoseInhalers- Dosage                  Mast Cell Stabilizers
                  Aventis(Europe,Austral     MDI                    Strength(nedocromil
                  ia)                                               sodium) : 2 milligram ;
                                                                    Dosing Frequency: 2-4
                                                                    a day
NCE   Sanofi-Aventis   · King Pharmaceuticals ·Metered-DoseInhalers- Dosage                Mast Cell Stabilizers
                       Inc. (USA)             MDI                    Strength(nedocromil
                                                                     sodium) : 1.75
                                                                     milligram ; Dosing
                                                                     Frequency: 4 a day
new formulation   Ventaira          -   ·LiquidInhalers/Nebuliz -   Corticosteroids
                                        ers




new formulation   Nipro Patch Co.   -   ·PatchesDrug-in-        -   -
                  Ltd.(Japan)           Adhesive
new formulation   LTS Lohmann            -   ·PatchesDrug-in-        -   Beta 2 Adrenergic
                                             Adhesive                    Agonists




new formulation   CyDex                  -   ·Metered-DoseInhalers- -    -
                  Pharmaceuticals, Inc       MDI·LiquidInhalers/Ne
                                             bulizers

NCE               Ventaira               -   ·LiquidInhalers/Nebuliz -   -
                                             ers


NCE               Abbott Laboratories    -   ·LiquidInhalers/Nebuliz -   -
                  Inc.                       ers

NCE               Viasys Healthcare      -   ·LiquidInhalers/Nebuliz -   -
                                             ers
generic           Otsuka                · Purdue Pharma   ·OralMatrixMR          Dosage                  Xanthines
                  Pharmaceutical Co.,   (USA)                                    Strengths(theophylline)
                  Ltd.(Japan)                                                    : 400, 600 milligram ;
                                                                                 Dosing Frequency: 1
                                                                                 per day




new formulation   MAP Pharmaceuticals · AstraZeneca Plc   ·DrugNanoparticles,Inh Dosage                   Corticosteroids
                  Inc.(USA)           (World)             alation·LiquidInhalers/ Strengths(budesonide)
                                                          Nebulizers              : 0.135, 0.25 milligram
                                                                                  ; Dosing Frequency: 2
                                                                                  per day




NCE               Grupo Uriach          -                 -                      -                       alpha4beta1 (VLA-4)
                                                                                                         Integrin Antagonists
generic           Vectura Group Plc   · Sandoz   ·DryPowderInhalers-   -   -
                                                 DPI




generic           Vectura Group Plc   · Sandoz   ·DryPowderInhalers-   -   -
                                                 DPI




new formulation   Vectura Group Plc   -          ·DryPowderInhalers-   -   -
                                                 DPI
BLA   GlaxoSmithKline Plc   -   -                     -   -


NCE   Cordex Pharma, Inc.   -   ·DryPowderInhalers-   -   -
                                DPI




NCE   PowerVerde Systems, -     ·INHALATION           -   -
      Inc.
NCE   Boehringer         -   ·DryPowderInhalers-   -   -
      Ingelheim(World)       DPI
new combination   GlaxoSmithKline   · GlaxoSmithKline Plc   ·Metered-DoseInhalers- Dosage                Beta 2 Adrenergic
                  Plc(ex-US)        (UK)                    MDI                    Strength(albuterol) : Agonists·Corticosteroi
                                                                                   0.1 milligram Dosage ds
                                                                                   Strength(beclomethas
                                                                                   one dipropionate) :
                                                                                   0.05 milligram ;
                                                                                   Dosing Frequency: 3-4
                                                                                   per day
new combination   GlaxoSmithKline   -   ·DryPowderInhalers-   Dosage                Beta 2 Adrenergic
                  Plc(Europe)           DPI                   Strengths(albuterol   Agonists·Corticosteroi
                                                              sulfate) : 0.2, 0.4   ds
                                                              milligram Dosage
                                                              Strengths(beclometha
                                                              sone dipropionate) :
                                                              0.1, 0.2 milligram ;
                                                              Dosing Frequency: 3-4
                                                              a day
new formulation   Meda AB(Europe)   -   ·DryPowderInhalers-   Dosage                  Beta 2 Adrenergic
                                        DPI                   Strength(albuterol) :   Agonists
                                                              0.1 milligram
new formulation   GlaxoSmithKline   -   ·DryPowderInhalers-   Dosage                 Beta 2 Adrenergic
                  Plc(UK)               DPI                   Strengths(albuterol    Agonists
                                                              sulfate) : 0.2, 0.4
                                                              milligram ; Dosing
                                                              Frequency: 1-4 a day
new formulation   GlaxoSmithKline   -   ·DryPowderInhalers-   Dosage                   Beta 2 Adrenergic
                  Plc(UK)               DPI                   Strength(albuterol       Agonists
                                                              sulfate) : 0.2 milligram
                                                              ; Dosing Frequency: 4
                                                              a day
NCE   GlaxoSmithKline   -   ·Metered-DoseInhalers- Dosage                Beta 2 Adrenergic
      Plc(USA)              MDI                    Strength(albuterol) : Agonists
                                                   0.09 milligram ;
                                                   Dosing Frequency: 2-4
                                                   per day
generic           Amphastar         -                       ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
                  Pharmaceuticals                           MDI                    Strength(albuterol) :   Agonists
                  Inc.(USA)                                                        0.09 milligram




new formulation   GlaxoSmithKline   · GlaxoSmithKline Plc   ·LiquidInhalers/Nebuliz Dosage                   Beta 2 Adrenergic
                  Plc(Europe)       (USA)                   ers                     Strength(albuterol       Agonists
                                                                                    sulfate) : 2.5 milligram
                                                                                    ; Dosing Frequency: 3-
                                                                                    4 per day
new formulation   GlaxoSmithKline   · Roxane Laboratories ·LiquidInhalers/Nebuliz Dosage                 Beta 2 Adrenergic
                  Plc(Europe)       Inc. (USA)            ers                     Strengths(albuterol    Agonists
                                                                                  sulfate) : 2.5, 5
                                                                                  milligram ; Dosing
                                                                                  Frequency: 4 per day




new formulation   GlaxoSmithKline   · GlaxoSmithKline Plc   ·DryPowderInhalers-   Dosage                 Beta 2 Adrenergic
                  Plc(Europe)       (USA)                   DPI                   Strengths(albuterol    Agonists
                                                                                  sulfate) : 0.2, 0.4
                                                                                  milligram ; Dosing
                                                                                  Frequency: 1-4 a day
new formulation   GlaxoSmithKline   · GlaxoSmithKline Plc   ·OralLiquidSolution   Dosage                 Beta 2 Adrenergic
                  Plc(UK)           (USA)                                         Strengths(albuterol    Agonists
                                                                                  sulfate) : 1, 2, 4
                                                                                  milligram ; Dosing
                                                                                  Frequency: 3-4 a day
new formulation   GlaxoSmithKline   · GlaxoSmithKline Plc   ·Metered-DoseInhalers- Dosage                 Beta 2 Adrenergic
                  Plc(USA)          (UK)                    MDI                    Strength(albuterol     Agonists
                                                                                   sulfate) : 0.12
                                                                                   milligram ; Dosing
                                                                                   Frequency: 1-4 a day
NCE   GlaxoSmithKline   -   ·NasalDelivery          Dosage                 Corticosteroids
      Plc(USA)                                      Strength(fluticasone
                                                    furoate) : 0.0275
                                                    milligram ; Dosing
                                                    Frequency: 1 per day




NCE   AstraZeneca Plc   -   ·LiquidInhalers/Nebuliz -                      Beta 2 Adrenergic
                            ers                                            Agonists
new formulation   Teva Pharmaceutical    -   ·Metered-DoseInhalers- -   Beta 2 Adrenergic
                  Industries Ltd.            MDI                        Agonists




new formulation   Teva Pharmaceutical    -   ·Metered-DoseInhalers- -   Beta 2 Adrenergic
                  Industries Ltd.(USA)       MDI                        Agonists
new formulation   GlaxoSmithKline   · GlaxoSmithKline Plc   ·OralOsmoticMR        Dosage                    Beta 2 Adrenergic
                  Plc(UK)           (USA)                                         Strengths(albuterol       Agonists
                                                                                  sulfate) : 4, 8 milligram
                                                                                  ; Dosing Frequency: 1
                                                                                  per day




new formulation   Pfizer Inc.       -                       ·DryPowderInhalers-   -                       Beta 2 Adrenergic
                                                            DPI                                           Agonists
BLA               Tanox, Inc.(USA)   · Genentech Inc.     ·INJECTABLES            Dosage                   Anti-IgE
                                     (USA)· Novartis AG                           Strengths(omalizumab
                                     (ex-US,Japan)· PDL                           ) : 150, 375 milligram ;
                                     Biopharma Inc.                               Dosing Frequency: 1-2
                                                                                  per month




new formulation   Genentech Inc.     · Novartis AG        ·PrefillableSyringes/Ca -                       Anti-IgE
                                                          rtridges
new formulation   Sepracor Inc.(USA)   -   ·Metered-DoseInhalers- Dosage                  Beta 2 Adrenergic
                                           MDI                    Strength(levalbuterol   Agonists
                                                                  tartrate) : 0.09
                                                                  milligram ; Dosing
                                                                  Frequency: 4-6 per
                                                                  day
generic   DEY L.P.(USA)   -   ·LiquidInhalers/Nebuliz -   Beta 2 Adrenergic
                              ers                         Agonists
NCE   Abbott Laboratories   · Cornerstone       ·ORALDRUGDELIVER Dosage                 5-lipoxygenase
      Inc.                  Therapeutics Inc.   Y                Strength(zileuton) :   Inhibitors
                            (USA)· DEY L.P.                      600 milligram ; Dosing
                            (USA)                                Frequency: 4 per day
BLA               Facet Biotech        · Biogen Idec Inc.    ·INJECTABLES       Dosage                 Anti-IL-2R
                  Corporation(USA,Euro (World)                                  Strength(daclizumab) :
                  pe)                                                           1 milligram/kg ;
                                                                                Dosing Frequency: 1
                                                                                for 2 weeks




new formulation   Asahi Kasei           · Alfresa Holdings   ·ORALDRUGDELIVER Dosage Strength : 0.6 -
                  Pharma(Japan)         Corp.                Y                percent
new formulation   Asahi Kasei           · Alfresa Holdings    ·ORALDRUGDELIVER -                               H1 (Histamine 1)
                  Pharma(Japan)         Corp.                 Y                                                Antagonists

NCE               Asahi Kasei           · Alfresa Holdings    ·ORALDRUGDELIVER -                               H1 (Histamine 1)
                  Pharma(Japan)         Corp.                 Y                                                Antagonists

new formulation   Abbott Laboratories   · Cornerstone         ·Cyclodextrins/Solubiliz Dosage                  5-lipoxygenase
                  Inc.                  Therapeutics Inc.     ers-Injectable           Strengths(zileuton) :   Inhibitors
                                        (World)                                        75, 150, 300, 600
                                                                                       milligram




NCE               Znomics, Inc.         -                     -                        -                       -

NCE               Britannia             · AirPharma· Bespak   ·DryPowderInhalers-      -                       Surfactants
                  Pharmaceuticals                             DPI
new formulation   Abbott Laboratories   · Cornerstone       ·OralMatrixMR   Dosage                 5-lipoxygenase
                  Inc.                  Therapeutics Inc.                   Strength(zileuton) :   Inhibitors
                                        (World)· DEY L.P.                   600 milligram ; Dosing
                                        (USA)                               Frequency: 2 a day
NCE   Discovery Laboratories -   ·LiquidInhalers/Nebuliz -   Surfactants
      Inc.                       ers




BLA   Medimmune Inc.         -   ·INJECTABLES            -   Anti-YKL-40

NCE   CGI Pharmaceuticals    -   ·ORALDRUGDELIVER -                  s
                                                             Bruton’ Tyrosine
                                 Y                           Kinase (BTK)
                                                             Inhibitors

NCE   CGI Pharmaceuticals    -   ·ORALDRUGDELIVER -                  s
                                                             Bruton’ Tyrosine
                                 Y                           Kinase (BTK)
                                                             Inhibitors

NCE   deCODE Genetics Inc. -     ·ORALDRUGDELIVER -          -
                                 Y
BLA   Evolutec Group plc    · Cobra               ·INJECTABLES   ; Dosing Frequency: 2- H4 (Histamine 4)
                            Biomanufacturing Plc.                4 per day              Antagonists




BLA   GTC Biotherapeutics   -                   ·INJECTABLES     -                     Elastase Inhibitors
      Inc.(ex-Europe)
BLA   Celtic Pharma     · Genentech Inc.   ·INJECTABLES   -   Anti-CD134
      Management L.P.   (World)· Roche




NCE   NascaCell         -                  -              -   Tryptase Inhibitors
      Technologies AG
Mechanisms            Molecule Type     PK Properties   Elimination Half Life Molecular Weight   Water Solubility
Explanation


-                     small molecule    -               -                    -                   -




Long-acting beta2     small molecule    -               -                    -                   -
agonist




PDE IV inhibitor      -                 -               -                    -                   -


Selective iNOS        -                 -               -                    -                   -
inhibitor




long-acting beta2      small molecule   -               -                    -                   -
agonist
Monoclonal antibody antibodies          -               -                    -                   -
with undisclosed
mechanism of action
Glucocorticoid agonist -                -               -                    -                   -
Novel glucocorticoid   -               -   -   -   -
agonist


Human anti-            antibodies      -   -   -   -
CCL2/MCP-1
monoclonal antibody
-                      -               -   -   -   -


Oral prostaglandin D2 small molecule   -   -   -   -
(PGD2) receptor
antagonist (CRTH2)
-                     small molecule   -   -   -   -
·Corticosteroid:       ·small molecule:   -   -   ·434.498: flunisolide   ·Practically Insoluble:
flunisolide            flunisolide                                        flunisolide




It is an immunoglobulin antibodies        -   -   -                       -
antibody

-                      -                  -   -   -                       -
V-Protectants® are       small molecule   -                     -   -   -
drugs that block a
class of signals, called
oxidant signals, which
are generated within
endothelial cells.
These oxidant signals
activate genes, which
produce inflammatory
proteins. The protein
products of these
selected genes,
including VCAM-1,
attract white blood
cells to the site of
chronic inflammation.



-                      -                  80% of microparticles -   -   -
                                          delivery to lung.
                                          Microparticles
                                          remained in the lung
                                          for up to 24 hours and
                                          the drug was released
                                          over a 12 to 24-hour
                                          period. Resperible
                                          fraction >25%.
                                          (Source: company
                                          website)
·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate




-                         -                   -   -   -                    -

Second-generation      oligonucleotide        -   -   -                    -
antisense inhibitor of
the alpha subunit of
the interleukin 4
receptor, IL4R-alpha.
Potently reduces IL4R-
alpha: mRNA and
protein levels
LAB CGRP is a 37        peptide   -   -   -   -
amino acid natural
neuropeptide
produced in the lung in
response to allergic
stimuli. As a potential
drug, it has
demonstrated in
preclinical studies a
profile that could make
it an ideal anti-
asthmatic drug
candidate with
bronchodilator,
bronchoprotector and
anti-inflammatory
properties.
·Pemirolast binds to    ·small molecule:       -   -   ·266: pemirolast   ·Freely Soluble:
the histamine H1        pemirolast potassium           potassium          pemirolast potassium
receptor. This blocks
the action of
endogenous
histamine, which
subsequently leads to
temporary relief of the
negative symptoms
brought on by
histamine. Pemirolast
has also been
observed to block
antigen-stimulated
calcium ion influx into
mast cells. Pemirolast
inhibits the chemotaxis
of eosinophils into
ocular tissue, and
prevents inflammatory
mediator release from
human eosinophils.:
pemirolast potassium
·Pemirolast binds to    ·small molecule:       -   -   ·266: pemirolast   ·Freely Soluble:
the histamine H1        pemirolast potassium           potassium          pemirolast potassium
receptor. This blocks
the action of
endogenous
histamine, which
subsequently leads to
temporary relief of the
negative symptoms
brought on by
histamine. Pemirolast
has also been
observed to block
antigen-stimulated
calcium ion influx into
mast cells. Pemirolast
inhibits the chemotaxis
of eosinophils into
ocular tissue, and
prevents inflammatory
mediator release from
human eosinophils.:
pemirolast potassium




-                      vaccine                 -   -   -                  -
5-lipoxygenase-         small molecule   -   -   -   -
activating protein
(FLAP) inhibitor




Selective antagonist of -                -   -   -   -
the receptor DP2 (also
known as CRTH2 or
chemoattractant
receptor-homologous
molecule expressed
on Th2 lymphocytes)

-                       small molecule   -   -   -   -

A monoclonal antibody antibodies         -   -   -   -
that blocks the actions
of interleukin-4 (IL-4)
and interleukin-13 (IL-
13), cytokines that are
believed to play a role
in asthma.

antagonist of the       -                -   -   -   -
receptors of
prostaglandin D2 (D-
prostanoid and
chemoattractant
receptor-homologous
molecule expressed
on Th2 cells)
Antagonist against the   small molecule         -   -   -                 -
receptor CRTH2
·Tryptase inhibitor:     ·small molecule: APC   -   -   ·440.5: APC 366   ·: APC 366
APC 366                  366
Beta 2 Adrenergic        small molecule         -   -   -                 -
agonist ,
Corticosteroids




-                        -                      -   -   -                 -

It is a second-          oligonucleotide        -   -   -                 -
generation antisense
inhibitor of VLA-4

Selective A2B            small molecule         -   -   -                 -
adenosine receptor
antagonists
Selective A2B            small molecule         -   -   -                 -
adenosine receptor
antagonists
Inhibition of cytokine   -                      -   -   -                 -
production
-                        -                      -   -   -                 -


TLR-9 agonist            small molecule         -   -   -                 -
Coley’s TLR       oligonucleotide   -   -   -   -
Therapeutic
compounds for
respiratory diseases
stimulate TLR9 and
initiate an immune
system cascade that
mimics the effects of
an infection, thereby
switching the immune
system away from the
Th2 state. Once the
immune system has
switched away from
the Th2 state, an
inappropriate allergic
reaction will no longer
occur in response to
that stimulus


Tryptase ß inhibitor    small molecule    -   -   -   -
The compound            small molecule    -   -   -   -
selectively inhibits or
prevents the
production of
immunoglobulin
epsilon (IgE)
antibodies. It has also
demonstrated an
ability to suppress the
antigen-stimulated IL-4
and IL-5 responses
with potencies similar
to those observed for
IgE suppression.
Double-stranded so-       oligonucleotide   -   -   -                   -
called decoy
oligodeoxynucleotides
(decoy ODNs) target
transcription factors,
each of which bear
one or more DNA
binding domains that
attach themselves to
DNA in a sequence-
specific manner.
Decoy ODNs mimic
these sequences and
remove the
corresponding
transcription factors
from further
interactions, effectively
neutralizing such
factors




·PDE4 inhibitor : AWD ·small molecule: AWD -    -   ·458.275: AWD 12-281 ·: AWD 12-281
12-281                12-281

Second-generation        -                  -   -   -                   -
TLR-9 agonists
-                        -                  -   -   -                   -
CRTh2 receptor       small molecule     -   -   -   -
antagonist (2008
company report, page
5)




-                      small molecule   -   -   -   -

-                      small molecule   -   -   -   -

iLABA(2008 company small molecule       -   -   -   -
report, page 6)

Chemokine receptor     small molecule   -   -   -   -
antagonist
-                      small molecule   -   -   -   -
CRTh2                  -                -   -   -   -
antagonist(2008
company report, page
6)
CRTh2 antagonist       -                -   -   -   -

-                      -                -   -   -   -




-                      -                -   -   -   -
AZX100 is a 24-amino peptide                   -   -   -                  -
acid peptide that has
the ability to relax
smooth muscle in
multiple tissue types.

·Triazolam is a short- ·small molecule:        -   -   ·343.21:           ·Practically Insoluble:
acting benzodiazepine triazolam·small                  triazolam·389.4:   triazolam·: reproterol
with general properties molecule: reproterol           reproterol
similar to those of
diazepam. It is used as
a hypnotic in the short-
term management of
insomnia.: triazolam·A
direct-acting
sympathomimetic with
predominantly beta-
adrenergic activity and
a selective action on
beta(2) receptors (a
beta(2) agonist). :
reproterol




Asthma Protein        antibodies               -   -   -                  -
Neutralizing Nanobody
·A synthetic, selective   ·small molecule:   ACCOLATE is rapidly -       ·575.683: zafirlukast   ·Practically Insoluble:
peptide leukotriene       zafirlukast        absorbed orally. It                                 zafirlukast
receptor antagonist                          undergoes extensive
(LTRA): zafirlukast                          hepatic metabolism.
                                             Administration of
                                             zafirlukast with food
                                             reduced the mean
                                             bioavailability by
                                             approximately 40%.
                                             Hydroxylated
                                             metabolites of
                                             zafirlukast excreted in
                                             the feces are formed
                                             through the
                                             cytochrome P450 2C9
                                             (CYP2C9) pathway.
                                             Additional in vitro
                                             studies utilizing human
                                             liver microsomes show
                                             that zafirlukast inhibits
                                             the cytochrome P450,
                                             CYP3A4 and CYP2C9
                                             isoenzymes at
                                             concentrations close to
                                             the clinically achieved
                                             total plasma
                                             concentrations. More
                                             than 99% bound to
                                             plasma proteins. Vd is
                                             70 L, t1/2 is 10 h and
                                             oral CL is 20 L/h.
·Albuterol sulfate, the   ·small molecule:    Following a 3 mg dose -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   of nebulized albuterol    sulfate              albuterol sulfate
albuterol and a                               in adults, the mean
relatively selective                          maximum albuterol
beta 2 -adrenergic                            plasma level at 0.5
bronchodilator:                               hours was 2.1 ng/mL
albuterol sulfate                             (range, 1.4 to 3.2
                                              ng/mL). Most of the
                                              absorbed dose was
                                              recovered in urine
                                              collected during the 24
                                              hours after drug
                                              administration.
                                              Following oral
                                              administration of 4 mg
                                              albuterol, t1/2 was 5-6
                                              h.

·Albuterol sulfate, the   ·small molecule:    -                     -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate                             sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate
Antagonist of 7-        small molecule       -   -   -                      -
transmembrane G-
protein coupled
receptors on
leukocytes,
eosinophils, basophils,
mast cells and
lymphocytes
·Corticosteroid with      ·small molecule:   -   -   ·500.57: fluticasone   ·Practically Insoluble:
mainly glucocorticoid fluticasone propionate         propionate             fluticasone propionate
activity. It has weak
affinity for the
progesterone receptor,
and virtually no affinity
for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
propionate
·Corticosteroid with        ·small molecule:       flutacasone: BA is     -   ·500.57: fluticasone   ·Practically Insoluble:
mainly glucocorticoid       fluticasone            18%. First pass liver      propionate·603.7:      fluticasone
activity. It has weak       propionate·small       metabolosim. Low           salmeterol xinafoate   propionate·Sparingly
affinity for the            molecule: salmeterol   concentration in                                  Soluble: salmeterol
progesterone receptor,      xinafoate              plasma. t1/2 is 5.33-                             xinafoate
and virtually no affinity                          7.65 h.
for the                                            salmeterol: Tmax is 20
mineralocorticoid,                                 min with detectable
estrogen, or androgen                              levels within 5 min.
receptors.: fluticasone                            Low concentration in
propionate·A long-                                 plasma.
acting beta 2 -
adrenergic agonist:
salmeterol xinafoate
·Corticosteroid with        ·small molecule:       Peak plasma            -   ·500.57: fluticasone   ·Practically Insoluble:
mainly glucocorticoid       fluticasone            concentrations of          propionate·603.7:      fluticasone
activity. It has weak       propionate·small       fluticasone propionate     salmeterol xinafoate   propionate·Sparingly
affinity for the            molecule: salmeterol   were achieved in 0.33                             Soluble: salmeterol
progesterone receptor,      xinafoate              to 1.5 hours and those                            xinafoate
and virtually no affinity                          of salmeterol were
for the                                            achieved in 5 to 10
mineralocorticoid,                                 minutes. Absolute
estrogen, or androgen                              bioavailability of
receptors.: fluticasone                            fluticasone propionate
propionate·A long-                                 from ADVAIR HFA in
acting beta 2 -                                    15 healthy subjects
adrenergic agonist:                                was 5.3%. Terminal
salmeterol xinafoate                               half-life estimates of
                                                   fluticasone propionate
                                                   for ADVAIR HFA,
                                                   ADVAIR DISKUS, and
                                                   fluticasone propionate
                                                   CFC inhalation aerosol
                                                   were similar and
                                                   averaged 5.9 hours.
                                                   No terminal half-life
                                                   estimates were
                                                   calculated for
                                                   salmeterol.
·The drug possesses ·small molecule:        -   -   ·433.96:             ·Freely Soluble:
antimalarial actions   hydroxychloroquine           hydroxychloroquine   hydroxychloroquine
and also exerts a      sulfate                      sulfate              sulfate
beneficial effect in
lupus erythematosus
(chronic discoid or
systemic) and acute or
chronic rheumatoid
arthritis. The precise
mechanism of action is
not known.:
hydroxychloroquine
sulfate




a fusion protein that  protein              -   -   -                    -
combines Secretory
Leukocyte Protease
Inhibitor (SLPI) and
rAAT. It inhibits
neutrophil elastase,
chymase, cathepsin G
and kallikrein through
the rAAT portion and
inhibits neutrophil
elastase and tryptase
through SLPI.
·Non-glycosylated 14 ·protein: pitrakinra   -   -   ·: pitrakinra   ·: pitrakinra
kDa IL-4 variant that
binds tightly to IL4Ra
receptor subunit. Two
amino acid
substitutions repel IL-
2Rg receptor subunit.
It is a potent inhibitor
of both the IL-4 and IL-
13 receptors.:
pitrakinra
·Corticosteroid:   ·small molecule:   Total systemic BA is   -   ·434.498: flunisolide   ·Practically Insoluble:
flunisolide        flunisolide        40%. t1/2 is 1.8 h.                                flunisolide
·Beta agonist: albuterol ·small molecule:   Aerodise salbutamol      -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          was studied in a single-                           albuterol
                                            centre, investigator-
                                            blinded, randomized,
                                            three-way crossover
                                            design. the trial
                                            enrolled twenty-four
                                            patients (non-smokers
                                            of which 10 were
                                            males) with at least a
                                            12 month history of
                                            moderate to severe
                                            persistent asthma.
                                            The Aerodose®
                                            Inhaler was
                                            approximately five
                                            times as efficient as
                                            the Pari LC Plus and
                                            Evohaler in relative
                                            lung delivery of
                                            salbutamol in
                                            moderate to severe
                                            asthmatics. REF-1
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·Ipratropium bromide is ·small molecule:      -   -   ·412.38: ipratropium   ·: ipratropium bromide
an anticholinergic      ipratropium bromide           bromide anhydrous      anhydrous
(parasympatholytic)     anhydrous
agent which, based on
animal studies,
appears to inhibit
vagally mediated
reflexes by
antagonizing the action
of acetylcholine, the
transmitter agent
released from the
vagus nerve.
Anticholinergics
prevent the increases
in intracellular
concentration of cyclic
guanosine
monophosphate (cyclic
GMP) which are
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
anhydrous



-                      -                      -   -   -                      -
·Theophylline has two ·small molecule:      -                        -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline                                                             theophylline
airways of patients
with reversible
obstruction; smooth
muscle relaxation (i.e.,
bronchodilation) and
suppression of the
response of the
airways to stimuli

: theophylline




·Beta agonist: albuterol ·small molecule:   Readily absorbed         -   ·239.213: albuterol     ·Sparingly Soluble:
                         albuterol          orally with Cmax                                     albuterol
                                            reached in 0.17 h.;
                                            undergoes first-pass
                                            metabolism in the liver;
                                            the main metabolite:
                                            an inactive sulfate
                                            conjugate; excreted
                                            unchanged in the urine
                                            (28%) and some in the
                                            faeces; t1/2: 4 to 6
                                            hours.
·Beta agonist: albuterol ·small molecule:   Albuterol (WHO             -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          designation is                                       albuterol
                                            salbutamol) is readily
                                            absorbed from the
                                            gastrointestinal tract. It
                                            is subject to first-pass
                                            metabolism in the liver
                                            and possibly in the gut
                                            wall; the main
                                            metabolite is an
                                            inactive sulfate
                                            conjugate.
                                            Approximately 72% of
                                            the inhaled dose is
                                            excreted within 24
                                            hours in the urine, and
                                            consists of 28% as
                                            unchanged drug and
                                            44% as metabolite.;
                                            there is some
                                            excretion in the
                                            faeces.
                                            Albuterol/Salbutamol
                                            does not appear to be
                                            metabolised in the
                                            lung, therefore its
                                            ultimate metabolism
                                            and excretion following
                                            inhalation depends
                                            upon the delivery
                                            method used, which
                                            determines the
                                            proportion of inhaled
                                            salbutamol relative to
·Albuterol sulfate, the   ·small molecule:    Because of its gradual -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   absorption from the        sulfate              albuterol sulfate
albuterol and a                               bronchi, systemic
relatively selective                          levels of albuterol
beta 2 -adrenergic                            inhalation aerosol are
bronchodilator:                               low after inhalation of
albuterol sulfate                             recommended doses.
                                              Tmax is 2 - 4 hrs. The
                                              urinary excretion
                                              provided data
                                              indicated that albuterol
                                              has an elimination half-
                                              life of 3.8 hours.
                                              Approximately 72% of
                                              the inhaled dose is
                                              excreted within 24
                                              hours in the urine, and
                                              consists of 28% as
                                              unchanged drug and
                                              44% as metabolite.
·Beta agonist: albuterol ·small molecule:   Albuterol (WHO             -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          designation is                                       albuterol
                                            salbutamol) is readily
                                            absorbed from the
                                            gastrointestinal tract. It
                                            is subject to first-pass
                                            metabolism in the liver
                                            and possibly in the gut
                                            wall; the main
                                            metabolite is an
                                            inactive sulfate
                                            conjugate.
                                            Approximately 72% of
                                            the inhaled dose is
                                            excreted within 24
                                            hours in the urine, and
                                            consists of 28% as
                                            unchanged drug and
                                            44% as metabolite.;
                                            there is some
                                            excretion in the
                                            faeces.
                                            Albuterol/Salbutamol
                                            does not appear to be
                                            metabolised in the
                                            lung, therefore its
                                            ultimate metabolism
                                            and excretion following
                                            inhalation depends
                                            upon the delivery
                                            method used, which
                                            determines the
                                            proportion of inhaled
                                            salbutamol relative to
·Beta agonist: albuterol ·small molecule:   Albuterol (WHO             -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          designation is                                       albuterol
                                            salbutamol) is readily
                                            absorbed from the
                                            gastrointestinal tract. It
                                            is subject to first-pass
                                            metabolism in the liver
                                            and possibly in the gut
                                            wall; the main
                                            metabolite is an
                                            inactive sulfate
                                            conjugate.
                                            Approximately 72% of
                                            the inhaled dose is
                                            excreted within 24
                                            hours in the urine, and
                                            consists of 28% as
                                            unchanged drug and
                                            44% as metabolite.;
                                            there is some
                                            excretion in the
                                            faeces.
                                            Albuterol/Salbutamol
                                            does not appear to be
                                            metabolised in the
                                            lung, therefore its
                                            ultimate metabolism
                                            and excretion following
                                            inhalation depends
                                            upon the delivery
                                            method used, which
                                            determines the
                                            proportion of inhaled
                                            salbutamol relative to
·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate




·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate
·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate
·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol    ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate               albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate




Albuterol analog with     small molecule      -   -   -                     -
no systemic analog
·Direct H1-receptor       ·small molecule:    -   -   ·285.77: epinastine   ·Soluble: epinastine
antagonist : epinastine   epinastine                  hydrochloride         hydrochloride
hydrochloride             hydrochloride



·C5 complement          ·antibodies:          -   -   ·148000: eculizumab   ·: eculizumab
inhibitor that prevents eculizumab
the cleavage of human
complement
component C5 into its
pro-inflammatory
components:
eculizumab
·C5 complement          ·antibodies:          -   -   ·148000: eculizumab   ·: eculizumab
inhibitor that prevents eculizumab
the cleavage of human
complement
component C5 into its
pro-inflammatory
components:
eculizumab
·An antihistamine with ·small molecule:   ALLEGRA is rapidly      -   ·538.13: fexofenadine   ·Slightly Soluble:
selective peripheral H fexofenadine       absorbed into the body      hydrochloride           fexofenadine
1 -receptor antagonist hydrochloride      following oral                                      hydrochloride
activity: fexofenadine                    administration, with
hydrochloride                             Tmax at approximately
                                          1-3 hours post dose.
                                          The single and
                                          multiple dose
                                          pharmacokinetics of
                                          fexofenadine are linear
                                          for oral doses up to
                                          120mg BID.Plasma
                                          protein binding is 60-
                                          70%. Fexofenadine
                                          undergoes negligible
                                          metabolism (hepatic or
                                          non-hepatic), as it was
                                          the only major
                                          compound identified in
                                          urine and faeces of
                                          animals and man. The
                                          plasma concentration
                                          profiles of
                                          fexofenadine follow a
                                          bi-exponential decline
                                          with t1/2 of 11-15 h.
the inhibition of a     peptide                   -   -   -                     -
specific signal
transduction pathways
in mast cells by unique
cell-permeable
molecules.

·Although its precise      ·small molecule:       -   -   ·512.333: sodium      ·Soluble: sodium
mode of action             sodium                         cromoglycate·389.4:   cromoglycate·:
remains uncertain,         cromoglycate·small             reproterol            reproterol
sodium cromoglycate        molecule: reproterol
is believed to act
primarily by preventing
release of mediators of
inflammation from
sensitised mast cells
through stabilisation of
mast-cell membranes.
: sodium
cromoglycate·A direct-
acting
sympathomimetic with
predominantly beta-
adrenergic activity and
a selective action on
beta(2) receptors (a
beta(2) agonist). :
reproterol
·Although its precise      ·small molecule:       -   -   ·512.333: sodium      ·Soluble: sodium
mode of action             sodium                         cromoglycate·389.4:   cromoglycate·:
remains uncertain,         cromoglycate·small             reproterol            reproterol
sodium cromoglycate        molecule: reproterol
is believed to act
primarily by preventing
release of mediators of
inflammation from
sensitised mast cells
through stabilisation of
mast-cell membranes.
: sodium
cromoglycate·A direct-
acting
sympathomimetic with
predominantly beta-
adrenergic activity and
a selective action on
beta(2) receptors (a
beta(2) agonist). :
reproterol




-                          small molecule         -   -   -                     -
Alpha-1 antitrypsin-    ·protein: alpha1-       -   -   ·44324.5: alpha1-       ·: alpha1-proteinase
membrane                proteinase inhibitor,           proteinase inhibitor,   inhibitor, human
translocation signal    human                           human
(MTS) recombinant
fusion
protein.···Elastase
inhibitor: alpha1-
proteinase inhibitor,
human
·In vitro studies and in ·small molecule:   3% of dose delivered -      ·520.59:         ·Freely Soluble:
vivo pharmacologic       metaproterenol     intact to lungs with        metaproterenol   metaproterenol
studies have             sulphate           duration of effect 1.5 to   sulphate         sulphate
demonstrated that                           2 hrs. The major
metaproterenol sulfate                      metabolite,
has a preferential                          metaproterenol-3-0-
effect on beta-2                            sulfate, is produced in
adrenergic receptors                        the
compared with                               gastrointestinal tract.
isoproterenol. The                          Alupent is not
pharmacologic effects                       metabolized by
of beta adrenergic                          catechol-0-
agonist drugs are at                        methyltransferase nor
least in part                               have glucuronide
attributable to                             conjugates been
stimulation through                         isolated to date.
beta
adrenergic receptors
of intracellular adenyl
cyclase, the enzyme
which
catalyzes the
conversion of
adenosine
triphosphate (ATP) to
cyclic-3',5'-
adenosine
monophosphate (c-
AMP). Increased c-
AMP levels are
associated with
relaxation of bronchial
smooth muscle and
inhibition of
·In vitro studies and in ·small molecule:   Absorption,              -   ·520.59:         ·Freely Soluble:
vivo pharmacologic       metaproterenol     biotransformation and        metaproterenol   metaproterenol
studies have             sulphate           excretion studies            sulphate         sulphate
demonstrated that                           following
metaproterenol sulfate                      administration by
has a preferential                          inhalation have not
effect on beta-2                            been performed.
adrenergic receptors                        Following oral
compared with                               administration of tablet
isoproterenol. The                          and solution, an
pharmacologic effects                       average of 40% of the
of beta adrenergic                          drug was excreted as
agonist drugs are at                        the unchanged drug
least in part                               and its major
attributable to                             metabolite, a polar
stimulation through                         conjugate,
beta                                        metaproterenol-O-
adrenergic receptors                        sulfate.
of intracellular adenyl
cyclase, the enzyme
which
catalyzes the
conversion of
adenosine
triphosphate (ATP) to
cyclic-3',5'-
adenosine
monophosphate (c-
AMP). Increased c-
AMP levels are
associated with
relaxation of bronchial
smooth muscle and
inhibition of
·In vitro studies and in ·small molecule:   -   -   ·520.59:         ·Freely Soluble:
vivo pharmacologic       metaproterenol             metaproterenol   metaproterenol
studies have             sulphate                   sulphate         sulphate
demonstrated that
metaproterenol sulfate
has a preferential
effect on beta-2
adrenergic receptors
compared with
isoproterenol. The
pharmacologic effects
of beta adrenergic
agonist drugs are at
least in part
attributable to
stimulation through
beta
adrenergic receptors
of intracellular adenyl
cyclase, the enzyme
which
catalyzes the
conversion of
adenosine
triphosphate (ATP) to
cyclic-3',5'-
adenosine
monophosphate (c-
AMP). Increased c-
AMP levels are
associated with
relaxation of bronchial
smooth muscle and
inhibition of
·In vitro studies and in ·small molecule:   -   -   ·520.59:         ·Freely Soluble:
vivo pharmacologic       metaproterenol             metaproterenol   metaproterenol
studies have             sulphate                   sulphate         sulphate
demonstrated that
metaproterenol sulfate
has a preferential
effect on beta-2
adrenergic receptors
compared with
isoproterenol. The
pharmacologic effects
of beta adrenergic
agonist drugs are at
least in part
attributable to
stimulation through
beta
adrenergic receptors
of intracellular adenyl
cyclase, the enzyme
which
catalyzes the
conversion of
adenosine
triphosphate (ATP) to
cyclic-3',5'-
adenosine
monophosphate (c-
AMP). Increased c-
AMP levels are
associated with
relaxation of bronchial
smooth muscle and
inhibition of
·In vitro studies and in ·small molecule:   -   -   ·520.59:         ·Freely Soluble:
vivo pharmacologic       metaproterenol             metaproterenol   metaproterenol
studies have             sulphate                   sulphate         sulphate
demonstrated that
metaproterenol sulfate
has a preferential
effect on beta-2
adrenergic receptors
compared with
isoproterenol. The
pharmacologic effects
of beta adrenergic
agonist drugs are at
least in part
attributable to
stimulation through
beta
adrenergic receptors
of intracellular adenyl
cyclase, the enzyme
which
catalyzes the
conversion of
adenosine
triphosphate (ATP) to
cyclic-3',5'-
adenosine
monophosphate (c-
AMP). Increased c-
AMP levels are
associated with
relaxation of bronchial
smooth muscle and
inhibition of
·New generation         ·small molecule:      The oral BA of both    -   ·540.69: ciclesonide   ·Practically Insoluble:
inhaled corticosteroid ciclesonide            ciclesonide and the                               ciclesonide
with novel                                    active metabolite is
pharmacokinetic                               negligible (
properties: ciclesonide




·New generation        ·small molecule:       -                      -   ·540.69:               ·Practically Insoluble:
inhaled corticosteroid ciclesonide·small                                 ciclesonide·344.405:   ciclesonide·Slightly
with novel             molecule: formoterol                              formoterol             Soluble: formoterol
pharmacokinetic
properties:
ciclesonide·Selective
long-acting (12 hours)
ß2-adrenergic
stimulant
(bronchodilator):
formoterol
-                      antibodies             -                      -   -                      -

·Mucolytic agent:      ·small molecule:       -                      -   ·414.6: ambroxol       ·Sparingly Soluble:
ambroxol               ambroxol                                          hydrochloride          ambroxol
hydrochloride          hydrochloride                                                            hydrochloride
·Airway specific anti- ·small molecule:   Andolast was           -   ·333.314: andolast   ·: andolast
inflammatory agent,    andolast           absorbed after
belonging to a new                        inhalation and was
class of calcium-                         available to the
activated potassium                       systemic circulation.
(K+) channel openers.                     Cmax values were 6.3,
The compound is also                      10.9 and 30.5 ng ml(-
able to reduce the                        1) at the three doses,
expression of IgE                         respectively, and
triggered by specific                     occurred at 30, 52.5
cytokines in                              and 30 min (median
lymphocytes taken                         t(max)). The mean
from asthmatic                            AUC(t) values were
patients.: andolast                       1852, 2889 and 7677
                                          ng min ml(-1). CL:
                                          1141-1168 ml/min. Vd:
                                          430-486 L. t1/2: 4.5-5
                                          h. (REF 1- (Pubmed
                                          id:11745909))


Anti-Chitinase            antibodies      -                      -   -                    -
monoclonal antibody

humanized                 -               -                      -   -                    -
monoclonal antibody
that binds specifically
to IL-13
-                         antibodies      -                      -   -                    -
Aridol is a patented   ·small molecule:   -   -   ·182.17: mannitol   ·Freely Soluble:
biomarker for airway   mannitol                                       mannitol
inflammation···Osmotic
diuretic: mannitol
R(+) Isomer of        ·small molecule:   -   -   ·236.294: zileuton   ·Practically Insoluble:
Zileuton···Active     zileuton                                        zileuton
inhibitor of 5-
lipoxygenase, the
enzyme that catalyzes
the formation of
leukotrienes from
arachidonic acid.:
zileuton
·Corticosteroid with    ·small molecule:   Absorption from the       -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone     gastrointestinal tract is     beclomethasone   beclomethasone
activity:               dipropionate       slow and bioavailability      dipropionate     dipropionate
beclomethasone                             is low, suggesting that
dipropionate                               most of the absorbed
                                           drug is metabolised
                                           during its first passage
                                           through the liver. Since
                                           the dose of oral
                                           beclometasone
                                           dipropionate needed to
                                           suppress plasma
                                           cortisol is greater than
                                           that required by
                                           inhalation, this
                                           suggests that the
                                           portion absorbed from
                                           the lungs is mainly
                                           responsible for any
                                           systemic effects.


-                       -                  -                         -   -                -
·The precise            ·small molecule:     Cmax at steady state -     ·521.429: mometasone ·Practically Insoluble:
mechanism of            mometasone furoate   is 94 - 114 pcg/mL and     furoate              mometasone furoate
corticosteroid action                        the mean time to peak
on allergic rhinitis is                      levels ranged from
not known.                                   approximately 1.0 to
Corticosteroids have                         2.5 hours.
been shown to have a                         Mometasone furoate is
wide range of effects                        primarily and
on multiple cell types                       extensively
(e.g., mast cells,                           metabolized in the liver
eosinophils,                                 of all species
neutrophils,                                 investigated and
macrophages, and                             undergoes extensive
lymphocytes) and                             metabolism to multiple
mediators (e.g.,                             metabolites. In-vitro
histamine,                                   studies have
eicosanoids,                                 confirmed the primary
leukotrienes, and                            role of CYP 3A4 in the
cytokines) involved in                       metabolism of this
inflammation.                                compound. The in vitro
: mometasone furoate                         protein binding for
                                             mometasone furoate
                                             was reported to be 98 -
                                             99% (in a
                                             concentration range of
                                             5 to 500 ng/ml). The
                                             mean terminal t1/2is 5
                                             h and the mean steady-
                                             state Vd is 152 L.
·Beta agonist: albuterol ·small molecule:   10% delivered to         -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          airway. Readily                                    albuterol
                                            absorbed from GI tract
                                            but undergoes
                                            extensive first pass
                                            metabolism. CL is
                                            30L/hr. t1/2 is 3-7 hrs.
-                       small molecule   -   -   -   -




Inhaled NCE steroid     small molecule   -   -   -   -

-                       -                -   -   -   -




serotonin receptors     -                -   -   -   -

ß-Tryptase inhibitors   small molecule   -   -   -   -

-                       vaccine          -   -   -   -
CRTH2 receptor         -   -   -   -   -
(chemoattractant
receptor expressed on
T Helper type 2 cells)
antagonist
·: proxyphylline·alpha     ·small molecule:      -   -   ·238.25:                 ·Very Soluble:
and beta adrenergenic      proxyphylline·small           proxyphylline·201.695:   proxyphylline·Freely
agonist : ephedrine        molecule: ephedrine           ephedrine                Soluble: ephedrine
hydrochloride·Phenoba      hydrochloride·small           hydrochloride·232:       hydrochloride·Very
rbital, the longest-       molecule:                     phenobarbital            Slightly Soluble:
acting barbiturate, acts   phenobarbital                                          phenobarbital
on GABAA receptors,
increasing synaptic
inhibition. This has the
effect of elevating
seizure threshold and
reducing the spread of
seizure activity from a
seizure focus.
Phenobarbital may
also inhibit calcium
channels, resulting in a
decrease in excitatory
transmitter release.
The sedative-hypnotic
effects of
phenobarbital are likely
the result of its effect
on the polysynaptic
midbrain reticular
formation, which
controls CNS
arousal.
: phenobarbital
·A beta-2 agonist:   ·small molecule:   -   -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol                 hydrochloride         hydrochloride
hydrochloride        hydrochloride
·A beta-2 agonist:   ·small molecule:   -   -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol                 hydrochloride         hydrochloride
hydrochloride        hydrochloride
·Ipratropium bromide is ·small molecule:      -   -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic      ipratropium bromide           bromide hydrate        ipratropium bromide
(parasympatholytic)     hydrate                                              hydrate
agent which, based on
animal studies,
appears to inhibit
vagally mediated
reflexes by
antagonizing the action
of acetylcholine, the
transmitter agent
released from the
vagus nerve.
Anticholinergics
prevent the increases
in intracellular
concentration of cyclic
guanosine
monophosphate (cyclic
GMP) which are
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate
·Ipratropium bromide is ·small molecule:      Site specific action.  -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic      ipratropium bromide   Drug is not readily        bromide hydrate        ipratropium bromide
(parasympatholytic)     hydrate               absorbed systemically.                            hydrate
agent which, based on                         t1/2 is about 2 hrs.
animal studies,                               Ipratropium bromide is
appears to inhibit                            minimally bound (0 to
vagally mediated                              9% in vitro) to plasma
reflexes by                                   albumin and
antagonizing the action                       1-acid
of acetylcholine, the                         glycoprotein.
transmitter agent
released from the
vagus nerve.
Anticholinergics
prevent the increases
in intracellular
concentration of cyclic
guanosine
monophosphate (cyclic
GMP) which are
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate
·Ipratropium bromide is ·small molecule:      Following nebulization -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic      ipratropium bromide   of a 2 mg dose, a          bromide hydrate        ipratropium bromide
(parasympatholytic)     hydrate               mean 7% of the dose                               hydrate
agent which, based on                         was absorbed into the
animal studies,                               systemic circulation
appears to inhibit                            either from the surface
vagally mediated                              of the lung or from the
reflexes by                                   gastrointestinal tract.
antagonizing the action                       t1/2 is 1.6 h (IV). The
of acetylcholine, the                         volume of distribution
transmitter agent                             (Vβ) is 338 L (
released from the                             4.6 L/kg). The mean
vagus nerve.                                  total clearance of the
Anticholinergics                              drug is determined to
prevent the increases                         be 2.3 L/min. Minimally
in intracellular                              (0 to 9% in vitro)
concentration of cyclic                       bound to plasma
guanosine                                     albumin and a1-acid
monophosphate (cyclic                         glycoproteins. It is
GMP) which are                                partially metabolized.
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate
Avimer compound that protein               -   -   -                       -
inhibits IgE. Avimers
originate from the
recombination of
families of human
serum proteins. They
are single protein
chains composed of
modular binding
domains


-                       oligonucleotide    -   -   -                       -


-                       small molecule     -   -   -                       -

·Corticosteroid with    ·small molecule:   -   -   ·434.5: triamcinolone   ·Practically Insoluble:
mainly glucocorticoid   triamcinolone              acetonide               triamcinolone
activity, anti-         acetonide                                          acetonide
inflammatory.:
triamcinolone
acetonide
·Corticosteroid with    ·small molecule:   Based upon             -   ·434.5: triamcinolone   ·Practically Insoluble:
mainly glucocorticoid   triamcinolone      intravenous dosing of      acetonide               triamcinolone
activity, anti-         acetonide          triamcinolone                                      acetonide
inflammatory.:                             acetonide phosphate
triamcinolone                              ester, t1/2 of
acetonide                                  triamcinolone
                                           acetonide is 88 min,
                                           Vd is 1.42 L/kg (SD ±
                                           0.39) and CL is 0.65
                                           L/h/kg (SD ± 0.13).
                                           The overall mean
                                           percent fraction bound
                                           was approximately
                                           68%. The metabolism
                                           and excretion of
                                           triamcinolone
                                           acetonide were both
                                           rapid and extensive.
·Corticosteroid with    ·small molecule:   Systemic absorption of -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone     unchanged                  beclomethasone   beclomethasone
activity:               dipropionate       beclometasone              dipropionate     dipropionate
beclomethasone                             dipropionate (BDP)
dipropionate                               occurs through the
                                           lungs. There is
                                           negligible oral
                                           absorption of the
                                           swallowed dose of
                                           unchanged BDP.When
                                           administered orally the
                                           bioavailability of BDP
                                           is negligible but pre-
                                           systemic conversion to
                                           B-17-MP results in
                                           41% of the dose being
                                           absorbed as B-17-
                                           MP.The tissue
                                           distribution at steady-
                                           state for BDP is
                                           moderate (20 L) but
                                           more extensive for B-
                                           17-MP (424 L).
                                           Plasma protein binding
                                           is moderately high
                                           (87%).BDP is cleared
                                           very rapidly from the
                                           systemic circulation, by
                                           metabolism mediated
                                           via esterase enzymes
                                           that are found in most
                                           tissues. The main
                                           product of metabolism
                                           is the active metabolite
-                        -               -                         -   -   -




-                        antibodies      -                         -   -   -

-                        -               -                         -   -   -




-                        -               -                         -   -   -


Anti-interleukin-5 (IL-5) antibodies     -                         -   -   -
receptor MAb




N-substituted           small molecule   It is orally active (~80% -   -   -
aminocaprolactam.                        bioavailable) and has
BN83470 is a potent                      pharmacokinetics
inhibitor of chemokine-                  optimised for once-a-
induced leukocyte                        day dosing.
migration in vitro
(EC50 = 0.1nM) and
LPS-induced leukocyte
recruitment in vivo
(ED50 = 0.002 mg/kg).
Activation of regulatory antibodies        -                         -   -                      -
T-cells (2008 company
report, page 6)

·An active precursor of ·small molecule:   BA is 10%.                -   ·403.904: bambuterol   ·Freely Soluble:
the selective β2- bambuterol          Bambuterol is                 hydrochloride          bambuterol
adrenergic agonist      hydrochloride      metabolised in the liver                             hydrochloride
terbutaline.:                              and terbutaline is
bambuterol                                 formed by both
hydrochloride                              hydrolysis and
                                           oxidation. After
                                           absorption from the
                                           gut, about 2/3 of
                                           terbutaline is first-pass
                                           metabolised,
                                           bambuterol escapes
                                           this first-pass
                                           metabolism. 40–0% 5
                                           bound to plasma
                                           proteins and t1/2 is
                                            1
                                           9–7 h.

-                       -                  -                         -   -                      -
·Corticosteroid with    ·small molecule:   -                       -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone                                 beclomethasone   beclomethasone
activity:               dipropionate                                   dipropionate     dipropionate
beclomethasone
dipropionate




·Corticosteroid with    ·small molecule:   Readily absorbed in     -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone     pulmonary tract             beclomethasone   beclomethasone
activity:               dipropionate       (specific performance       dipropionate     dipropionate
beclomethasone                             data not available)
dipropionate
·Corticosteroid with    ·small molecule:   Readily absorbed in     -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone     pulmonary tract             beclomethasone   beclomethasone
activity:               dipropionate       (specific performance       dipropionate     dipropionate
beclomethasone                             data not available)
dipropionate




·Corticosteroid with    ·small molecule:   -                       -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone                                 beclomethasone   beclomethasone
activity:               dipropionate                                   dipropionate     dipropionate
beclomethasone
dipropionate
·Corticosteroid with    ·small molecule:   Readily absorbed in     -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone     pulmonary tract             beclomethasone   beclomethasone
activity:               dipropionate       (specific performance       dipropionate     dipropionate
beclomethasone                             data not available)
dipropionate
·The bronchodilating      ·small molecule:        Fenoterol               -   ·384.3: fenoterol      ·Soluble: fenoterol
effect of fenoterol is    fenoterol               hydrobromide:               hydrobromide·430.38:   hydrobromide·Freely
produced primarily by     hydrobromide·small      Incompletely absorbed       ipratropium bromide    Soluble: ipratropium
stimulation of b2-        molecule: ipratropium   from the                    hydrate                bromide hydrate
receptors in the          bromide hydrate         gastrointestinal tract
bronchial smooth                                  and subject to
muscles.: fenoterol                               extensive first-pass
hydrobromide·Ipratropi                            metabolism by sulfate
um bromide is an                                  conjugation. The t1/2
anticholinergic                                   for total excretion is
(parasympatholytic)                               7.2 hours and
agent which, based on                             absorption was
animal studies,                                   calculated to be
appears to inhibit                                60%.
vagally mediated                                  Ipratropium bromide:
reflexes by                                       Poorly absorbed from
antagonizing the action                           the gastro-intestinal
of acetylcholine, the                             tract and slow to cross
transmitter agent                                 mucous membranes
released from the                                 and the blood brain
vagus nerve.                                      barrier. Following
Anticholinergics                                  inhalation, uptake into
prevent the increases                             the plasma is minimal,
in intracellular                                  a peak blood
concentration of cyclic                           concentration is
guanosine                                         attained 1½ to 3 hours
monophosphate (cyclic                             after inhalation (and
GMP) which are                                    similarly for oral
caused by interaction                             administration).
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
·The bronchodilating     ·small molecule:   Rapidly absorbed in GI -   ·384.3: fenoterol   ·Soluble: fenoterol
effect of fenoterol is   fenoterol          tract with an              hydrobromide        hydrobromide
produced primarily by    hydrobromide       absorption level of
stimulation of b2-                          60%. Tmax is 2 h. t1/2
receptors in the                            is 6-7 h.
bronchial smooth
muscles.: fenoterol
hydrobromide




·The bronchodilating     ·small molecule:   Rapidly absorbed in GI -   ·384.3: fenoterol   ·Soluble: fenoterol
effect of fenoterol is   fenoterol          tract. Tmax is 2 h.        hydrobromide        hydrobromide
produced primarily by    hydrobromide       t1/2 is 6-7 h.
stimulation of b2-
receptors in the
bronchial smooth
muscles.: fenoterol
hydrobromide
A potent anti-         gene                -   -   -                       -
inflammatory agent
consisting of the gene
for p20 (transcription
factor inhibitor).

A potent anti-         protein             -   -   -                       -
inflammatory agent
consisting of the gene
for p20 (transcription
factor inhibitor).



·Acts by binding to the ·small molecule:   -   -   ·924.08: amphotericin   ·Practically Insoluble:
sterol component of a amphotericin B               B                       amphotericin B
cell membrane leading
to alterations in cell
permeability and cell
death.: amphotericin B




·anti-IL5 monoclonal  ·antibodies:         -   -   ·: mepolizumab          ·: mepolizumab
antibody: mepolizumab mepolizumab
·Brethine is a beta-     ·small molecule:      Brethine is variably    -      ·548.65: terbutaline   ·Soluble: terbutaline
adrenergic receptor      terbutaline sulfate   absorbed from the              sulfate                sulfate
agonist. In vitro and in                       gastrointestinal tract.
vivo pharmacologic                             Undergoes first-pass
studies have                                   metabolism in the liver
demonstrated that                              and the gut wall. About
terbutaline exerts a                           60% excreted
preferential effect on                         unchanged in the
beta2-adrenergic                               urine. CL is 311 (112)
receptors.: terbutaline                        mL/min and t1/2 is 2.9
sulfate                                        h.



·Brethine is a beta-     ·small molecule:      Brethine is variably       -   ·548.65: terbutaline   ·Soluble: terbutaline
adrenergic receptor      terbutaline sulfate   absorbed from the              sulfate                sulfate
agonist. In vitro and in                       gastrointestinal tract. It
vivo pharmacologic                             undergoes first-pass
studies have                                   metabolism in the liver
demonstrated that                              and the gut wall. About
terbutaline exerts a                           60% excreted
preferential effect on                         unchanged in the
beta2-adrenergic                               urine. CL is 311 (112)
receptors.: terbutaline                        mL/min and t1/2 is 2.9
sulfate                                        h.
·Brethine is a beta-     ·small molecule:      Food reduces              -   ·548.65: terbutaline   ·Soluble: terbutaline
adrenergic receptor      terbutaline sulfate   bioavailability following     sulfate                sulfate
agonist. In vitro and in                       oral dosing (10% on
vivo pharmacologic                             average). Fasting
studies have                                   values of 14-15% have
demonstrated that                              been obtained. Vd is
terbutaline exerts a                           114 L. Total body CL is
preferential effect on                         213 ml/min. Terminal
beta2-adrenergic                               t½ is 16-20 h.
receptors.: terbutaline
sulfate



·Brethine is a beta-     ·small molecule:      Less than 10% of the -        ·548.65: terbutaline   ·Soluble: terbutaline
adrenergic receptor      terbutaline sulfate   dose is absorbed from         sulfate                sulfate
agonist. In vitro and in                       the airways. The
vivo pharmacologic                             remaining 90% is
studies have                                   swallowed but is
demonstrated that                              largely prevented from
terbutaline exerts a                           entering the systemic
preferential effect on                         circulation due to
beta2-adrenergic                               extensive first pass
receptors.: terbutaline                        metabolism.
sulfate



·Thromboxane A2          ·small molecule:      -                         -   ·354.4: seratrodast    ·: seratrodast
receptor antagonist:     seratrodast
seratrodast
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide




·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide




·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide




·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide




·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·Corticosteroid with    ·small molecule:   Budesonide is rapidly -     ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide         and almost completely                             budesonide
activity : budesonide                      absorbed following
                                           administration by
                                           mouth, but has poor
                                           systemic availability
                                           (about 10%) due to
                                           extensive first-pass
                                           metabolism in the liver,
                                           mainly by the
                                           cytochrome P450
                                           isoenzyme CYP3A4.
                                           The major metabolites,
                                           6-β-
                                           hydroxybudesonide
                                           and 16-α-
                                           hydroxyprednisolone
                                           have less than 1% of
                                           the glucocorticoid
                                           activity of unchanged
                                           budesonide.
                                           Budesonide is
                                           reported to have a
                                           terminal t1/2 of about 2-
                                           4 h. (REF 1- (Pubmed
                                           id:11475468), REF 2-
                                           (Pubmed id:15355126)
                                           )
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide




·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·Beta agonist: albuterol ·small molecule:   Salbutamol is readily -      ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          absorbed from the                                  albuterol
                                            gastrointestinal tract. It
                                            is subject to first-pass
                                            metabolism in the liver
                                            and possibly in the gut
                                            wall; the main
                                            metabolite is an
                                            inactive sulfate
                                            conjugate. Salbutamol
                                            is rapidly excreted in
                                            the urine as
                                            metabolites and
                                            unchanged drug; there
                                            is some excretion in
                                            the faeces. Salbutamol
                                            does not appear to be
                                            metabolised in the
                                            lung. The plasma t1/2
                                            is 4 - 6 hrs. (REF 1-
                                            (Pubmed id:5081599),
                                            REF 2- (Pubmed
                                            id:974663), REF 3-
                                            (Pubmed id:17520),
                                            REF 4- (Pubmed
                                            id:3790406), REF 5-
                                            (Pubmed id:2687008),
                                            REF 6- (Pubmed
                                            id:2598971), REF 7-
                                            (Pubmed id:1457264),
                                            REF 8- (Pubmed
                                            id:1635728))
·Beta agonist: albuterol ·small molecule:   -   -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol                                        albuterol




Human anti-IL13         antibodies          -   -   -                     -
monoclonal antibody
·CC-10004 is a           ·small molecule:   -   -   ·460.5: apremilast     ·: apremilast
member of a              apremilast
proprietary pipeline of
novel small molecules
with anti-inflammatory
activities that inhibit
the production of
multiple
proinflammatory
mediators including,
PDE-4, TNF-alpha,
interleukin-2 (IL-2),
interferon-gamma,
leukotrienes, and nitric
oxide synthase. :
apremilast




MAP3K9 inhibitor        small molecule      -   -   -                      -


·Beta-2 agonist:        ·small molecule:    -   -   ·368.431: carmoterol   ·: carmoterol
carmoterol              carmoterol
·Beta-2 agonist:          ·small molecule:     -   -   ·368.431:             ·:
carmoterol·Corticoster carmoterol·small                carmoterol·430.53:    carmoterol·Practically
oid with mainly           molecule: budesonide         budesonide            Insoluble: budesonide
glucocorticoid activity :
budesonide




Smooth muscle           -                      -   -   -                     -
myosin inhibitors

·Mucoactive cysteine    ·small molecule:       -   -   ·179.24: fudosteine   ·Freely Soluble:
derivative acts as an   fudosteine                                           fudosteine
expectorant.:
fudosteine
-                       -                  -   -   -                     -




·PDE4 inhibitor:        ·small molecule:   -   -   ·339.46: tofimilast   ·: tofimilast
tofimilast              tofimilast

·Corticosteroid with    ·small molecule:   -   -   ·392.464:             ·Practically Insoluble:
mainly glucocorticoid   betamethasone              betamethasone         betamethasone
activity :
betamethasone
·Synthetic                ·small molecule:   -   -   ·360.5: prednisolone   ·Very Slightly Soluble:
glucocorticoid with anti- prednisolone                                      prednisolone
inflammatory effects.:
prednisolone




CR 3465 is the           -                   -   -   -                      -
optimised lead of a
new series of
derivatives that are
potent, selective and
orally effective Cys-
leukotriene (Cys-LT1,
formerly LTD4)
receptor antagonists.
CRTH2 receptor        -                      -   -   -                      -
antagonist
Oral prostaglandin D2 -                      -   -   -                      -
(CRTh2) receptor
antagonist
cytokine                  ·small molecule:        -   -   ·360.5:               ·Very Slightly Soluble:
modulator···Synthetic prednisolone·small                  prednisolone·263.4:   prednisolone·:
glucocorticoid with anti- molecule: nortriptyline         nortriptyline         nortriptyline
inflammatory effects.:
prednisolone·Similar to
protriptyline,
nortriptyline is a
tricyclic antidepressant
of the
dibenzocycloheptene
type and is the active
metabolite of
amitriptyline. It is
believed that
nortriptyline either
inhibits the reuptake of
the neurotransmitter
serotonin at the
neuronal membrane or
acts at beta-adrenergic
receptors. Tricyclic
antidepressants do not
inhibit monoamine
oxidase nor do they
affect dopamine
reuptake.: nortriptyline
cytokine                  ·small molecule:        -   -   ·360.5:               ·Very Slightly Soluble:
modulator···Synthetic prednisolone·small                  prednisolone·263.4:   prednisolone·:
glucocorticoid with anti- molecule: nortriptyline         nortriptyline         nortriptyline
inflammatory effects.:
prednisolone·Similar to
protriptyline,
nortriptyline is a
tricyclic antidepressant
of the
dibenzocycloheptene
type and is the active
metabolite of
amitriptyline. It is
believed that
nortriptyline either
inhibits the reuptake of
the neurotransmitter
serotonin at the
neuronal membrane or
acts at beta-adrenergic
receptors. Tricyclic
antidepressants do not
inhibit monoamine
oxidase nor do they
affect dopamine
reuptake.: nortriptyline
·Protein-digesting and ·protein: bromelains   -   -   ·: bromelains   ·: bromelains
milk-clotting enzymes
found in pineapple fruit
juice and stem tissue:
bromelains




Selective A2B-         small molecule         -   -   -               -
adenosine receptor
antagonist
The compound             vaccine   -   -   -   -
consists of the
ImmunodrugTM
candidate QbG10
which is comprised of
the virus-like particle
Qb filled with an
immunostimulatory
DNA sequence called
G10. CYT003-QbG10
is designed to induce a
potent Th1 type
immune response in
order to suppress
a
“ llergic”Th2 type
immune responses.
CYT003-QbG10
combined with house
dust mite allergen
extract (CYT005-
AllQbG10) showed
significant efficacy for
house dust mite
allergy. Additionally,
first clinical data with
CYT003-
QbG10 in grass pollen
allergy (monotherapy)
indicate that the
QbG10 component
itself acts
through an allergen-
independent
mechanism of action
Based on its versatile vaccine   -   -   -   -
Immunodrug™
platform, Cytos
Biotechnology is
developing a novel
type of vaccines
designed for induction
of an efficient
"non-allergic" Th1 type
immune response.The
Immunodrug™
candidates comprise
an
allergen extract of
choice mixed with
the
Immunodrug™    carrier
QbG10. QbG10
consists of the virus-
like particle Qb
packaged with an
immunostimulatory
sequence called G10.
G10 serves as an
adjuvant enhancing
the establishment of a
Th1 type immune
response
·A glucocorticoid:      ·small molecule:   Well absorbed orally    -   ·441.5: deflazacort   ·Practically Insoluble:
deflazacort             deflazacort        and immediately                                   deflazacort
                                           converted by plasma
                                           esterases to the
                                           pharmacologically
                                           active metabolite (D
                                           21OH), which
                                           achieves peak plasma
                                           concentrations in 1.5
                                           to 2 hours. Metabolism
                                           of D 21-OH is
                                           extensive. 40% protein-
                                           bound. t1/2 is 1.1-1.9
                                           h.


·Corticosteroid with    ·small molecule:   When Captisol-         -    ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide         Enabled Budesonide                                budesonide
activity : budesonide                      Solution is
                                           administered,
                                           budesonide is
                                           delivered to the lung
                                           and subsequently
                                           absorbed into the
                                           blood stream for rapid
                                           clearance of Captisol
                                           and budesonide. Dose
                                           proportinalty has been
                                           shown. Scintographic
                                           images have shown
                                           better distribution of
                                           the captisol solution
                                           vs. Pulmicort
                                           Respules.
Tryptase is a secreted -                -   -   -   -
serine protease, stored
in granules and
released from mast
cells upon
degranulation after
allergen challenge.
Elevated tryptase
levels have been
detected in serum and
bronchoalveolar
lavage fluid of patients
with allergic asthma.
Celera Genomics has
identified different
classes of compounds
that potently and
selectively inhibit
human tryptase.




PDE-4 Inhibitor        small molecule   -   -   -   -
Itk (IL2-inducible T-cell small molecule   -   -   -   -
kinase) inhibitors. A
member of the protein
tyrosine-kinase family.
Itk regulates the
activity of at least two
types of cells in the
immune system, T-
lymphocytes and mast
cells. Itk transduces
the signal which is
generated when the
receptors on these
cells are stimulated,
leading to the
production of cytokines
and to the proliferation
of these cells.



PI3Kδ inhibitor    small molecule     -   -   -   -

PDE-IV Inhibitors       -                  -   -   -   -
·Bronchodilator;         ·small molecule:        Protein binding is 40%. -   ·283.33: oxtriphylline   ·Freely Soluble:
asthma                   oxtriphylline                                                                oxtriphylline
prophylactic— Theophylli
ne directly relaxes
smooth muscle in the
bronchial airways and
pulmonary blood
vessels. This action is
believed to be
mediated by selective
inhibition of specific
phosphodiesterases
(PDEs), which in turn
produces an increase
in intracellular cyclic
3´, 5´-adenosine
monophosphate (cyclic
AMP).: oxtriphylline


Bronchodilator            ·small molecule:       -                       -   ·283.33: choline         ·: choline theophylline
agents···Bronchodilato    choline theophylline                               theophylline
r agents : choline
theophylline
·New generation           ·small molecule:       -                       -   ·540.69: ciclesonide     ·Practically Insoluble:
inhaled corticosteroid    ciclesonide                                                                 ciclesonide
with novel
pharmacokinetic
properties: ciclesonide
·Cintredekin besudotox ·protein: cintredekin   -   -   ·50708.2: cintredekin   ·: cintredekin
is a recombinant          besudotox                    besudotox               besudotox
protein consisting of a
single molecule
composed of two
parts: a tumor-
targeting molecule
(Interleukin-13) and a
cytotoxic agent
(Pseudomonas
Exotoxin, or PE). IL13
receptors are present
in appreciable
numbers on malignant
glioma cells, but only
to a minimal amount if
at all on healthy brain
cells. The IL13 portion
binds to receptors on
the tumor like a key fits
into a lock. The cancer
cell latches onto and
absorbs the IL13 and
the attached PE,
causing destruction of
the cancer cell.:
cintredekin besudotox
-                       small molecule     -                       -   -                -




·Corticosteroid with    ·small molecule:   Readily absorbed in     -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone     pulmonary tract             beclomethasone   beclomethasone
activity:               dipropionate       (specific performance       dipropionate     dipropionate
beclomethasone                             data not available)
dipropionate
·Ipratropium bromide is   ·small molecule:      Ipratropium bromide is -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic        ipratropium bromide   not readily absorbed       bromide                ipratropium bromide
(parasympatholytic)       hydrate·small         into the systemic          hydrate·548.24:        hydrate·Freely Soluble:
agent which, based on     molecule: albuterol   circulation either from    albuterol sulfate      albuterol sulfate
animal studies,           sulfate               the surface of the lung
appears to inhibit                              or from the
vagally mediated                                gastrointestinal tract.
reflexes by                                     t1/2 is 2 h. Minimally
antagonizing the action                         bound (0 to 9% in
of acetylcholine, the                           vitro) to plasma
transmitter agent                               albumin and α1-
released from the                               acid glycoprotein. It is
vagus nerve.                                    partially
Anticholinergics                                metabolized to inactive
prevent the increases                           ester hydrolysis
in intracellular                                products. The mean
concentration of cyclic                         terminal t1/2 of
guanosine                                       albuterol is 3.9 hours
monophosphate (cyclic                           with a mean CL of 439
GMP) which are                                  mL/min/1.73 m2. It
caused by interaction                           crosses blood-brain
of acetylcholine with                           barrier.
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate·Albuterol
sulfate, the racemic
form of albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate
·Selective long-acting   ·small molecule:   -   -   ·344.405: formoterol   ·Slightly Soluble:
(12 hours) ß2-           formoterol                                        formoterol
adrenergic stimulant
(bronchodilator):
formoterol

·A beta-agonist for the ·small molecule:    -   -   ·275.8: levalbuterol   ·Freely Soluble:
treatment of reversible levalbuterol                hydrochloride          levalbuterol
bronchospasm.:          hydrochloride                                      hydrochloride
levalbuterol
hydrochloride
Inhaled formulation of ·small molecule:   -   -   ·234.34: lidocaine   ·Practically Insoluble:
lidocaine which has       lidocaine                                    lidocaine
been shown to cause
cell death of
eosinophils, white
blood cells that exist at
elevated levels in
asthmatics. This effect
on eosinophils is the
same as seen with
steroid therapies. The
therapy may therefore
eliminate the need for
steroids, which can
have unwanted side
effects···Lidocaine is
an amide-type local
anesthetic agent and
is suggested to
stabilize neuronal
membranes by
inhibiting the ionic
fluxes required for the
initiation and
conduction of
impulses. : lidocaine
·Cromolyn sodium, a ·small molecule:        Poorly absorbed from   -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium   GI tract but readily       sodium              sodium
allergy medication, is                      absorbed in lung.
an FDA-approved drug
for the management of
mild-to-moderate
persistent asthma. It
inhibits the release of
mediators of
inflammation, induced
by specific antigens as
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Cromolyn sodium, a ·small molecule:        -   -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium           sodium              sodium
allergy medication, is
an FDA-approved drug
for the management of
mild-to-moderate
persistent asthma. It
inhibits the release of
mediators of
inflammation, induced
by specific antigens as
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium




·Cromolyn is a          ·small molecule:    -   -   ·468.4: cromolyn    ·Soluble: cromolyn
synthetic compound      cromolyn
that is used to prevent
some allergic
reactions. : cromolyn
Targeted at the B2AR small molecule         -   -   -                       -
receptor
-                    -                      -   -   -                       -

-                        -                  -   -   -                       -

An immune response -                        -   -   -                       -
modifier with agonistic
activity against Toll-like
receptor 7 (TLR7).

·Roflumilast is a        ·small molecule:   -   -   ·403.211: roflumilast   ·: roflumilast
phosphodiesterase        roflumilast
type-4 inhibitor.:
roflumilast




·Theophylline has two ·small molecule:      -   -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline                                        theophylline
airways of patients
with reversible
obstruction; smooth
muscle relaxation (i.e.,
bronchodilation) and
suppression of the
response of the
airways to stimuli

: theophylline
Dual Target inhibitor of antibodies   -   -   -   -
key cytokines in
asthma pathogenesis
targets IL-4 + IL-13
·Selective              ·small molecule:        When a single dose of -    ·282.73: ozagrel   ·Soluble: ozagrel
thromboxane             ozagrel hydrochloride   200 mg is orally           hydrochloride      hydrochloride
synthetase inhibitor:                           administered to
ozagrel hydrochloride                           healthy adults, the
                                                plasma concentration
                                                reaches its peak in
                                                about 1.3
                                                hours. Its
                                                concentration is
                                                approximately 1.9
                                                μg/mL. The
                                                plasma half-life is
                                                approximately 1.45
                                                hours. 74.6% of the
                                                dose administered is
                                                excreted into the urine
                                                within 48 hours after
                                                administration, and the
                                                majority of it is
                                                excreted within 8
                                                hours after
                                                administration. The
                                                principal metabolites in
                                                the plasma
                                                and urine are the beta-
                                                oxide form of the
                                                propenoic acid portion
                                                and its reduced form.
                                                Some of these and the
                                                unchanged drug
                                                are excreted into the
                                                urine as glucuronic
                                                acid conjugates
Dual PI3K                -                -   -   -   -
gamma/delta
inhibitors, which retain
their selectivity over
the other members of
the PI-kinase family

-                        -                -   -   -   -


-                        -                -   -   -   -


An antisense            oligonucleotide   -   -   -   -
oligonucleotide for the
treatment of asthma
developed to attenuate
the production of the
adenosine A1 receptor
in the cells lining the
lung.


Cyclosporine A analog. -                  -   -   -   -
Calcineurin inhibitor;
demonstrated to
suppress some
humoral immunity and
to a greater extent, cell-
mediated immune
reactions.
Cyclosporine A analog. -                         -   -   -                      -
Calcineurin inhibitor;
demonstrated to
suppress some
humoral immunity and
to a greater extent, cell-
mediated immune
reactions.


Combination of EPI-        ·small molecule:      -   -   ·: undisclosed small   ·: undisclosed small
12323 with a long          undisclosed small             molecule·: undisclosed molecule·: undisclosed
acting beta agonist.···:   molecule·small                small molecule         small molecule
undisclosed small          molecule: undisclosed
molecule·: undisclosed     small molecule
small molecule
The compound has the small molecule   -   -   -   -
potential to reduce
exacerbation of
asthma and to reduce
the intake of inhaled
corticosteroids and
bronchodilators,
thereby reducing their
side-effects.


-                    -                -   -   -   -
·Cromolyn sodium, a ·small molecule:        poorly absorbed from -    ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium   the gastrointestinal      sodium              sodium
allergy medication, is                      tract, with a reported
an FDA-approved drug                        bioavailability of only
for the management of                       1%. The elimination
mild-to-moderate                            half-life has been
persistent asthma. It                       reported to be about
inhibits the release of                     20 to 60 minutes after
mediators of                                intravenous
inflammation, induced                       administration, but the
by specific antigens as                     elimination half-life
well as nonspecific                         following oral
mechanisms, such as                         administration or
exercise, from mast                         inhalation is longer,
cells. Cromolyn may                         being stated to be
also inhibit the activity                   about 80 minutes.
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Most potent stimulant ·small molecule:   -   -   ·183.204: epinephrine ·Very Slightly Soluble:
(sympathomimetic) of epinephrine                                        epinephrine
adrenergic alpha and
beta-receptors,
resulting in increased
heart rate and force of
contraction,
vasoconstriction or
vasodilation, relaxation
of bronchiolar and
intestinal smooth
muscle: epinephrine
·Theophylline has two ·small molecule:   -   -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline                                     theophylline
airways of patients
with reversible
obstruction; smooth
muscle relaxation (i.e.,
bronchodilation) and
suppression of the
response of the
airways to stimuli

: theophylline
·Theophylline has two ·small molecule:   -   -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline                                     theophylline
airways of patients
with reversible
obstruction; smooth
muscle relaxation (i.e.,
bronchodilation) and
suppression of the
response of the
airways to stimuli

: theophylline




Compounds targeting   peptide            -   -   -                       -
G protein-coupled
receptors (GPCRs)




A molecular approach siRNA               -   -   -                       -
using a unique siRNA
and antisense DNA
treatments to prevent
the production of Syk
kinase which is a
molecule in
inflammatory cells
required for the
release of mediators
and cytokines that
cause organ damage.
Inhibits the production peptide   Results of Phase I       -   -   -
of inflammatory                   have shown that
cytokines.                        FAR404 is a safe, non-
                                  toxic and well-tolerated
                                  bio-available
                                  compound with no side
                                  effects in healthy
                                  human volunteers.


VPAC2 agonists         -          -                        -   -   -
suppress the release
of inflammatory
mediators (TNF-alpha,
IL-12), as well as
suppressing the
eosinophil response to
stimuli.
·Corticosteroid with      ·small molecule:       -   -   ·521.04:              ·Practically Insoluble:
mainly glucocorticoid     beclomethasone                 beclomethasone        beclomethasone
activity:                 dipropionate·small             dipropionate·804.9:   dipropionate·Slightly
beclomethasone            molecule: formoterol           formoterol fumarate   Soluble: formoterol
dipropionate·Long-        fumarate                                             fumarate
acting beta(2) agonist:
formoterol fumarate




A3 antagonist             -                      -   -   -                     -
·Corticosteroid with      ·small molecule:       Oral BA is less than -   ·500.57: fluticasone    ·Practically Insoluble:
mainly glucocorticoid fluticasone propionate     1%. Systemic BA from     propionate              fluticasone propionate
activity. It has weak                            inhalation averaged
affinity for the                                 13.5%
progesterone receptor,
and virtually no affinity
for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
propionate


·Prednisolone is a        ·small molecule:       -                    -   ·402.484: prednisolone ·Practically Insoluble:
corticosteroid with       prednisolone acetate                            acetate                prednisolone acetate
mainly glucocorticoid
activity : prednisolone
acetate
·Corticosteroid with      ·small molecule:   Oral BA                    -   ·500.57: fluticasone   ·Practically Insoluble:
mainly glucocorticoid fluticasone propionate                                propionate             fluticasone propionate
activity. It has weak
affinity for the
progesterone receptor,
and virtually no affinity
for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
propionate



·Corticosteroid with      ·small molecule:     Oral BA is less than     -   ·500.57: fluticasone   ·Practically Insoluble:
mainly glucocorticoid fluticasone propionate   1%. Systemic BA from         propionate             fluticasone propionate
activity. It has weak                          inhalation averaged
affinity for the                               18%. First pass
progesterone receptor,                         metabolism. Vd is 4.2
and virtually no affinity                      L/kg. Plasma protein
for the                                        binding is 91%. Total
mineralocorticoid,                             CL is 0.066 L/h. t1/2 is
estrogen, or androgen                          7.8 hrs.
receptors.: fluticasone
propionate
·Corticosteroid with      ·small molecule:     Fluticasone propionate -   ·500.57: fluticasone   ·Practically Insoluble:
mainly glucocorticoid fluticasone propionate   is poorly absorbed         propionate             fluticasone propionate
activity. It has weak                          from the
affinity for the                               gastrointestinal tract
progesterone receptor,                         and undergoes
and virtually no affinity                      extensive first-pass
for the                                        metabolism; oral
mineralocorticoid,                             bioavailability is
estrogen, or androgen                          reported to be only
receptors.: fluticasone                        about 1%. In healthy
propionate                                     subjects the mean
                                               systemic BA of
                                               Flixotide Evohaler is
                                               28.6%. In patients with
                                               asthma the mean
                                               systemic absolute BA
                                               was reduced by 62%.
                                               Systemic absorption
                                               occurs mainly through
                                               the lungs and has
                                               been shown to be
                                               linearly related to dose
                                               over the dose range
                                               500 to 2000
                                               micrograms.
                                               Absorption is initially
                                               rapid then prolonged
                                               and the remainder of
                                               the dose may be
                                               swallowed.
Fluasterone will be an ·small molecule:      -   -   ·290.415: fluasterone   ·: fluasterone
alternative to fibrates fluasterone
for lowering triglyceride
in
combination therapy
with a statin in insulin-
resistant patients. It
also inhibits NF-kB
activation and reduces
oxidative
stress.···Fluasterone is
a synthetically stable
adrenocortical steroid
analogue
of
dehydroepiandrosteron
e (DHEA). It also
inhibits NF-kB
activation and reduces
oxidative stress.:
fluasterone

·Corticosteroid with      ·small molecule:   -   -   ·500.57: fluticasone    ·Practically Insoluble:
mainly glucocorticoid fluticasone propionate         propionate              fluticasone propionate
activity. It has weak
affinity for the
progesterone receptor,
and virtually no affinity
for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
propionate
·Selective long-acting     ·small molecule:        -                    -   ·344.405:              ·Slightly Soluble:
(12 hours) ß2-             formoterol·small                                 formoterol·500.57:     formoterol·Practically
adrenergic stimulant       molecule: fluticasone                            fluticasone propionate Insoluble: fluticasone
(bronchodilator):          propionate                                                              propionate
formoterol·Corticostero
id with mainly
glucocorticoid activity.
It has weak affinity for
the progesterone
receptor, and virtually
no affinity for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
propionate



·Long-acting beta(2)       ·small molecule:        Cmax of 92 pg/mL is -    ·804.9: formoterol     ·Slightly Soluble:
agonist: formoterol        formoterol fumarate     reached within 5         fumarate               formoterol fumarate
fumarate                                           minutes of dosing.
                                                   Binding to plasma
                                                   proteins is 61%-64%.
                                                   Four cytochrome P450
                                                   isozymes (CYP2D6,
                                                   CYP2C19, CYP2C9
                                                   and CYP2A6) are
                                                   involved in the
                                                   metabolism. t1/2 is 10
                                                   hrs.
·Long-acting beta(2)   ·small molecule:      -   -   ·804.9: formoterol   ·Slightly Soluble:
agonist: formoterol    formoterol fumarate           fumarate             formoterol fumarate
fumarate
·Long-acting beta(2)   ·small molecule:      Inhaled formoterol is   -   ·804.9: formoterol   ·Slightly Soluble:
agonist: formoterol    formoterol fumarate   rapidly absorbed. It is     fumarate             formoterol fumarate
fumarate                                     largely metabolised by
                                             glucuronidation and O-
                                             demethylation, with
                                             about 10% being
                                             excreted as
                                             unchanged drug. The
                                             terminal t1/2 is
                                             estimated to be 8 hrs.
                                             Onset of action in 1-3
                                             minutes with 12 hours
                                             of bronchodilation.
·Selective long-acting   ·small molecule:      Inhaled formoterol is   -   ·344.405: formoterol   ·Slightly Soluble:
(12 hours) ß2-           formoterol            rapidly absorbed. It is                            formoterol
adrenergic stimulant                           largely metabolised by
(bronchodilator):                              glucuronidation and O-
formoterol                                     demethylation, with
                                               about 10% being
                                               excreted as
                                               unchanged drug. The
                                               terminal elimination
                                               t1/2 is estimated to be
                                               8 hrs.
·Long-acting beta(2)     ·small molecule:      -                       -   ·804.9: formoterol     ·Slightly Soluble:
agonist: formoterol      formoterol fumarate                               fumarate               formoterol fumarate
fumarate
·Long-acting beta(2)     ·small molecule:      Inhaled formoterol is   -   ·804.9: formoterol     ·Slightly Soluble:
agonist: formoterol      formoterol fumarate   rapidly absorbed and        fumarate               formoterol fumarate
fumarate                                       metabolised by
                                               glucuronidation and O-
                                               demethylation, with
                                               about 10% being
                                               excreted as
                                               unchanged drug. The
                                               terminal t1/2 after
                                               inhalation is estimated
                                               to be 8 h.




·Long-acting beta(2)     ·small molecule:      -                       -   ·804.9: formoterol     ·Slightly Soluble:
agonist: formoterol      formoterol fumarate                               fumarate               formoterol fumarate
fumarate




·Selective long-acting   ·small molecule:      -                       -   ·344.405: formoterol   ·Slightly Soluble:
(12 hours) ß2-           formoterol                                                               formoterol
adrenergic stimulant
(bronchodilator):
formoterol
·Corticosteroid with      ·small molecule:       Preliminary           -   ·521.04:              ·Practically Insoluble:
mainly glucocorticoid     beclomethasone         pharmacokinetic and       beclomethasone        beclomethasone
activity:                 dipropionate·small     pharmacodynamic           dipropionate·804.9:   dipropionate·Slightly
beclomethasone            molecule: formoterol   investigations with       formoterol fumarate   Soluble: formoterol
dipropionate·Long-        fumarate               Foster® DPI have                                fumarate
acting beta(2) agonist:                          been completed.
formoterol fumarate                              (source: company
                                                 website)
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide




IL-13 is a central      protein            -   -   -                     -
mediator of T helper
cell (Th2 responses).
·A highly selective     ·small molecule:   -   -   ·516.3: oglemilast    ·: oglemilast
PDE-4 inhibitor:        oglemilast
oglemilast

Reduce the number of peptide               -   -   -                     -
respitatory
inflammatory cells and
their marker enzymes
in a rodent model of
allergic asthma.

RNA interference       siRNA               -   -   -                     -
(RNAi)-based
therapeutics
·Inhaled bifunctional, ·small molecule:    -   -   ·137.136: MABA        ·Slightly Soluble:
muscarinic antagonist/ MABA                                              MABA
beta2 agonist: MABA
·Muscarinic            ·small molecule:      -   -   ·425.4: darotropium   ·: darotropium bromide
acetylcholine          darotropium bromide           bromide
antagonist:
darotropium bromide




Long-acting beta2      small molecule        -   -   -                     -
agonist

·Corticosteroid with      ·small molecule:   -   -   ·538.6: fluticasone   ·Practically Insoluble:
mainly glucocorticoid fluticasone furoate            furoate               fluticasone furoate
activity. It has weak
affinity for the
progesterone receptor,
and virtually no affinity
for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
furoate
A combination of the ·small molecule:          -   -   ·538.6: fluticasone   ·Practically Insoluble:
corticosteroid           fluticasone furoate           furoate               fluticasone furoate
GW685698X and the
long-acting ß2-agonist
GW642444M···Cortico
steroid with mainly
glucocorticoid activity.
It has weak affinity for
the progesterone
receptor, and virtually
no affinity for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
furoate



Galapagos has used small molecule              -   -   -                     -
the knock-in and
knock-down adenoviral
vector technology to
discover and validate
novel small molecule
drugable targets in
rheumatoid arthritis,
osteoarthritis and
osteoporosis. Potential
drug targets have
been identified for all
three of its core
disease area as well
as in Alzheimer’ s
disease and asthma.
Leukotriene inhibitor     small molecule        -   -   -                      -
that acts on 5-
lipoxygenase (5-LO)
·Ipratropium bromide is   ·small molecule:      -   -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic        ipratropium bromide           bromide hydrate        ipratropium bromide
(parasympatholytic)       hydrate                                              hydrate
agent which, based on
animal studies,
appears to inhibit
vagally mediated
reflexes by
antagonizing the action
of acetylcholine, the
transmitter agent
released from the
vagus nerve.
Anticholinergics
prevent the increases
in intracellular
concentration of cyclic
guanosine
monophosphate (cyclic
GMP) which are
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate
·Ipratropium bromide is ·small molecule:      -   -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic      ipratropium bromide           bromide hydrate        ipratropium bromide
(parasympatholytic)     hydrate                                              hydrate
agent which, based on
animal studies,
appears to inhibit
vagally mediated
reflexes by
antagonizing the action
of acetylcholine, the
transmitter agent
released from the
vagus nerve.
Anticholinergics
prevent the increases
in intracellular
concentration of cyclic
guanosine
monophosphate (cyclic
GMP) which are
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate
·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate




·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate




Ii-Key/allergen epitope peptide               -   -   -                    -
hybrid peptides
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·Corticosteroid with    ·small molecule:   Budesonide is rapidly -    ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide         and almost completely                            budesonide
activity : budesonide                      absorbed following
                                           administration by
                                           mouth, but has poor
                                           systemic availability
                                           (about 10%) due to
                                           extensive first-pass
                                           metabolism in the liver,
                                           mainly by the
                                           cytochrome P450
                                           isoenzyme CYP3A4.
                                           The major metabolites,
                                           6-β-
                                           hydroxybudesonide
                                           and 16-α-
                                           hydroxyprednisolone
                                           have less than 1% of
                                           the glucocorticoid
                                           activity of unchanged
                                           budesonide. t1/2 is 2 -
                                           4 hrs. (REF 1-
                                           (Pubmed
                                           id:11475468), REF 2-
                                           (Pubmed
                                           id:15355126))
·Corticosteroid with   ·small molecule:       -   -   ·430.53:              ·Practically Insoluble:
mainly glucocorticoid budesonide·small                budesonide·344.405:   budesonide·Slightly
activity :             molecule: formoterol           formoterol            Soluble: formoterol
budesonide·Selective
long-acting (12 hours)
ß2-adrenergic
stimulant
(bronchodilator):
formoterol
·LAMA. Glycopyrrolate ·small molecule:         -   -   ·398.335:              ·Soluble:
binds to the muscarinic glycopyrrolate bromide         glycopyrrolate bromide glycopyrrolate bromide
acetylcholine receptor.
Like other
anticholinergic
(antimuscarinic)
agents, inhibits the
action of acetylcholine
on structures
innervated by
postganglionic
cholinergic nerves and
on smooth muscles
that respond to
acetylcholine but lack
cholinergic
innervation.:
glycopyrrolate bromide




HAE1 binds to            antibodies            -   -   -                      -
circulating IgE thereby
blocking the binding of
IgE to the high affinity
receptor on mast cells
and inhibiting
inflammatory mediator
release.
T-regulatory cell     protein                -   -   -                      -
activator providing
blockade of
inapporopriate
inflammatory response
without broad or
unspecific immune
suppression.
·: undisclosed small   ·small molecule:      -   -   ·: undisclosed small   ·: undisclosed small
molecule·: undisclosed undisclosed small             molecule·: undisclosed molecule·: undisclosed
small molecule         molecule·small                small molecule         small molecule
                       molecule: undisclosed
                       small molecule
-                   -                -   -   -   -


Small molecule      small molecule   -   -   -   -
modulators of the
HSP20 signal.
·Adrenergic beta2-       ·small molecule:   After a single           -   ·227.73: tulobuterol   ·Practically Insoluble:
agonist similar to       tulobuterol        transdermal                                         tulobuterol
albuterol: tulobuterol                      application
                                            of 2mg via patch for
                                            24hrs to healthy
                                            adults, are
                                            Cmax(ng/mL): 1.35
                                            Tmax(hr): 11.8 AUC0-
                                            ∞(ng・h
                                            r/mL): 27.8
                                            T1/2(hr):5.9. A single
                                            transdermal
                                            application of
                                            tulobuterol for 24hrs to
                                            pediatric patients with
                                            bronchial asthma was
                                            performed with a 1mg
                                            patch for patients 4 to
                                            9 years of age (weight
                                            18.0 to 26.5kg) and
                                            2mg patch for patients
                                            9 to 13 years of age
                                            (weight 33.0 to 41.7kg)
                                            respectively.After one
                                            tulobuterol patch
                                            (4mg) was applied to
                                            the skin of healthy
                                            adults for 24hrs, the
                                            unchanged
                                            compound,
                                            3-hydroxy compound,
                                            4-hydroxy compound,
                                            5-hydroxy compound
                                            and their conjugates, 4-
kinase inhibitor project -                  -                        -   -                      -
-                       -         -   -   -   -


-                       -         -   -   -   -


-                       -         -   -   -   -


-                       -         -   -   -   -


Supresses signalling    peptide   -   -   -   -
of the cytokines IL-4
and IL-13



Protein-based product protein     -   -   -   -
candidate designed to
bind both the
interleukin-4 and
interleukin-13 (called
IL-4 and IL-13)
cytokines and prevent
their interaction with
cell surface receptors.
·Cintredekin besudotox ·protein: cintredekin   -   -   ·50708.2: cintredekin   ·: cintredekin
is a recombinant          besudotox                    besudotox               besudotox
protein consisting of a
single molecule
composed of two
parts: a tumor-
targeting molecule
(Interleukin-13) and a
cytotoxic agent
(Pseudomonas
Exotoxin, or PE). IL13
receptors are present
in appreciable
numbers on malignant
glioma cells, but only
to a minimal amount if
at all on healthy brain
cells. The IL13 portion
binds to receptors on
the tumor like a key fits
into a lock. The cancer
cell latches onto and
absorbs the IL13 and
the attached PE,
causing destruction of
the cancer cell.:
cintredekin besudotox




Targets IL-4            peptide                -   -   -                       -

-                       vaccine                -   -   -                       -
·A humanized antibody      ·antibodies:       -   -   ·145400:             ·: anrukinzumab
to human IL-13:            anrukinzumab               anrukinzumab
anrukinzumab
INV102 is an oral, daily   ·small molecule:   -   -   ·309.4: nadolol      ·Slightly Soluble:
therapy that acts as a     nadolol                                         nadolol
beta inverse agonist
up-regulating the
corresponding
receptors .···Non-
selective beta-blocker:
nadolol




·Inhibits the release of ·small molecule:     -   -   ·499.65: suplatast   ·: suplatast tosilate
cytokines (IL-4, IL-5)   suplatast tosilate           tosilate
from Th2 cells without
effects on IFN-gamma
from Th1 cells in vitro.
: suplatast tosilate
·Inhibits the release of ·small molecule:       -   -   ·499.65: suplatast    ·: suplatast tosilate
cytokines (IL-4, IL-5)   suplatast tosilate             tosilate
from Th2 cells without
effects on IFN-gamma
from Th1 cells in vitro.
: suplatast tosilate

An oral, second      small molecule             -   -   -                     -
generation LSAID(TM)
(Leukocyte Selective
Anti-Inflammatory
Drug)

An oral LSAID(TM)         small molecule        -   -   -                     -
(Leukocyte Selective
Anti-Inflammatory
Drug),
·Icatibant is a potent    ·peptide: icatibant   -   -   ·1304.52: icatibant   ·Soluble: icatibant
and highly specific
competitive antagonist
of the bradykinin B2
receptor. Bradykinin is
a peptide hormone
that is formed locally in
the body, very often as
a response to trauma.
Bradykinin increases
vascular permeability,
dilates blood vessels:
icatibant



IL-1ß inhibitors         small molecule         -   -   -                     -
·Corticosteroid with      ·small molecule:    -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid     budesonide                                        budesonide
activity : budesonide




Interleukin-1 receptor    -                   -   -   -                     -

·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol    ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate               albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate




Formulated ISS for       vaccine              -   -   -                     -
pulmonary delivery
with no linked allergen,
relying on natural
exposure to multiple
allergens to produce
specific long-term
immunity
·Cromolyn sodium, a ·small molecule:        This drug is a product -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium   in which the inactive      sodium              sodium
allergy medication, is                      ingredients of
an FDA-approved drug                        chlorofluorocarbon
for the management of                       group (specific fron),
mild-to-moderate                            etc. contained in
persistent asthma. It                       INTAL
inhibits the release of                     Aerosol are altered.
mediators of                                After a dose of two
inflammation, induced                       sprays (2 mg as
by specific antigens as                     sodium
well as nonspecific                         cromoglicate) of this
mechanisms, such as                         product and INTAL
exercise, from mast                         Aerosol inhaled
cells. Cromolyn may                         in 35 healthy adults by
also inhibit the activity                   cross-over method,
of other cell types that                    maximum plasma
produce inflammation.                       concentrations were
It is the only                              3.15 ng/mL at 0.33
antiasthmatic that                          hours and 3.20
blocks both early and                       ng/mL
late asthmatic                              at 0.20 hours,
responses induced by                        respestively. In 11
allergen inhalation and                     healthy adults inhaled
exercise. : cromolyn                        the
sodium                                      above dose of this
                                            product and INTAL
                                            Aerosol, urinary
                                            excretion
                                            rates up to 24 hours
                                            after the inhalation
                                            were 6.83% and
                                            5.61% of the
                                            administered dose,
·Cromolyn sodium, a ·small molecule:        One capsule of this     -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium   product (20 mg as           sodium              sodium
allergy medication, is                      sodium
an FDA-approved drug                        cromoglicate)
for the management of                       with an inhaling
mild-to-moderate                            instrument for the
persistent asthma. It                       exclusive use of
inhibits the release of                     this product
mediators of                                (Spinhaler) and one
inflammation, induced                       ampoule of INTAL
by specific antigens as                     Nebuliser
well as nonspecific                         Solution (20 mg as
mechanisms, such as                         sodium cromoglicate/2
exercise, from mast                         mL) with
cells. Cromolyn may                         an electromotive
also inhibit the activity                   nebulizer were
of other cell types that                    administered to 10
produce inflammation.                       healthy
It is the only                              adults, respectively by
antiasthmatic that                          cross-over method.
blocks both early and                       The urinary excretion
late asthmatic                              rates up to 24 hours
responses induced by                        after inhalation were
allergen inhalation and                     7.92%
exercise. : cromolyn                        and 4.83% of
sodium                                      administered dose,
                                            respectively.3) The
                                            difference
                                            of the results was
                                            considered to be due
                                            to difference
                                            of inhalation method.
                                            In 4 healthy volunteers
                                            administered
·Cromolyn sodium, a ·small molecule:        -   -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium           sodium              sodium
allergy medication, is
an FDA-approved drug
for the management of
mild-to-moderate
persistent asthma. It
inhibits the release of
mediators of
inflammation, induced
by specific antigens as
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Cromolyn sodium, a ·small molecule:        Poorly absorbed from   -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium   GI tract but readily       sodium              sodium
allergy medication, is                      absorbed in lung. 8%
an FDA-approved drug                        of delivered dose is
for the management of                       absorbed in lung.
mild-to-moderate
persistent asthma. It
inhibits the release of
mediators of
inflammation, induced
by specific antigens as
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Cromolyn sodium, a ·small molecule:        After administration by -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium   inhalation,                 sodium              sodium
allergy medication, is                      approximately 8% of
an FDA-approved drug                        the total cromolyn
for the management of                       sodium dose
mild-to-moderate                            administered is
persistent asthma. It                       absorbed and rapidly
inhibits the release of                     excreted unchanged,
mediators of                                approximately equally
inflammation, induced                       divided between urine
by specific antigens as                     and bile.
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Cromolyn sodium, a ·small molecule:        -   -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium           sodium              sodium
allergy medication, is
an FDA-approved drug
for the management of
mild-to-moderate
persistent asthma. It
inhibits the release of
mediators of
inflammation, induced
by specific antigens as
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Cromolyn sodium, a ·small molecule:        -   -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium           sodium              sodium
allergy medication, is
an FDA-approved drug
for the management of
mild-to-moderate
persistent asthma. It
inhibits the release of
mediators of
inflammation, induced
by specific antigens as
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Cromolyn sodium, a ·small molecule:        Poorly absorbed from   -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium   GI tract but readily       sodium              sodium
allergy medication, is                      absorbed in lung. 8%
an FDA-approved drug                        of delivered dose is
for the management of                       absorbed in lung.
mild-to-moderate
persistent asthma. It
inhibits the release of
mediators of
inflammation, induced
by specific antigens as
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Cromolyn sodium, a ·small molecule:        -   -   ·512.33: cromolyn   ·Soluble: cromolyn
non-steroidal anti-       cromolyn sodium           sodium              sodium
allergy medication, is
an FDA-approved drug
for the management of
mild-to-moderate
persistent asthma. It
inhibits the release of
mediators of
inflammation, induced
by specific antigens as
well as nonspecific
mechanisms, such as
exercise, from mast
cells. Cromolyn may
also inhibit the activity
of other cell types that
produce inflammation.
It is the only
antiasthmatic that
blocks both early and
late asthmatic
responses induced by
allergen inhalation and
exercise. : cromolyn
sodium
·Ipratropium bromide is ·small molecule:      -   -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic      ipratropium bromide           bromide hydrate        ipratropium bromide
(parasympatholytic)     hydrate                                              hydrate
agent which, based on
animal studies,
appears to inhibit
vagally mediated
reflexes by
antagonizing the action
of acetylcholine, the
transmitter agent
released from the
vagus nerve.
Anticholinergics
prevent the increases
in intracellular
concentration of cyclic
guanosine
monophosphate (cyclic
GMP) which are
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate
·Ipratropium bromide is ·small molecule:      small amount of          -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic      ipratropium bromide   ipratropium enters the       bromide hydrate        ipratropium bromide
(parasympatholytic)     hydrate               systemic circulation, if                            hydrate
agent which, based on                         some ipratropium is
animal studies,                               swallowed, it is poorly
appears to inhibit                            absorbed from GI
vagally mediated                              tract.
reflexes by
antagonizing the action
of acetylcholine, the
transmitter agent
released from the
vagus nerve.
Anticholinergics
prevent the increases
in intracellular
concentration of cyclic
guanosine
monophosphate (cyclic
GMP) which are
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate
·Although its precise    ·small molecule:      -   -   ·512.333: sodium     ·Soluble: sodium
mode of action           sodium cromoglycate           cromoglycate         cromoglycate
remains uncertain,
sodium cromoglycate
is believed to act
primarily by preventing
release of mediators of
inflammation from
sensitised mast cells
through stabilisation of
mast-cell membranes.
: sodium cromoglycate



-                         -                    -   -   -                    -

Blocking the function     antibodies           -   -   -                    -
of a particular protein
target with the
neutralizing
antibody.[17872]
·A sulfidopeptide         ·small molecule:     -   -   ·530.7: tipelukast   ·: tipelukast
leukotriene receptor      tipelukast
antagonist: tipelukast
·: undisclosed small   ·small molecule:      -   -   ·: undisclosed small   ·: undisclosed small
molecule·: undisclosed undisclosed small             molecule·: undisclosed molecule·: undisclosed
small molecule         molecule·small                small molecule         small molecule
                       molecule: undisclosed
                       small molecule




-                      small molecule        -   -   -                      -

-                      small molecule        -   -   -                      -


Leukotriene D(4) and   -                     -   -   -                      -
Thromboxane A(2)
Receptor dual
antagonist
-                      carbohydrate          -   -   -                     -

·Selective beta2-      ·small molecule:      -   -   ·955.1: bedoradrine   ·: bedoradrine sulfate
adenoreceptor agonist. bedoradrine sulfate           sulfate
The drug's selectivity
for the beta2 receptor
is hoped to limit
cardiological side
effects.: bedoradrine
sulfate
Phosphodiesterase       -                  -   -   -                    -
(PDE)-IV inhibitor with
a higher anti-
inflammatory activity
than that of
leukotrienes
·Non-selective          ·small molecule:   -   -   ·230.31: ibudilast   ·Very Slightly Soluble:
phosphodiesterase       ibudilast                                       ibudilast
(PDE) inhibitor.
Approved molecule in
Japan: ibudilast




-                       small molecule     -   -   -                    -

-                       small molecule     -   -   -                    -

A2B adenosine        -                     -   -   -                    -
antagonist
backup for LAS100977 -                     -   -   -                    -

-                       -                  -   -   -                    -




-                       -                  -   -   -                    -
-                        -   -   -   -   -


LDTI has been            -   -   -   -   -
successfully
expressed in yeasts
and is an inhibitor of
human mast cell
tryptase and inhibits
tryptase-induced
human fibroblast
proliferation.
·Corticosteroid with    ·small molecule:            has
                                           Lodotra™ been            -   ·358.431: prednisone   ·Very Slightly Soluble:
mainly glucocorticoid   prednisone         designed so that                                    prednisone
activity: prednisone                       maximum plasma
                                           levels are reached six
                                           hours after intake. This
                                           enables a patient to
                                           swallow the tablet at
                                           10pm before going to
                                           sleep, with the dose of
                                           prednisone not being
                                           released until 2am,
                                           reaching maximum
                                           plasma levels at 4am
                                           which is regarded as
                                           the optimal timing to
                                           relieve the stiffness
                                           and pain on waking.




Long-Acting Beta        -                  -                        -   -                      -
Agonists
·Loteprednol etabonate ·small molecule:          In the randomized,        -   ·466.95: loteprednol   ·: loteprednol
is a corticosteroid used loteprednol etabonate   double-blind (except          etabonate              etabonate
for its glucocorticoid                           for fluticasone
activity in the topical                          propionate ), parallel-
management of                                    group study (n =
inflammatory and                                 8/group), all subjects
allergic disorders of                            received for 14 days
the eye.: loteprednol                            once daily in the
etabonate                                        morning two puffs of
                                                 the following nasal
                                                 spray formulations into
                                                 each nostril: LE 0.1%
                                                 (400 microg/day), LE
                                                 0.2% (800
                                                 microg/day), FP 0.05%
                                                 (200 microg/day), and
                                                 placebo. All
                                                 formulations were
                                                 rapidly absorbed
                                                 (t(max) less than 1 h).
                                                 The rather short mean
                                                 terminal half-lives of
                                                 2.2 +/- 1.5 hours and
                                                 1.8 +/- 1.0 hours for LE
                                                 400 microg and LE
                                                 800 microg,
                                                 respectively, and 4.2 +/-
                                                 1.8 hours for the 200-
                                                 microg FP treatment
                                                 explained the lack of
                                                 any accumulation.
                                                 Mean peak
                                                 concentrations
                                                 (C(max)) were 139 +/-
·Loteprednol etabonate ·small molecule:        -   -   ·466.95: loteprednol   ·: loteprednol
is a corticosteroid used loteprednol etabonate         etabonate              etabonate
for its glucocorticoid
activity in the topical
management of
inflammatory and
allergic disorders of
the eye.: loteprednol
etabonate
·Dyphylline is a         ·small molecule:   It is absorbed rapidly in -   ·254.25: diphylline   ·Freely Soluble:
xanthine derivative      diphylline         therapeutically active                              diphylline
with pharmacologic                          form and in healthy
actions similar to                          volunteers reaches a
theophylline and other                      mean peak plasma
members of this class                       concentration of 17.1
of drugs. Its primary                       mcg/mL in
action is that of                           approximately 45
bronchodilation, but it                     minutes following a
also exhibits peripheral                    single oral dose of
vasodilatory and other                      1000 mg of LUFYLLIN.
smooth muscle
relaxant activity to a
lesser degree. The
bronchodilatory action
of dyphylline, as with
other xanthines, is
thought to be mediated
through competitive
inhibition of
phosphodiesterase
with a resulting
increase in cyclic AMP
producing relaxation of
bronchial smooth
muscle. : diphylline
·An antibody against    ·antibodies:     In a Phase I, single-       -   ·: lumiliximab   ·: lumiliximab
CD23 which is an        lumiliximab      dose, dose-escalating
important protein on                     clinical trial for allergic
leukemia cells and                       asthma, Cohorts of 3
certain cells in the                     to 6 patients received
body's immune                            single IV infusions of
system: lumiliximab                      either placebo or IDEC-
                                         152 (0.05, 0.25, 1.0,
                                         4.0, 10.0, or 15.0
                                         mg/kg) and Cmax and
                                         AUC of IDEC-152
                                         found to be
                                         proportional to the
                                         dose administered for
                                         the dose range 4.0 to
                                         15.0 mg/kg and t1/2 of
                                         the IDEC-152 antibody
                                         increased from 2 to 10
                                         days with increasing
                                         doses. [Ref 1-
                                         (Pubmed
                                         id:13679816)]




M40403 may be able      small molecule   -                           -   -                -
to supplement the
activity of naturally
occurring SODs
Undisclosed steroids    small molecule   -                           -   -                -
·Corticosteroid with   ·small molecule:       -   -   ·430.53:              ·Practically Insoluble:
mainly glucocorticoid budesonide·small                budesonide·344.405:   budesonide·Slightly
activity :             molecule: formoterol           formoterol            Soluble: formoterol
budesonide·Selective
long-acting (12 hours)
ß2-adrenergic
stimulant
(bronchodilator):
formoterol




Leukotriene D4          small molecule        -   -   -                     -
antagonist with
inhibition of
bronchoconstriction
and allergic response
The companies           antibodies      -                         -   -   -
believe that either the
systemic delivery of an
anti-IL-9 product (an
antibody or a
recombinant molecule)
to the lung will block
the interaction of IL-9
with its receptor.




Inhibits PDE-4,        small molecule   Studies in three          -   -   -
phosphodiesterase,                      species demonstrate
the enzyme that                         high oral bioavailability
breaks down cAMP                        with a safety profile,
levels in the brain.                    that is significantly
                                        superior to other PDE-
                                        4 inhibitors.
·A beta-2 agonist:   ·small molecule:   -   -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol                 hydrochloride         hydrochloride
hydrochloride        hydrochloride
·A beta-2 agonist:   ·small molecule:   When MEPTIN              -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol         Drysyrup 0.005% were         hydrochloride         hydrochloride
hydrochloride        hydrochloride      administered orally to
                                        44 healthy male
                                        subjects at
                                        single doses of 100
                                        μg/subject (The
                                        approved dose for a
                                        single administration
                                        of
                                        MEPTIN Drysyrup
                                        0.005% for adults is 50
                                        μg), Cmax
                                        (pg/mL): 298±111;
                                        tmax (hr): 1.3±0.7; t1/2
                                        (hr): 4.2±1.7; AUC13hr
                                        (pg.hr/mL): 1207±338.

                                        When MEPTIN
                                        Tablets were
                                        administered orally at
                                        single
                                        doses of 50 and 100
                                        μg/subject as
                                        procaterol
                                        hydrochloride, 9.93%
                                        and 11.65% of the
                                        dose wasexcreted into
                                        the urine within 24
                                        hours
                                        postdosing,respectivel
                                        y.

                                        The enzyme is mainly
·A beta-2 agonist:   ·small molecule:   When MEPTIN             -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol         Tablets were                hydrochloride         hydrochloride
hydrochloride        hydrochloride      administered orally to
                                        6 healthy male
                                        subjects at single
                                        doses of 50 and 100
                                        μg/subject as
                                        procaterol
                                        hydrochloride (The
                                        approved dose for a
                                        single oral
                                        administration
                                        of MEPTIN Tablets for
                                        adults is 50 μg.),
                                        Cmax: 97 pg/mL, 226
                                        pg/mL;
                                        Tmax: 1.1 hr, 1.5 hr;
                                        t1/2: not determined,
                                        3.6 hr, respectively.

                                        When MEPTIN
                                        Tablets were
                                        administered orally at
                                        single
                                        doses of 50 and 100
                                        μg/subject as
                                        procaterol
                                        hydrochloride, 9.93%
                                        and 11.65% of the
                                        dose were
                                        excreted into the urine
                                        within 24 hours
                                        postdosing,
                                        respectively.
·A beta-2 agonist:   ·small molecule:   When MEPTIN             -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol         Inhalation Solution was     hydrochloride         hydrochloride
hydrochloride        hydrochloride      administered by
                                        inhalation to 6 healthy
                                        male subjects as 4
                                        doses (40 μg
                                        per
                                        subject as procaterol
                                        hydrochloride), a peak
                                        plasma
                                        concentration of 128
                                        pg/mL was attained at
                                        15 min post-dosing,
                                        followed by a gradual
                                        decline.

                                        When MEPTIN Air
                                        was administered by
                                        inhalation as 4
                                        doses (40 μg per
                                        subject as procaterol
                                        hydrochloride),
                                        14.36% of the dose
                                        was excreted in the
                                        urine within 24
                                        hours post-dosing.

                                        The enzyme is mainly
                                        CYP3A4.

                                        (The approved dose
                                        for a single
                                        administration of
                                        MEPTIN Air is 20
·A beta-2 agonist:   ·small molecule:   -   -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol                 hydrochloride         hydrochloride
hydrochloride        hydrochloride
·A beta-2 agonist:   ·small molecule:   When MEPTIN Syrup -        ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol         was administered           hydrochloride         hydrochloride
hydrochloride        hydrochloride      orally to 44 healthy
                                        male subjects at a
                                        single dose of 100
                                        μg/ subject (The
                                        approved dose for a
                                        single administration of
                                        MEPTIN Syrup for
                                        adults is 50 μg)
                                        as procaterol
                                        hydrochloride in a
                                        fasting condition,
                                        Cmax (pg/mL): 263 ±
                                        104; tmax
                                        (hr): 1.3 ± 0.7; t1/2
                                        (hr): 4.1 ± 1.8;
                                        AUC13hr
                                        (pg.hr/mL): 1151 ±
                                        288.

                                        When MEPTIN
                                        Tablets were
                                        administered orally at
                                        single
                                        doses of 50 and 100
                                        μg/subject as
                                        procaterol
                                        hydrochloride,
                                        9.93% and 11.65% of
                                        the dose were
                                        excreted into the
                                        urine
                                        within 24 hours
·A beta-2 agonist:   ·small molecule:   When MEPTIN            -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol         Tablets were               hydrochloride         hydrochloride
hydrochloride        hydrochloride      administered orally to
                                        6 healthy male
                                        subjects as single
                                        doses of 50 or 100
                                        μg/subject as
                                        procaterol
                                        hydrochloride (The
                                        approved dose for a
                                        single oral
                                        administration of
                                        MEPTIN Tablets for
                                        adults is 50 μg),
                                        Cmax: 97 pg/mL, 226
                                        pg/mL; Tmax: 1.1 hr,
                                        1.5 hr; t1/2: not
                                        determined, 3.6 hr,
                                        respectively.

                                        When MEPTIN
                                        Tablets were
                                        administered orally at
                                        single
                                        doses of 50 and 100
                                        μg/subject as
                                        procaterol
                                        hydrochloride,
                                        9.93% and 11.65% of
                                        the dose were
                                        excreted into the
                                        urine
                                        within 24 hours
                                        postdosing,
·A beta-2 agonist:   ·small molecule:   When MEPTIN              -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol         Tablets were                 hydrochloride         hydrochloride
hydrochloride        hydrochloride      administered orally to
                                        6 healthy male
                                        subjects at single
                                        doses of 50 and 100
                                        μg/subject as
                                        procaterol
                                        hydrochloride (The
                                        approved dose for a
                                        single oral
                                        administration of
                                        MEPTIN Tablets for
                                        adults is 50 μg.),
                                        Cmax: 97 pg/mL, 226
                                        pg/mL; Tmax: 1.1 hr,
                                        1.5 hr; t1/2: not
                                        determined, 3.6 hr,
                                        respectively. When
                                        MEPTIN Tablets were
                                        administered orally at
                                        single doses of 50 and
                                        100 μg/subject
                                        as procaterol
                                        hydrochloride, 9.93%
                                        and 11.65% of the
                                        dose were excreted
                                        into the urine within 24
                                        hours postdosing,
                                        respectively. The
                                        enzyme is mainly
                                        CYP3A4.
·An oral, selective      ·small molecule:   -   -   ·358.843: etoricoxib   ·Practically Insoluble:
cyclo-oxygenase2         etoricoxib                                        etoricoxib
(COX2) inhibitor :
etoricoxib




Monoclonal antibodies antibodies            -   -   -                      -
which target the
interleukin-13 (IL-13)
receptor alpha1
subunit
to�inhibit IL-13
activity
CrTh2 receptor           small molecule     -   -   -                      -
antagonist

·A sulfidopeptide        ·small molecule:   -   -   ·530.7: tipelukast     ·: tipelukast
leukotriene receptor     tipelukast
antagonist: tipelukast
-                        antibodies         -   -   -                      -

A decoy that works     oligonucleotide      -   -   -                      -
against NF κB, a
genetic transcription
gene that functions as
a genetic switch to
activate the
immunological
reaction.


Cytokine Receptor        -                  -   -   -                      -
Regulation
·In vitro studies and in ·small molecule:     Low systemic             -   ·300.353: pirbuterol   ·Freely Soluble:
vivo pharmacologic       pirbuterol acetate   concentration. t1/2 is       acetate                pirbuterol acetate
studies have                                  2 hrs.
demonstrated that
pirbuterol has a
preferential effect on
beta-2 adrenergic
receptors compared
with isoproterenol.:
pirbuterol acetate
·A beta-2 agonist:   ·small molecule:   -   -   ·335.83: procaterol   ·Soluble: procaterol
procaterol           procaterol                 hydrochloride         hydrochloride
hydrochloride        hydrochloride




-                    small molecule     -   -   -                     -


-                    -                  -   -   -                     -
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·The precise              ·small molecule:       -   -   ·521.429: mometasone ·Practically Insoluble:
mechanism of              mometasone                     furoate·344.405:     mometasone
corticosteroid action     furoate·small                  formoterol           furoate·Slightly
on allergic rhinitis is   molecule: formoterol                                Soluble: formoterol
not known.
Corticosteroids have
been shown to have a
wide range of effects
on multiple cell types
(e.g., mast cells,
eosinophils,
neutrophils,
macrophages, and
lymphocytes) and
mediators (e.g.,
histamine,
eicosanoids,
leukotrienes, and
cytokines) involved in
inflammation.
: mometasone
furoate·Selective long-
acting (12 hours) ß2-
adrenergic stimulant
(bronchodilator):
formoterol
·Inhibits              ·small molecule:     -   -   ·608.18: montelukast   ·Freely Soluble:
bronchoconstriction    montelukast sodium           sodium                 montelukast sodium
due to antigen
challenge. Montelukast
is a selective
leukotriene receptor
antagonist of the
cysteinyl leukotriene
CysLT 1 receptor.:
montelukast sodium


·Sodium pyruvate is a ·small molecule:      -   -   ·110.044: sodium       ·Very Soluble: sodium
reactive oxygen          sodium pyruvate            pyruvate               pyruvate
species (ROS)
antagonist that has
been shown to
neutralize oxygen
radicals (specifically
lowering the
overproduction of
superoxide anions),
regulate the production
and level of other
inflammatory
mediators, and
regulate the synthesis
of nitric oxide. Sodium
pyruvate also
increases cellular
levels of glutathione
which is reduced
dramatically in antigen-
induced lung disease
patients.: sodium
pyruvate
-                        -                  -   -   -                      -




-                        -                  -   -   -                      -

·Adrenergic beta2-       ·small molecule:   -   -   ·227.73: tulobuterol   ·Practically Insoluble:
agonist similar to       tulobuterol                                       tulobuterol
albuterol: tulobuterol




-                        small molecule     -   -   -                      -

-                        -                  -   -   -                      -


An orally active         -                  -   -   -                      -
inhibitor of
phosphodiesterase
and thromboxane
synthetase.
An inhaled non-           small molecule   -   -   -   -
glucocorticoid steroid
that targets the
inflammatory and
airway obstruction
cascade in the
asthmatic lung by
inhibiting the build-up
of adenosine in the
lung
·Aminophylline, a        ·small molecule:   When NEOPHYLLIN -          ·420.4: aminophylline   ·Freely Soluble:
complex of               aminophylline      Injection 250 mg was                               aminophylline
theophylline with                           intravenous
ethylenediamine,                            drip-infused to 6
readily liberates                           healthy adult
theophylline in the                         volunteers
body. Aminophylline                         (nonsmokers)
has the actions and                         at a single dose of two
uses of theophylline.:                      ampulesnote) (400mg
aminophylline                               of
                                            theophylline) for 30
                                            min, the peak plasma
                                            theophylline
                                            concentration reached
                                            immediately after
                                            administration,
                                            and was theophylline
                                            disappeared from the
                                            plasma
                                            with a half-life of 9.51
                                            hr. The half-life of
                                            elimination
                                            from the plasma
                                            tended to be shorter in
                                            smokers than in
                                            non-smokers. The
                                            area under the plasma
                                            concentration
                                            time-curve for smokers
                                            was significantly as
                                            compared
                                            to non-smokers (p<
                                            0.05).1)
·Aminophylline, a        ·small molecule:   When NEOPHYLLIN -          ·420.4: aminophylline   ·Freely Soluble:
complex of               aminophylline      Powder was                                         aminophylline
theophylline with                           administered orally
ethylenediamine,                            to 8 healthy adult male
readily liberates                           volunteers at 100 mg
theophylline in the                         of
body. Aminophylline                         aminophylline four
has the actions and                         times a day every 6 hr
uses of theophylline.:                      (400
aminophylline                               mg/day) for 13
                                            consecutive times, the
                                            plasma theophylline
                                            concentration
                                            increased gradually for
                                            2 days and
                                            reached an almost
                                            steady-state on the
                                            third day after
                                            administration (after 48
                                            hr). Range of effective
                                            blood concentration: 8-
                                            20&#956;g/mL in
                                            adults
                                            Main cytochrome P450
                                            subfamily involved in
                                            metabolism:
                                            CYP1A2.
·Aminophylline, a        ·small molecule:   When NEOPHYLLIN -           ·420.4: aminophylline   ·Freely Soluble:
complex of               aminophylline      Tablets 100 mg was                                  aminophylline
theophylline with                           administered
ethylenediamine,                            orally to 7 healthy adult
readily liberates                           male volunteers at
theophylline in the                         100
body. Aminophylline                         mg of aminophylline
has the actions and                         four times a day every
uses of theophylline.:                      6 hr (400
aminophylline                               mg/day) for 13
                                            consecutive times, the
                                            plasma theophylline
                                            concentration
                                            increased gradually for
                                            2 days and
                                            reached an almost
                                            steady-state on the
                                            third day after
                                            administration (after 48
                                            hr). Range of effective
                                            blood concentration: 8-
                                            20&#956;g/mL in
                                            adults
                                            Main cytochrome P450
                                            subfamily involved in
                                            metabolism:
                                            CYP1A2.
Tachykinin NK2          ·peptide: nepadutant   -   -   ·965.025: nepadutant   ·: nepadutant
receptor antagonist···A
Tachykinin NK2
receptor antagonist. :
nepadutant

inhibition of leukotriene -                    -   -   -                      -
pathway, antioxidation
and 5-HT2b blocking




·C5a receptor          ·antibodies:            -   -   ·: neutrazumab         ·: neutrazumab
antagonist; blocks C5a neutrazumab
activity and prevent
chemotaxis. :
neutrazumab
·Lysozyme activity has ·protein: lysozyme   Among 10 healthy        -   ·14400: lysozyme   ·Soluble: lysozyme
been demonstrated to hydrochloride          adult male volunteers,      hydrochloride      hydrochloride
be effective in                             five received a 90mg
attacking the cell wall                     tablet of NEUZYM
polysaccharide of                           after fasting overnight
different bacterial                         and five served as the
species leading to                          control and received
break down of the cell                      no treatment. Upon
wall and killing the                        measuring the serum
micro-organisms.                            lysozyme
Lysozyme is most                            concentration over
effective in hydrolysing                    time by the two-site
a tetrasaccharide                           enzyme immunoassay
found most often in                         for the subjects who
Gram-positive                               received NEUZYM, the
bacteria. Model                             lysozyme
studies indicate that                       concentration peaked
Lysozyme, under                             at 1,700pg/mL within
certain conditions,                         1h and decreased to a
either alone or in                          non-detectable level by
presence of                                 48h.
potentiating
compounds, has
antibacterial activity
against the following
pathogenic organisms:
Lysteria
monocytogenes,
Clostridium botulinum,
Campylobacter jejuni,
Pseudomonas spp.,
Salmonella enteritidis
and the food spoilage
organisms: Clostridium
·Lysozyme activity has ·protein: lysozyme   Among 10 healthy        -   ·14400: lysozyme   ·Soluble: lysozyme
been demonstrated to hydrochloride          adult male volunteers,      hydrochloride      hydrochloride
be effective in                             five received a 90mg
attacking the cell wall                     tablet of NEUZYM
polysaccharide of                           after fasting overnight
different bacterial                         and five served as the
species leading to                          control and received
break down of the cell                      no treatment. Upon
wall and killing the                        measuring the serum
micro-organisms.                            lysozyme
Lysozyme is most                            concentration over
effective in hydrolysing                    time by the two-site
a tetrasaccharide                           enzyme immunoassay
found most often in                         for the subjects who
Gram-positive                               received NEUZYM, the
bacteria. Model                             lysozyme
studies indicate that                       concentration peaked
Lysozyme, under                             at 1,700pg/mL within
certain conditions,                         1h and decreased to a
either alone or in                          non-detectable level by
presence of                                 48h.
potentiating
compounds, has
antibacterial activity
against the following
pathogenic organisms:
Lysteria
monocytogenes,
Clostridium botulinum,
Campylobacter jejuni,
Pseudomonas spp.,
Salmonella enteritidis
and the food spoilage
organisms: Clostridium
·Lysozyme activity has ·protein: lysozyme   Among 10 healthy        -   ·14400: lysozyme   ·Soluble: lysozyme
been demonstrated to hydrochloride          adult male volunteers,      hydrochloride      hydrochloride
be effective in                             five received a 90mg
attacking the cell wall                     tablet of NEUZYM
polysaccharide of                           after fasting overnight
different bacterial                         and five served as
species leading to                          the control and
break down of the cell                      received no
wall and killing the                        treatment.
micro-organisms.                            Upon measuring the
Lysozyme is most                            serum lysozyme
effective in hydrolysing                    concentration over
a tetrasaccharide                           time
found most often in                         by the two-site enzyme
Gram-positive                               immunoassay for the
bacteria. Model                             subjects who
studies indicate that                       received
Lysozyme, under                             NEUZYM, the
certain conditions,                         lysozyme
either alone or in                          concentration peaked
presence of                                 at
potentiating                                1,700pg/mL within 1h
compounds, has                              and decreased to a
antibacterial activity                      non-detectable level
against the following                       by 48h.
pathogenic organisms:
Lysteria
monocytogenes,
Clostridium botulinum,
Campylobacter jejuni,
Pseudomonas spp.,
Salmonella enteritidis
and the food spoilage
organisms: Clostridium
Nitric Oxide-Enhancing small molecule       -                       -   -                  -
PDE Inhibitors
Nitric Oxide-Enhancing small molecule      -   -   -                     -
Steroids provides
faster onset of action;
increased airway
circulation
·Corticosteroid with    ·small molecule:   -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                       budesonide
activity : budesonide
·Theophylline has two ·small molecule:   Rapidly and             -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     completely absorbed                                 theophylline
airways of patients                      after oral
with reversible                          administration in
obstruction; smooth                      solution or immediate-
muscle relaxation (i.e.,                 release solid oral
bronchodilation) and                     dosage form.
suppression of the                       Undergoes extensive
response of the                          hepatic metabolism.
airways to stimuli                       CL: 0.65 mL/kg/min.
                                         t1/2: 8.7 h. 40% bound
: theophylline                           to plasma proteins. In
                                         adults, about 10% of a
                                         dose of theophylline is
                                         excreted unchanged in
                                         the urine. Vd: 0.45
                                         L/kg (range 0.3-0.7
                                         L/kg).


CRTH2 antagonist        small molecule   -                       -   -                       -

inhibits the 15-        small molecule   -                       -   -                       -
lipoxygenase enzyme
(15-LO)
PDE4 inhibitor          -                -                       -   -                       -




Dual-acting drug with   -                -                       -   -                       -
bronchodilating and
anti-inflammatory
effects
-                        -          -   -   -   -




OX40 Ligand               protein   -   -   -   -
expressed on
activated T cells
(OX40L), and on
antigen presenting
cells, are a pair of
interacting cell-surface
proteins which are
important for the
induction and
regulation of immunity.
The therapeutic
potential of these cell-
surface proteins lies in
their ability to modulate
the immune system.
Manipulation of the
immune system
through the use of
OX40 or OX40 Ligand
fusion proteins (OX40 -
lgG or OX40L-lgG) or
antibodies that bind to
OX40 Ligand or OX40




-                        protein    -   -   -   -
-   -                -   -   -   -




-   small molecule   -   -   -   -
·A selective,           ·small molecule:    When ONON® was          -   ·490.51: pranlukast   ·Practically Insoluble:
competitive antagonist pranlukast hydrate   administered orally to      hydrate               pranlukast hydrate
of the cysteinyl                            5 healthy adults after
leukotrienes (LT) C(4),                     meals at a single dose
LTD(4) and LTE(4). :                        of 225 mg, the plasma
pranlukast hydrate                          concentration reached
                                            a maximum of 642
                                            ng/mL about 5 hours
                                            after administration
                                            and decreased with a
                                            half-life of about 1.2
                                            hours.Pranlukast
                                            hydrate was mainly
                                            metabolized by a
                                            hepatic
                                            drug-metabolizing
                                            enzyme cytochrome
                                            P450 (CYP3A4).
                                            Urinary and fecal
                                            excretions were 0.24%
                                            and 98.9%,
                                            respectively.The
                                            protein binding rate to
                                            human serum was
                                            99.7 -
                                            99.8%.(Reference:
                                            Japan Label)
·A selective,           ·small molecule:    When ONON® Dry          -   ·490.51: pranlukast   ·Practically Insoluble:
competitive antagonist pranlukast hydrate   Syrup was                   hydrate               pranlukast hydrate
of the cysteinyl                            administered orally to
leukotrienes (LT) C(4),                     6 healthy adults after
LTD(4) and LTE(4). :                        meals at a single dose
pranlukast hydrate                          of 2.25g (containing
                                            225 mg of pranlukast
                                            hydrate), the plasma
                                            concentration reached
                                            a maximum of 859
                                            ng/mL about 5 hours
                                            after administration
                                            and decreased with a
                                            half-life of about 1.5
                                            hours. AUC was 3,487
                                            ng&#8901;hr/mL.Pranl
                                            ukast hydrate was
                                            mainly metabolized by
                                            a hepatic drug-
                                            metabolizing enzyme
                                            cytochrome P450
                                            (CYP3A4). Urinary and
                                            fecal excretion were
                                            0.24% and 98.9%,
                                            respectively.The
                                            protein-binding rate to
                                            human serum was
                                            99.7 -
                                            99.8%.(Reference:
                                            Japan Label)




-                      -                    -                       -   -                     -
·Prednisolone is a       ·small molecule:      Well absorbed.       -   ·484.39: prednisolone   ·Freely Soluble:
corticosteroid with      prednisolone sodium   Solution produces        sodium phosphate        prednisolone sodium
mainly glucocorticoid    phosphate             14% higher Cmax and                              phosphate
activity: prednisolone                         20% faster Tmax than
sodium phosphate                               tablets.
·Prednisolone is a       ·small molecule:      Prednisolone is rapidly -   ·484.39: prednisolone   ·Freely Soluble:
corticosteroid with      prednisolone sodium   and well absorbed           sodium phosphate        prednisolone sodium
mainly glucocorticoid    phosphate             from the GI tract                                   phosphate
activity: prednisolone                         following oral
sodium phosphate                               administration. Under
                                               fasted conditions,
                                               Orapred ODT is
                                               bioequivalent to
                                               Orapred Solution




·New generation         ·small molecule:       -                       -   ·540.69: ciclesonide    ·Practically Insoluble:
inhaled corticosteroid ciclesonide                                                                 ciclesonide
with novel
pharmacokinetic
properties: ciclesonide
G-protein coupled      -                     -                     -   -                    -
receptors.


·Long-acting beta(2)   ·small molecule:      Rapidly absorbed with -   ·804.9: formoterol   ·Slightly Soluble:
agonist: formoterol    formoterol fumarate   Tmax is 15 min. 28-       fumarate             formoterol fumarate
fumarate                                     49% of drug is
                                             delivered to lung.
                                             Total systemic BA is
                                             61%. Plasma protein
                                             binding is 50%. t1/2 is
                                             8 hrs (estimated).




PAC-G31P is a           peptide              -                     -   -                    -
selective antagonist of
interleukin-8 (IL-8)
binding to CXCR1 and
CXCR2 receptors
-                      -                     -                     -   -                    -
-                       -                  -   -   -                     -




Long-Acting Beta 2      small molecule     -   -   -                     -
Agonist
PI3 Kinase inhibitor    small molecule     -   -   -                     -


·Cytosolic              ·small molecule:   -   -   ·745.25: giripladib   ·: giripladib
phospholipase A2        giripladib
inhibitor: giripladib




Serine protease         small molecule     -   -   -                     -
inhibitors
·Albuterol sulfate, the   ·small molecule:    The systemic levels of -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   albuterol are low after    sulfate              albuterol sulfate
albuterol and a                               inhalation of
relatively selective                          recommended
beta 2 -adrenergic                            doses.
bronchodilator:                               Cmax and systemic
albuterol sulfate                             exposure (AUCinf)
                                              values are
                                              approximately 4,100
                                              pg/mL and 28,426
                                                 h
                                              pg• r/mL, respectively
                                              compared to
                                              approximately 3,900
                                              pg/mL and 28,395
                                                 h
                                              pg• r/mL,
                                              respectively following
                                              the same dose of an
                                              active HFA-134a
                                              albuterol inhaler
                                              comparator. The
                                              terminal plasma t1/2 of
                                              albuterol delivered by
                                              ProAir HFA
                                              Inhalation Aerosol was
                                              approximately 6 hrs.
                                              The primary enzyme
                                              responsible for the
                                              metabolism of
                                              albuterol in humans is
                                              SULTIA3
                                              (sulfotransferase). (R)-
                                              albuterol is
                                              preferentially
                                              metabolized in the
The mode of action of protein           -   -   -   -
the Anticalin®
candidate is via
modulation of the site
of binding for multiple
ligands
CXCR2 antagonist       small molecule   -   -   -   -




A vascular cell        small molecule   -   -   -   -
adhesion molecule
(VCAM) antagonist
-                      small molecule   -   -   -   -




Inhibits immune cell   small molecule   -   -   -   -
trafficking


Targets SSAO/VAP-1 -                    -   -   -   -
protein (2008 company
report page 7)
-                        small molecule     -                      -   -                     -




-                        -                  -                      -   -                     -
H4 (Histamine 4)         -                  -                      -   -                     -
Antagonists

·Aminophylline, a        ·small molecule:   Aminophylline          -   ·456: aminophylline   ·Freely Soluble:
complex of               aminophylline      (theophylline) is well     dihydrate             aminophylline
theophylline with        dihydrate          absorbed and at least                            dihydrate
ethylenediamine,                            60% may be bound to
readily liberates                           plasma proteins. The
theophylline in the                         main urinary
body. Aminophylline                         metabolites are 1,3
has the actions and                         dimethyl uric acid and
uses of theophylline :                      3-methylxanthine.
aminophylline                               About 10% is excreted
dihydrate                                   unchanged.
·Aminophylline, a        ·small molecule:   Aminophylline          -   ·456: aminophylline   ·Freely Soluble:
complex of               aminophylline      (theophylline) is well     dihydrate             aminophylline
theophylline with        dihydrate          absorbed and at least                            dihydrate
ethylenediamine,                            60% may be bound to
readily liberates                           plasma proteins. The
theophylline in the                         main urinary
body. Aminophylline                         metabolites are 1,3
has the actions and                         dimethyl uric acid and
uses of theophylline :                      3-methylxanthine.
aminophylline                               About 10% is excreted
dihydrate                                   unchanged.
·Aminophylline, a        ·small molecule:   Aminophylline           -   ·456: aminophylline   ·Freely Soluble:
complex of               aminophylline      (theophylline) is well      dihydrate             aminophylline
theophylline with        dihydrate          absorbed from                                     dihydrate
ethylenediamine,                            PHYLLOCONTIN
readily liberates                           CONTINUS tablets
theophylline in the                         and at least 60% may
body. Aminophylline                         be bound to plasma
has the actions and                         proteins. The main
uses of theophylline :                      urinary metabolites are
aminophylline                               1,3 dimethyl uric acid
dihydrate                                   and 3-methylxanthine.
                                            About 10% is excreted
                                            unchanged.




Phylomer® drugs          -                  -                       -   -                     -
target Toll-like
Receptors and other
inflammatory
associated pathways.

Undisclosed              small molecule     -                       -   -                     -
an orally active, broad- ·small molecule:   Preclinical studies       -   ·381.4: pleconaril   ·: pleconaril
spectrum                   pleconaril       have demonstrated
antipicornaviral agent                      that the bioavailability
which demonstrates                          of pleconaril in a solid-
excellent penetration                       dose form is increased
into the central                            approximately
nervous system, liver,                      sevenfold in the
and nasal                                   presence of food
epithelium···Pleconaril                     compared to under
is an orally active                         fasting conditions.
broad-spectrum                              Inadults at 2.86 mg/k
antiviral agent.                            dose CL/F = 0.34 ±
Pleconaril, like similar                    0.12 liters/kg and
[(oxazolylphenoxy)alkyl                     VSS/F = 3.2 ± 2.0
]isoxazole compounds,                       liters/kg, the mean
inhibits viral replication                  elimination half-life of
at the site of viral                        pleconaril is 5.7 h. Its
attachment and                              oral bioavailability is
uncoating. These                            approximately 70%
hydrophobic                                 when administered in
compounds insert                            a fed state. (REF 1-
themselves into a                           (Pubmed id:9756781))
pocket beneath the
canyon site on the
icosahedral face of the
virion, raising the floor
of the canyon and thus
altering the ability of
the virus to attach to
the cellular receptor.
Additionally, these
agents increase the
stability of the viral
capsid to receptor and
·A synthetic form of       ·small molecule:   -   -   ·1355.38:        ·Sparingly Soluble:
vitamin B12 with           cyanocobalamin             cyanocobalamin   cyanocobalamin
equivalent vitamin B12
activity. Vitamin B12 is
essential to growth,
cell reproduction,
hematopoiesis, and
nucleoprotein and
myelin synthesis.
Cells
characterized by rapid
division (e.g., epithelial
cells, bone marrow,
myeloid cells) appear
to have the greatest
requirement for vitamin
B12. Cyanocobalamin
is the most stable and
widely used form of
vitamin B12, and has
hematopoietic activity
apparently identical to
that of the antianemia
factor in purified liver
extract.:
cyanocobalamin
·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol    ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate               albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate




·Corticosteroid with      ·small molecule:    -   -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid     budesonide                                        budesonide
activity : budesonide
·Although its precise    ·small molecule:      -   -   ·512.333: sodium   ·Soluble: sodium
mode of action           sodium cromoglycate           cromoglycate       cromoglycate
remains uncertain,
sodium cromoglycate
is believed to act
primarily by preventing
release of mediators of
inflammation from
sensitised mast cells
through stabilisation of
mast-cell membranes.
: sodium cromoglycate
·Most potent stimulant ·small molecule:   -   -   ·183.204: epinephrine ·Very Slightly Soluble:
(sympathomimetic) of epinephrine                                        epinephrine
adrenergic alpha and
beta-receptors,
resulting in increased
heart rate and force of
contraction,
vasoconstriction or
vasodilation, relaxation
of bronchiolar and
intestinal smooth
muscle: epinephrine
·Albuterol sulfate, the   ·small molecule:    -                        -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate                                sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate




·Histamine H1 receptor ·small molecule:       Bioavailability is about -   ·425.5: ketotifen    ·Sparingly Soluble:
antagonist: ketotifen  ketotifen fumarate     50% due to a first-pass      fumarate             ketotifen fumarate
fumarate                                      effect of about 50% in
                                              the liver and its
                                              bioavailability is not
                                              influenced by food
                                              intake. Maximal
                                              plasma concentration
                                              reaches within 2-4
                                              hours. Plasma protein
                                              binding is 75%.
                                              Ketotifen is eliminated
                                              biphasically with a
                                              short half-life of 3 - 5
                                              hours and a longer
                                              one of 21 hours. About
                                              60 % - 70 % of the
                                              administered dose is
                                              excreted as
                                              metabolites and 1 % is
                                              excreted unchanged in
                                              the urine.
Synairgen is using      -                     -   -   -                    -
proteomic approaches
to perform protein
expression profiling on
epithelial secretions
obtained from tissue
models using clinical
samples obtained from
donors without or with
asthma.



·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate
·Albuterol sulfate, the   ·small molecule:    Salbutamol is readily -     ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   absorbed from the GI        sulfate              albuterol sulfate
albuterol and a                               tract. It is subject to
relatively selective                          first-pass metabolism
beta 2 -adrenergic                            in the liver and
bronchodilator:                               possibly in the gut wall;
albuterol sulfate                             the main metabolite is
                                              an inactive sulfate
                                              conjugate. Salbutamol
                                              is rapidly excreted in
                                              the urine as
                                              metabolites and
                                              unchanged drug; there
                                              is some excretion in
                                              the faeces. Salbutamol
                                              does not appear to be
                                              metabolised in the
                                              lung, therefore its
                                              ultimate metabolism
                                              and excretion following
                                              inhalation depends
                                              upon the delivery
                                              method used, which
                                              determines the
                                              proportion of inhaled
                                              salbutamol relative to
                                              the proportion
                                              inadvertently
                                              swallowed. It has been
                                              suggested that the
                                              majority of an inhaled
                                              dose is swallowed and
                                              absorbed from the gut.
·Corticosteroid with    ·small molecule:   -                        -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                                            budesonide
activity : budesonide




·Corticosteroid with    ·small molecule:   The metabolism of        -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide         budesonide is primarily                            budesonide
activity : budesonide                      mediated by CYP3A4,
                                           one of the cytochrome
                                           p450 enzymes.
                                           Systemic availability
                                           after inhalation is 70%.
                                           t1/2 is 2 hrs.
·Corticosteroid with    ·small molecule:   Tmax is 10-30 min and -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide         Cmax is 2.6 nmol/L,                             budesonide
activity : budesonide                      BA is 6%. Extensive
                                           first pass liver
                                           metabolism. Terminal
                                           t1/2 is 2.3 hrs and CL
                                           is 0.5 L/min.




·Corticosteroid with    ·small molecule:   -                     -   ·430.53: budesonide   ·Practically Insoluble:
mainly glucocorticoid   budesonide                                                         budesonide
activity : budesonide
·Corticosteroid with    ·small molecule:    Tmax is 1-2 hrs and    -   ·430.53: budesonide    ·Practically Insoluble:
mainly glucocorticoid   budesonide          34% of dose deposited                             budesonide
activity : budesonide                       in lungs. BA is 39%.
                                            Extensive first pass
                                            liver metabolism. t1/2
                                            is 2-3 hrs.




·Beta agonist: albuterol ·small molecule:   -                      -   ·239.213: albuterol    ·Sparingly Soluble:
                         albuterol                                                            albuterol




·A long-acting beta2-   ·small molecule:    -                      -   ·392.49: indacaterol   ·: indacaterol
agonist: indacaterol    indacaterol




Glucocorticosteroid     -                   -                      -   -                      -
CCR3 antagonist         -                   -                      -   -                      -
TLR9 agonists are       oligonucleotide        -   -   -                      -
strong inducers of Th1-
type cytokines, and
animal models of
allergic asthma show
that IMO™ compounds
discovered by Idera
reversed the
imbalance of Th2
activity and improved
lung function.
·A long-acting beta2-     ·small molecule:     -   -   ·392.49:               ·:
agonist:                  indacaterol·small            indacaterol·521.429:   indacaterol·Practically
indacaterol·The           molecule:                    mometasone furoate     Insoluble:
precise mechanism of      mometasone furoate                                  mometasone furoate
corticosteroid action
on allergic rhinitis is
not known.
Corticosteroids have
been shown to have a
wide range of effects
on multiple cell types
(e.g., mast cells,
eosinophils,
neutrophils,
macrophages, and
lymphocytes) and
mediators (e.g.,
histamine,
eicosanoids,
leukotrienes, and
cytokines) involved in
inflammation.
: mometasone furoate
·Corticosteroid with    ·small molecule:   -   -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone             beclomethasone   beclomethasone
activity:               dipropionate               dipropionate     dipropionate
beclomethasone
dipropionate




·Corticosteroid with    ·small molecule:   -   -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone             beclomethasone   beclomethasone
activity:               dipropionate               dipropionate     dipropionate
beclomethasone
dipropionate
·Corticosteroid with    ·small molecule:   -                     -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone                               beclomethasone   beclomethasone
activity:               dipropionate                                 dipropionate     dipropionate
beclomethasone
dipropionate




·Corticosteroid with    ·small molecule:   Tmax is 30 min. Three -   ·521.04:         ·Practically Insoluble:
mainly glucocorticoid   beclomethasone     major metabolites are     beclomethasone   beclomethasone
activity:               dipropionate       formed via cytochrome     dipropionate     dipropionate
beclomethasone                             P450 3A catalyzed
dipropionate                               biotransformation. The
                                           mean t1/2 of 17-BMP
                                           is 2.8 hrs.
-                      antibodies         -   -   -   -




Syk kinase inhibitor     small molecule   -   -   -   -
that is designed to bind
to syk in mast cells
and interrupt the
signal from the IgE
receptor, thus
preventing cellular
activation and
subsequent chemical
mediator release, and
potentially blocking an
allergic
response in allergic
asthma.
·A selective integrin  ·small molecule:       After 100 mg IV         -   ·641.4: valategrast   ·: valategrast
receptor antagonist.   valategrast            infusion of RO0270608       hydrochloride         hydrochloride
This drug acts through hydrochloride          (active metabolite of
a non-steroidal                               R411) , CL (mean +/-
mechanism, blocking                           standard deviation)
VLA-4 integrin                                was 19.4 +/- 7.1 L/h,
receptor sites:                               and the Vd was 93.1 +/-
valategrast                                   36.1 L. [Ref 1 -
hydrochloride                                 (Pubmed
                                              id:15545307)]


Anti-CD134/OX40.         antibodies           -                       -   -                     -
Antibody which
selectively blocks the
interaction of the OX40
ligand and its receptor.
[29913]
·Albuterol sulfate, the   ·small molecule:    -                       -   ·548.24: albuterol    ·Freely Soluble:
racemic form of           albuterol sulfate                               sulfate               albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate
·Anti-inflammatory and ·small molecule:   The blood tranilast     -   ·327.33: tranilast   ·Practically Insoluble:
anti-angiogenic agent. tranilast          concentration peaked                             tranilast
Exerts its effects by                     2
inhibiting the                            hours after
expression of                             administration, and
mediators such as                         was below one-tenth of
MCP-1, TGF-&#946;,                        the maximal blood
TNF-&#945; induced                        concentration after 24
vascular cell adhesion                    hours. The half-life of
molecule-1 (VCAM-1),                      the blood
intracellular adhesion                    concentration was
molecule-1 (ICAM-1)                       about 5 hours. The
and E-selectin. It also                   urinary excretion ratio
inhibits antigen-                         during the first 96
specific T cell                           hours was
proliferation, skews a                    37.7%, and 28.8% was
TH1-type T cell                           excreted within 24
response to TH2 and                       hours. 100 mg oral
suppresses the                            administration, C max
activation of antigen                     (&#956;g/mL) is 12.6,
presenting cells by                       AUC (&#956;g hr/mL)
interfering with signal                   is 114.4.
transducer and
activator of
transcription (STAT)
pathways.: tranilast
·Anti-inflammatory and ·small molecule:   The blood tranilast     -   ·327.33: tranilast   ·Practically Insoluble:
anti-angiogenic agent. tranilast          concentration peaked                             tranilast
Exerts its effects by                     2
inhibiting the                            hours after
expression of                             administration, and
mediators such as                         was below one-tenth of
MCP-1, TGF-&#946;,                        the maximal blood
TNF-&#945; induced                        concentration after 24
vascular cell adhesion                    hours. The half-life of
molecule-1 (VCAM-1),                      the blood
intracellular adhesion                    concentration was
molecule-1 (ICAM-1)                       about 5 hours. The
and E-selectin. It also                   urinary excretion ratio
inhibits antigen-                         during the first 96
specific T cell                           hours was
proliferation, skews a                    37.7%, and 28.8% was
TH1-type T cell                           excreted within 24
response to TH2 and                       hours. 100 mg oral
suppresses the                            administration, C
activation of antigen                     max
presenting cells by                       (&#956;g/mL) is 12.6,
interfering with signal                   AUC (&#956;g hr/mL)
transducer and                            is 114.4.
activator of
transcription (STAT)
pathways.: tranilast



Novel long acting      small molecule     -                       -   -                    -
inhibitor of both
phosphodiesterase 3
and
phosphodiesterase 4
enzymes
Resolvins are anti-   small molecule        -   -   -                -
inflammatory lipid
mediators generated
through the oxidation
of the omega-3 fatty
acids
eicosapentaenoic acid
(EPA) and
docosahexaenoic acid
(DHA).
(Pubmed id:15890784)


·Racepinephrine is a     ·small molecule:   -   -   ·183.204:        ·Very Slightly Soluble:
racemic mixture of the racepinephrine               racepinephrine   racepinephrine
enantiomorphs of
epinephrine and refers
to the mixture of 'd'
and 'l' isomers of
epinephrine in equal
parts. Epinephrine is a
potent stimulant
(sympathomimetic) of
adrenergic alpha and
beta-receptors,
resulting in increased
heart rate and force of
contraction,
vasoconstriction or
vasodilation, relaxation
of bronchiolar and
intestinal smooth
muscle.:
racepinephrine
Reslizumab is a          ·antibodies: reslizumab -   -   ·: reslizumab          ·: reslizumab
humanized mAb
against IL-
5···treatment of
bronchial asthma as
well as a
pharmacological tool
to elucidate the role of
IL-5 in human
eosinophilic
diseases
: reslizumab
·Anti-inflammatory      ·small molecule:        -    -   ·485.401: etiprednol   ·: etiprednol
corticosteroid.:        etiprednol dicloacetate          dicloacetate           dicloacetate
etiprednol dicloacetate

-                       -                        -   -   -                      -
·Ipratropium bromide is ·small molecule:      Ipratoprium bromide is -   ·430.38: ipratropium   ·Freely Soluble:
an anticholinergic      ipratropium bromide   a quaternary               bromide hydrate        ipratropium bromide
(parasympatholytic)     hydrate               ammonium compound                                 hydrate
agent which, based on                         which is poorly
animal studies,                               absorbed from the
appears to inhibit                            gastro-intestinal tract,
vagally mediated                              and is slow to cross
reflexes by                                   mucous membranes
antagonizing the action                       and the blood/brain
of acetylcholine, the                         barrier. Following,
transmitter agent                             inhalation, uptake into
released from the                             the plasma is minimal,
vagus nerve.                                  a peak blood
Anticholinergics                              concentration is
prevent the increases                         obtained 1½ to 3 hours
in intracellular                              after inhalation.
concentration of cyclic                       Excretion is chiefly via
guanosine                                     the kidneys.
monophosphate (cyclic
GMP) which are
caused by interaction
of acetylcholine with
the muscarinic
receptor on bronchial
smooth muscle.:
ipratropium bromide
hydrate



Recombinant Alpha 1- protein                  -                      -   -                      -
antitrypsin (rAAT)
·Anti-inflammatory and ·small molecule:      -   -   ·327.33: tranilast   ·Practically Insoluble:
anti-angiogenic agent. tranilast                                          tranilast
Exerts its effects by
inhibiting the
expression of
mediators such as
MCP-1, TGF-&#946;,
TNF-&#945; induced
vascular cell adhesion
molecule-1 (VCAM-1),
intracellular adhesion
molecule-1 (ICAM-1)
and E-selectin. It also
inhibits antigen-
specific T cell
proliferation, skews a
TH1-type T cell
response to TH2 and
suppresses the
activation of antigen
presenting cells by
interfering with signal
transducer and
activator of
transcription (STAT)
pathways.: tranilast



·Anti-allergic drug       ·small molecule:   -   -   ·355.4: repirinast   ·: repirinast
which inhibits chemical   repirinast
mediator release:
repirinast
·Anti-allergic drug       ·small molecule:   -   -   ·355.4: repirinast   ·: repirinast
which inhibits chemical   repirinast
mediator release:
repirinast
·Prostaglandin D2       ·small molecule: S-    -   -   ·: S-5751              ·: S-5751
receptor antagonist: S- 5751
5751
Cr Th2 antagonist       -                      -   -   -                      -

A3A antagonist          -                      -   -   -                      -

TRL9 agonist            -                      -   -   -                      -

DP1 antagonist          -                      -   -   -                      -

·Interferons are a      ·protein: interferon   -   -   ·20025.1: interferon   ·: interferon beta
family of naturally     beta                           beta
occurring proteins that
are produced by
eukaryotic cells in
response to viral
infection and other
biological inducers.:
interferon beta
·Interferons are a      ·protein: interferon   -   -   ·20025.1: interferon   ·: interferon beta
family of naturally     beta                           beta
occurring proteins that
are produced by
eukaryotic cells in
response to viral
infection and other
biological inducers.:
interferon beta
-                       -                      -   -   -                      -
-                       -                      -   -   -                      -

-                       -                      -   -   -                      -
-                       -                      -   -   -                      -
It suppresses         -                        -   -   -                      -
inflammatory mediator
release/production

·Interferons are a      ·protein: interferon   -   -   ·20025.1: interferon   ·: interferon beta
family of naturally     beta                           beta
occurring proteins that
are produced by
eukaryotic cells in
response to viral
infection and other
biological inducers.:
interferon beta
reorganises and re-     protein                -   -   -                      -
establishes the barrier
without promoting
unwanted structural
changes
in the lung
The Company has         -                      -   -   -                      -
isolated a novel
molecule from
Mycobacterium vaccae
that is potently active
in a pre-clinical model
of asthma. SRP312 is
a A synthetic version
of this molecule.


Adenosine A3            small molecule         -   -   -                      -
antagonist

Soft corticosteroid.    small molecule         -   -   -                      -
Glucocorticoid
receptor agonist.
·Beta agonist: albuterol ·small molecule:   Salbutamol is readily      -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          absorbed from the                                    albuterol
                                            gastro-intestinal tract.
                                            It is subject to
                                            first pass metabolism
                                            in the liver. The
                                            plasma t1/2 has been
                                            estimated to range
                                            from about 2 - 7 hrs.




·Beta agonist: albuterol ·small molecule:   -                          -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol                                                               albuterol
·Beta agonist: albuterol ·small molecule:   -   -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol                                        albuterol




·Beta agonist: albuterol ·small molecule:   -   -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol                                        albuterol




·Beta agonist: albuterol ·small molecule:   -   -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol                                        albuterol
·Beta agonist: albuterol ·small molecule:   Readily absorbed from -    ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          the gastrointestinal                             albuterol
                                            tract. T1/2: 4-6 hours.
                                            It is subject to first-
                                            pass metabolism in the
                                            liver and possibly in
                                            the gut wall.




·Beta agonist: albuterol ·small molecule:   Lung deposition is     -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          24% of metered dose                              albuterol
                                            with high inhalation
                                            rate and 10% with a
                                            low rate. Peak serum
                                            of Taifun are 20-90%
                                            greater than Ventolin
                                            comparator.
                                            Undergoes extensive
                                            first pass metabolism.
                                            t1/2 is 3-7 hrs.
Small molecule          ·small molecule:   After 50 mg, 100 mg, -    ·323.3: senicapoc      ·: senicapoc
inhibitor of the KCa3.1 senicapoc          and 150 mg given to
potassium ion                              different patient
channel···Senicapoc is                     groups, overall mean
an inhibitor of the                        t1/2 was determined to
Gardos calcium-                            be 12.8 days. Mean
activated potassium                        peak plasma
channel. It is expected                    concentrations rose
to inhibit RBC                             between the 50- and
dehydration and thus                       100-mg dose levels
should prevent or                          but plateaued at 150
delay the sickling                         mg (59.1, 108.7, and
process. By reducing                       109.1 ng/ml,
sickled cells, an                          respectively). The rate
improvement in                             of absorption,
anemia, a reduction in                     however, appeared to
painful crises, and                        be delayed at doses
ultimately, less end-                      greater than 100 mg.
organ disease is                           [Ref 1- (Pubmed
anticipated. :                             id:17064199)]
senicapoc


·New generation         ·small molecule:   -                     -   ·540.69: ciclesonide   ·Practically Insoluble:
inhaled corticosteroid ciclesonide                                                          ciclesonide
with novel
pharmacokinetic
properties: ciclesonide
·A long-acting beta 2 -    ·small molecule:        Salmeterol produces -      ·603.7: salmeterol     ·Sparingly Soluble:
adrenergic agonist:        salmeterol              12 hrs of                  xinafoate·500.57:      salmeterol
salmeterol                 xinafoate·small         bronchodilation.           fluticasone propionate xinafoate·Practically
xinafoate·Corticosteroi    molecule: fluticasone   Salmeterol acts locally                           Insoluble: fluticasone
d with mainly              propionate              in the lung therefore                             propionate
glucocorticoid activity.                           plasma levels are
It has weak affinity for                           low
the progesterone                                   The absolute BA of
receptor, and virtually                            inhaled fluticasone
no affinity for the                                propionate in healthy
mineralocorticoid,                                 subjects varies
estrogen, or androgen                              between approximately
receptors.: fluticasone                            10-30% of the nominal
propionate                                         dose depending on the
                                                   inhalation device used.
                                                   Plasma protein binding
                                                   is 91%. Terminal t1/2
                                                   is about 8 hrs. The
                                                   main pathway is
                                                   metabolism to an
                                                   inactive carboxylic acid
                                                   metabolite, by the
                                                   cytochrome P450
                                                   enzyme CYP3A4.
·A long-acting beta 2 - ·small molecule:       Salmeterol acts locally -   ·603.7: salmeterol   ·Sparingly Soluble:
adrenergic agonist:     salmeterol xinafoate   in the lung, therefore      xinafoate            salmeterol xinafoate
salmeterol xinafoate                           plasma levels are not
                                               predictive of
                                               therapeutic effect. In
                                               addition there are only
                                               limited data available
                                               on the
                                               pharmacokinetics of
                                               salmeterol because of
                                               the technical difficulty
                                               of assaying the drug in
                                               plasma because of the
                                               very low plasma
                                               concentrations
                                               (approximately 200
                                               pg/ml or less)
                                               achieved after inhaled
                                               dosing. After regular
                                               dosing with salmeterol
                                               xinafoate, xinafoic acid
                                               can be detected in the
                                               systemic circulation,
                                               reaching steady state
                                               concentrations of
                                               approximately 100
                                               ng/ml. These
                                               concentrations are up
                                               to 1000-fold lower than
                                               steady state levels
                                               observed in toxicity
                                               studies. These
                                               concentrations in long
                                               term regular dosing
·A long-acting beta 2 - ·small molecule:       Cmax of 167 pg/mL is -      ·603.7: salmeterol   ·Sparingly Soluble:
adrenergic agonist:     salmeterol xinafoate   reached at 20 min.          xinafoate            salmeterol xinafoate
salmeterol xinafoate                           Plasma protein binding
                                               is 96%. Drug detected
                                               in plasma in 5-45
                                               minutes. t1/2 is 5.5
                                               hrs.




·A long-acting beta 2 - ·small molecule:       Salmeterol acts locally -   ·603.7: salmeterol   ·Sparingly Soluble:
adrenergic agonist:     salmeterol xinafoate   in the lung therefore       xinafoate            salmeterol xinafoate
salmeterol xinafoate                           plasma levels are not
                                               an indication of
                                               therapeutic effects. In
                                               addition there are only
                                               limited data available
                                               on the
                                               pharmacokinetics of
                                               salmeterol because of
                                               the technical difficulty
                                               of assaying the active
                                               substance in plasma
                                               due to the low plasma
                                               concentrations at
                                               therapeutic doses
                                               (approximately 200
                                               picogram/ml or less)
                                               achieved after inhaled
                                               dosing.
·A long-acting beta 2 - ·small molecule:       Salmeterol acts locally -   ·603.7: salmeterol   ·Sparingly Soluble:
adrenergic agonist:     salmeterol xinafoate   in the lung. Binding of     xinafoate            salmeterol xinafoate
salmeterol xinafoate                           salmeterol to human
                                               plasma proteins
                                               averages 96%.
                                               Salmeterol base is
                                               extensively
                                               metabolized by
                                               hydroxylation, with
                                               subsequent elimination
                                               predominantly in the
                                               feces. The terminal
                                               elimination t1/2 is
                                               about 5.5 hrs.
·A human monoclonal ·antibodies:   Following               -   ·146943: golimumab   ·: golimumab
antibody that binds to golimumab   subcutaneous (SC)
both the soluble and               administration of
transmembrane                      SIMPONI to healthy
bioactive forms of                 subjects and patients
human TNF?.:                       with active R.A, T max
golimumab                          ranged from 2 to 6
                                   days and Cmax
                                   approximately 2.5
                                   g/mL. Following a
                                   single IV
                                   administration ovèr the
                                   same dose range in
                                   patients with activeRA,
                                   mean systemic
                                   clearance of SIMPONI
                                   was estimated to be
                                   4.9 to 6.7 mL/day/kg,
                                   and mean volume of
                                   distrbution Vd ranged
                                   from 58 to 126
                                   mL/kg.
                                   Median terminal half-
                                   life values were
                                   estimated to be
                                   approximately 2 weeks
                                   inhealthy subjects
                                   and
                                   patients with active
                                   RA,PsA or AS. By
                                   cross-study
                                   comparisons of mean
                                   AUCinfvalues following
                                   an
·Inhibits              ·small molecule:     Rapidly absorbed        -   ·608.18: montelukast   ·Freely Soluble:
bronchoconstriction    montelukast sodium   orally. Tmax is 2 - 2.5     sodium                 montelukast sodium
due to antigen                              h in the fasted state.
challenge. Montelukast                      The mean oral BA is
is a selective                              73% in the fasted state
leukotriene receptor                        versus 63% when
antagonist of the                           administered with a
cysteinyl leukotriene                       standard meal in the
CysLT 1 receptor.:                          morning. Extensively
montelukast sodium                          metabolized in the
                                            liver. 99% bound to
                                            plasma proteins. Vd is
                                            8 - 11L. t1/2 is 2.7 -
                                            5.5 h.
·Inhibits              ·small molecule:     Montelukast is rapidly -   ·608.18: montelukast   ·Freely Soluble:
bronchoconstriction    montelukast sodium   absorbed following oral    sodium                 montelukast sodium
due to antigen                              administration. The 4-
challenge. Montelukast                      mg oral granule
is a selective                              formulation is
leukotriene receptor                        bioequivalent to the 4-
antagonist of the                           mg chewable tablet
cysteinyl leukotriene                       when administered to
CysLT 1 receptor.:                          adults in the fasted
montelukast sodium                          state. A high fat meal
                                            in the morning
                                            did not affect the AUC
                                            of montelukast oral
                                            granules; however, the
                                            meal decreased Cmax
                                            by 35% and prolonged
                                            Tmax from 2.3 ± 1.0
                                            hours to 6.4 ± 2.9
                                            hours. Montelukast is
                                            more than 99% bound
                                            to plasma proteins.
                                            The steady state Vd
                                            averages 8 to 11 liters.
                                            Cytochromes P450
                                            3A4 and 2C9 are
                                            involved in the
                                            metabolism.The
                                            plasma clearance of
                                            montelukast averages
                                            45 mL/min. Following
                                            an oral dose of
                                            radiolabeled
                                            montelukast, 86% of
                                            the radioactivity was
·Inhibits              ·small molecule:     Rapidly absorbed         -   ·608.18: montelukast   ·Freely Soluble:
bronchoconstriction    montelukast sodium   orally. Oral BA: 64%.        sodium                 montelukast sodium
due to antigen                              After administration of
challenge. Montelukast                      the 10-mg film-coated
is a selective                              tablet to fasted adults,
leukotriene receptor                        Cmax is achieved in 3
antagonist of the                           to 4 hours (Tmax).
cysteinyl leukotriene                       99% bound to plasma
CysLT 1 receptor.:                          proteins. Vd: 8 to 11
montelukast sodium                          liters. Extensively
                                            metabolized in the
                                            liver. t1/2: 2.7 to 5.5
                                            hours. The mean oral
                                            BA is 73% in the
                                            fasted state versus
                                            63% when
                                            administered with a
                                            standard meal in the
                                            morning.



siRNA based product siRNA                   -                        -   -                      -
targeting key cytokines
that play a critical role
in inflammation and
bronchconstriction.
·As a benzopyrano-       ·small molecule:   -   -   ·298.3: amlexanox   ·: amlexanox
bipyridine carboxylic    amlexanox
acid derivative,
amlexanox has anti-
inflammatory and
antiallergic properties.
It inhibits chemical
mediatory release of
the slow-reacting
substance of
anaphylaxis (SRS-A)
and may have
antagonistic effects on
interleukin-3.:
amlexanox
·Tiotropium bromide is ·small molecule:      Following inhalation of -   ·490.4: tiotropium  ·Sparingly Soluble:
a new long-acting       tiotropium bromide   the solution by young       bromide monohydrate tiotropium bromide
inhaled anticholinergic monohydrate          healthy volunteers,                             monohydrate
agent: tiotropium                            urinary excretion data
bromide monohydrate                          suggest that
                                             approximately 33% of
                                             the inhaled dose reach
                                             the systemic
                                             circulation. At steady
                                             state, tiotropium
                                             bromide plasma levels
                                             in COPD patients at
                                             peak were 10.5-11.7
                                             pg/ml when measured
                                             10 minutes after
                                             administration of a 5
                                             microgram dose
                                             delivered by the
                                             Respimat inhaler and
                                             decreased rapidly in a
                                             multi-compartmental
                                             manner. Steady state
                                             trough plasma
                                             concentrations were
                                             1.49-1.68 pg/ml. Food
                                             is not expected to
                                             influence the
                                             absorption of this
                                             quaternary ammonium
                                             compound.The drug is
                                             bound by 72% to
                                             plasma proteins.
                                             Tiotropium is excreted
                                             largely unchanged in
·Tiotropium bromide is ·small molecule:      Tiotropium bromide is -   ·490.4: tiotropium  ·Sparingly Soluble:
a new long-acting       tiotropium bromide   absorbed from the         bromide monohydrate tiotropium bromide
inhaled anticholinergic monohydrate          lung, with a systemic                         monohydrate
agent: tiotropium                            BA of about 20%
bromide monohydrate                          reported. It is about
                                             72% bound to plasma
                                             proteins. Tiotropium is
                                             excreted largely
                                             unchanged in the
                                             urine, although it may
                                             undergo some
                                             metabolism by non-
                                             enzymatic cleavage
                                             and by the cytochrome
                                             P450 isoenzymes
                                             CYP2D6 and CYP3A4.
                                             Tiotropium shows a Vd
                                             of 32 L/kg indicating
                                             that the drug binds
                                             extensively
                                             to tissues. The
                                             terminal t1/2 is 5 - 6
                                             days and total CL is
                                             880 mL/min
·A direct-acting        ·small molecule:   -   -   ·313.7: clenbuterol   ·Soluble: clenbuterol
sympathomimetic with clenbuterol                   hydrochloride         hydrochloride
predominantly beta-     hydrochloride
adrenergic activity and
a selective action on
beta2 receptors (a
beta2 agonist).:
clenbuterol
hydrochloride
·Corticosteroid with    ·small molecule:       Orally inhaled          -   ·430.53:              ·Practically Insoluble:
mainly glucocorticoid   budesonide·small       budesonide is rapidly       budesonide·840.9:     budesonide·Slightly
activity :              molecule: formoterol   absorbed in the lung        formoterol fumarate   Soluble: formoterol
budesonide·Selective    fumarate dihydrate     and peak                    dihydrate             fumarate dihydrate
beta-2-agonist:                                concentrations are
formoterol fumarate                            reached within 20
dihydrate                                      minutes. Orally
                                               inhaled formoterol is
                                               rapidly absorbed in the
                                               lung and peak
                                               concentrations are
                                               reached within 5-10
                                               minutes.
·Corticosteroid with   ·small molecule:       Budesonide is rapidly -    ·430.53:              ·Practically Insoluble:
mainly glucocorticoid budesonide·small        and almost completely      budesonide·344.405:   budesonide·Slightly
activity :             molecule: formoterol   absorbed orally.           formoterol            Soluble: formoterol
budesonide·Selective                          Extensive first-pass
long-acting (12 hours)                        metabolism in the liver.
ß2-adrenergic                                 t1/2 is 2.5 h. Liver
stimulant                                     metabolism.
(bronchodilator):                             The binding of
formoterol                                    formoterol to human
                                              plasma proteins in
                                              vitro is 61%-64% at
                                              concentrations from
                                              0.1 to 100 ng/mL.
                                              Binding to human
                                              serum albumin in vitro
                                              is 31%-38% over a
                                              range of 5 to 500
                                              ng/m. Vd is 3 lt/kg.
                                              Inhaled formoterol is
                                              rapidly absorbed. t1/2
                                              is 8 hours. and CL is
                                              1.2 lt/h/kg. Hepatic
                                              metabolism.
Synairgen is             protein          -   -   -   -
developing the
inhalable formulation
of a novel growth
factor based on the
idea that severe
asthma can be
regarded as a chronic
“ ound”of the
w
conducting airways in
which there is an
increased susceptibility
of the lining of the
asthmatic airway (the
‘ pithelium’ to injury
e           )
and a delayed or
impaired epithelial
repair response.


Calcium release-         small molecule   -   -   -   -
activated calcium
modulator (CRACM)
channel inhibitor
Genetically engineered -                  -   -   -   -
IL-13 antagonists
applied to block the IL-
13 receptors and their
signalling pathway.

Genetically engineered -                  -   -   -   -
IL-13 antagonists
applied to block the IL-
13 receptors and their
signalling pathway.
Genetically engineered -                           -   -   -                        -
IL-13 antagonists
applied to block the IL-
13 receptors and their
signalling pathway.

·Pan-selectin            ·small molecule:          -   -   ·862.91: bimosiamose ·: bimosiamose
antagonist:              bimosiamose
bimosiamose

CCR3 antagonist          -                         -   -   -                        -

VLA-4 antagonists        small molecule            -   -   -                        -

Selective PI3 kinase     small molecule            -   -   -                        -
with the ability to
suppress vascular
leakage and
inflammation
-                        -                         -   -   -                        -

Interleukin-13 inhibitor antibodies                -   -   -                        -
(an important growth
factor for malignant
Hodgkin's lymphoma
cells)
·: nitric oxide-donating ·small molecule: nitric   -   -   ·: nitric oxide-donating ·: nitric oxide-donating
derivative of            oxide-donating                    derivative of            derivative of
budesonide               derivative of                     budesonide               budesonide
                         budesonide
Contains two modified oligonucleotide   -   -   -   -
phosphorothioate
antisense
oligonucleotides
(ODNs), directed
against human CCR3
and the common beta
chain (&#946;c) of IL-
3, IL-5, and GM-CSF
receptors, thereby
downregulating
expression of CCR3
and &#946;c.



TRPA1 antagonist      -                 -   -   -   -
·Nonnarcotic              ·small molecule:      -   -   ·333.469:               ·: carbetapentane
antitussive that has      carbetapentane                carbetapentane          tannate·: pyrilamine
atropine-like and         tannate·small                 tannate·1995.98:        tannate·Sparingly
anesthestic properties.   molecule: pyrilamine          pyrilamine              Soluble: phenylephrine
Its cough suppressing     tannate·small                 tannate·1867.99:        tannate
activity is due to its    molecule:                     phenylephrine tannate
action on the cough       phenylephrine tannate
center of the medulla.:
carbetapentane
tannate·An
antihistamine, H1
receptor blocking
agent belonging to the
ethylenediamine class
of antihistamines.:
pyrilamine
tannate·Alpha-agonist
effects: phenylephrine
tannate
·Nonnarcotic              ·small molecule:      -   -   ·333.469:               ·: carbetapentane
antitussive that has      carbetapentane                carbetapentane          tannate·: pyrilamine
atropine-like and         tannate·small                 tannate·1995.98:        tannate·Sparingly
anesthestic properties.   molecule: pyrilamine          pyrilamine              Soluble: phenylephrine
Its cough suppressing     tannate·small                 tannate·1867.99:        tannate
activity is due to its    molecule:                     phenylephrine tannate
action on the cough       phenylephrine tannate
center of the medulla.:
carbetapentane
tannate·An
antihistamine, H1
receptor blocking
agent belonging to the
ethylenediamine class
of antihistamines.:
pyrilamine
tannate·Alpha-agonist
effects: phenylephrine
tannate




·Corticosteroid with      ·small molecule:      -   -   ·430.53: budesonide     ·Practically Insoluble:
mainly glucocorticoid     budesonide                                            budesonide
activity : budesonide
·Selective long-acting   ·small molecule:    -   -   ·344.405: formoterol   ·Slightly Soluble:
(12 hours) ß2-           formoterol                                         formoterol
adrenergic stimulant
(bronchodilator):
formoterol
·Corticosteroid with     ·small molecule:    -   -   ·521.04:               ·Practically Insoluble:
mainly glucocorticoid    beclomethasone              beclomethasone         beclomethasone
activity:                dipropionate                dipropionate           dipropionate
beclomethasone
dipropionate




·Corticosteroid with      ·small molecule:   -   -   ·500.57: fluticasone   ·Practically Insoluble:
mainly glucocorticoid fluticasone propionate         propionate             fluticasone propionate
activity. It has weak
affinity for the
progesterone receptor,
and virtually no affinity
for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
propionate
·Theophylline has two ·small molecule:   Theophylline is rapidly -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     and completely                                      theophylline
airways of patients                      absorbed from liquid
with reversible                          preparations,
obstruction; smooth                      capsules, and
muscle relaxation (i.e.,                 uncoated tablets; the
bronchodilation) and                     rate, but not the
suppression of the                       extent, of absorption is
response of the                          decreased by food,
airways to stimuli                       and food may also
                                         affect theophylline
: theophylline                           clearance.
                                         Theophylline is
                                         approximately 40%
                                         bound to plasma
                                         proteins. Theophylline
                                         is metabolised in the
                                         liver to 1,3-dimethyluric
                                         acid, 1-methyluric acid
                                         (via the intermediate 1-
                                         methylxanthine), and 3-
                                         methylxanthine.
·Brethine is a beta-     ·small molecule:      -   -   ·548.65: terbutaline   ·Soluble: terbutaline
adrenergic receptor      terbutaline sulfate           sulfate                sulfate
agonist. In vitro and in
vivo pharmacologic
studies have
demonstrated that
terbutaline exerts a
preferential effect on
beta2-adrenergic
receptors.: terbutaline
sulfate
·Theophylline has two ·small molecule:   (Japan label) for 200 -     ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     mg; Cmax                                            theophylline
airways of patients                      (&#956;g/mL) is 3.0 ±
with reversible                          0.5, tmax (h) is 7.2 ±
obstruction; smooth                      1.6,
muscle relaxation (i.e.,                 AUC0&#8594;&#8734;
bronchodilation) and                     (&#956;g&#65381;h/m
suppression of the                       L) is 53.9 ± 10.8. After
response of the                          9 times at 12-hour
airways to stimuli                       intervals oral
                                         administration of two
: theophylline                           THEODUR Tablets
                                         100 mg, healthy non-
                                         eldery, Cmax
                                         (&#956;g/mL) is 8.7 ±
                                         2.2, tmax (h) is 3.9 ±
                                         1.4,
                                         AUC96&#8594;108
                                         (&#956;g&#65381;h/m
                                         L) is 93.1 ± 25.5,
                                         healthy elderly adults,
                                         Cmax (&#956;g/mL) is
                                         10.3 ± 2.3, tmax (h) is
                                         4.8 ± 1.7,
                                         AUC96&#8594;108
                                         (&#956;g&#65381;h/m
                                         L) is 111.6 ± 24.7.
                                         Metabolized mainly in
                                         the liver. Metabolites in
                                         urine were identified to
                                         be 1, 3-dimethyluric
                                         acid, 1-methyluric acid,
                                         and 3-methylxanthine.
                                         Unchanged
·Theophylline has two ·small molecule:   In two-separate single- -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     dose studies utilizing                              theophylline
airways of patients                      different subjects, the
with reversible                          following BA variables
obstruction; smooth                      were observed. Theo-
muscle relaxation (i.e.,                 Dur Sprinkle
bronchodilation) and                     administered in a 500-
suppression of the                       mg dose as pellets on
response of the                          applesauce to 6
airways to stimuli                       healthy adults
                                         produced Cmax of
: theophylline                           9.03 ± 2.59 mcg/ml at
                                         8.67 ± 1.03 hours
                                         following
                                         administration.
                                         Administration of two
                                         lots of Theo-Dur
                                         Sprinkle as intact
                                         capsules in a 600-mg
                                         dose to 6 healthy
                                         adults produced Cmax
                                         of 9.08 ±1.30 mcg/ml
                                         and 7.60 ± 0.95
                                         mcg/ml at 8.33 ± 1.50
                                         and 8.67 ± 3.01 hours
                                         after administration,
                                         respectively. In these
                                         studies, Theo-Dur
                                         Sprinkle exhibited
                                         complete bioavailability
                                         when compared with
                                         an immediate release
                                         product.
·Theophylline has two ·small molecule:   Approximately 90% of -     ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     the dose is                                        theophylline
airways of patients                      metabolized in the
with reversible                          liver. The total body CL
obstruction; smooth                      is 0.016-0.06 L/h/kg,
muscle relaxation (i.e.,                 t1/2 is 6.1-12.8 h and
bronchodilation) and                     the apparent Vd is 0.3-
suppression of the                       0.7 L/kg.
response of the
airways to stimuli

: theophylline




·Theophylline has two ·small molecule:   -                      -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline                                                        theophylline
airways of patients
with reversible
obstruction; smooth
muscle relaxation (i.e.,
bronchodilation) and
suppression of the
response of the
airways to stimuli

: theophylline
·Theophylline has two ·small molecule:   Theophylline is           -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     approximately 40%                                     theophylline
airways of patients                      bound to plasma
with reversible                          proteins. Theophylline
obstruction; smooth                      is metabolised in the
muscle relaxation (i.e.,                 liver to 1,3-dimethyluric
bronchodilation) and                     acid, 1-methyluric acid
suppression of the                       (via the intermediate 1-
response of the                          methylxanthine), and 3-
airways to stimuli                       methylxanthine.

: theophylline
·Theophylline has two ·small molecule:   THEOLONG Tablets -         ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     were administered to                               theophylline
airways of patients                      seven patients with
with reversible                          asthma at a dose of
obstruction; smooth                      200 mg of theophylline
muscle relaxation (i.e.,                 twice daily for three
bronchodilation) and                     days to achieve a
suppression of the                       steady state in the
response of the                          theophylline blood
airways to stimuli                       concentration. The
                                         blood theophylline
: theophylline                           concentration was
                                         determined 12 hr after
                                         the final
                                         administration. The
                                         mean blood
                                         concentration (Cave)
                                         was 10.16
                                         &#956;g/mL. Cmax:
                                         12.58 &#956;g/mL,
                                         Tmax: 4.9 hr.
                                         Theophylline is little
                                         affected by the first-
                                         pass effect but is
                                         metabolized in the liver
                                         and is almost
                                         completely excreted in
                                         the urine
·Theophylline has two ·small molecule:   THEOLONG Tablets -         ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     were administered to                               theophylline
airways of patients                      seven patients with
with reversible                          asthma at a dose of
obstruction; smooth                      200 mg of theophylline
muscle relaxation (i.e.,                 twice daily for three
bronchodilation) and                     days to achieve a
suppression of the                       steady state in the
response of the                          theophylline blood
airways to stimuli                       concentration. The
                                         blood theophylline
: theophylline                           concentration was
                                         determined
                                         12 hr after the final
                                         administration. The
                                         mean blood
                                         concentration (Cave)
                                         was 10.16
                                         &#956;g/mL.
                                         Cmax: 12.58
                                         &#956;g/mL, Tmax:
                                         4.9 hr. Theophylline is
                                         little affected by the
                                         first-pass effect but is
                                         metabolized in the liver
                                         and is almost
                                         completely excreted in
                                         the urine
·Theophylline has two ·small molecule:   -   -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline                                     theophylline
airways of patients
with reversible
obstruction; smooth
muscle relaxation (i.e.,
bronchodilation) and
suppression of the
response of the
airways to stimuli

: theophylline




·Theophylline has two ·small molecule:   -   -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline                                     theophylline
airways of patients
with reversible
obstruction; smooth
muscle relaxation (i.e.,
bronchodilation) and
suppression of the
response of the
airways to stimuli

: theophylline
·Theophylline has two ·small molecule:   The total body CL is    -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline     0.27-1.03 ml/kg/min                                 theophylline
airways of patients                      and t1/2 is 6.1-12.8
with reversible                          hrs. The apparent Vd
obstruction; smooth                      of theophylline is
muscle relaxation (i.e.,                 approximately 0.3-0.7
bronchodilation) and                     L/kg.
suppression of the
response of the
airways to stimuli

: theophylline




·Theophylline has two ·small molecule:   -                       -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline                                                         theophylline
airways of patients
with reversible
obstruction; smooth
muscle relaxation (i.e.,
bronchodilation) and
suppression of the
response of the
airways to stimuli

: theophylline
·Nedocromil sodium is ·small molecule:       After inhalation of       -   ·415.3: nedocromil   ·Soluble: nedocromil
a mast cell stabilizer   nedocromil sodium   nedocromil sodium (in         sodium               sodium
and inhibits the release                     common with other
of mediators from cells                      drugs inhaled using an
involved in                                  MDI) a small fraction
hypersensitivity                             (generally 10%)
reactions. Decreased                         reaches the lungs,
chemotaxis and                               while a major portion
decreased activation                         of the dose is
of eosinophils have                          deposited in the mouth
been demonstrated. :                         or oropharynx and
nedocromil sodium                            swallowed. The oral
                                             absorption of
                                             nedocromil sodium
                                             from the
                                             gastrointestinal tract is
                                             low, being
                                             approximately 2% of
                                             an orally administered
                                             dose. Hence,
                                             nedocromil sodium
                                             measured in plasma
                                             following inhalation is
                                             considered to
                                             represent mainly the
                                             drug absorbed by the
                                             airways. After
                                             inhalation, plasma
                                             concentrations of
                                             nedocromil sodium
                                             reach a maximum
                                             within one hour post-
                                             dosing and decline
                                             with a half-life of 1-2
·Nedocromil sodium is ·small molecule:       Absolute BA is 8% for -   ·415.3: nedocromil   ·Soluble: nedocromil
a mast cell stabilizer   nedocromil sodium   single and 17% for        sodium               sodium
and inhibits the release                     multiple doses. t1/2 is
of mediators from cells                      3.3 hrs. 89% bound to
involved in                                  plasma proteins.
hypersensitivity
reactions. Decreased
chemotaxis and
decreased activation
of eosinophils have
been demonstrated. :
nedocromil sodium
·Corticosteroid with     ·small molecule:   -   -   ·434.5: triamcinolone   ·Practically Insoluble:
mainly glucocorticoid    triamcinolone              acetonide               triamcinolone
activity, anti-          acetonide                                          acetonide
inflammatory.:
triamcinolone
acetonide




·Adrenergic beta2-       ·small molecule:   -   -   ·227.73: tulobuterol    ·Practically Insoluble:
agonist similar to       tulobuterol                                        tulobuterol
albuterol: tulobuterol
·Adrenergic beta2-       ·small molecule:   -   -   ·227.73: tulobuterol   ·Practically Insoluble:
agonist similar to       tulobuterol                                       tulobuterol
albuterol: tulobuterol




-                        -                  -   -   -                      -




-                        small molecule     -   -   -                      -




-                        -                  -   -   -                      -


-                        -                  -   -   -                      -
·Theophylline has two ·small molecule:     Rapidly and             -   ·180.16: theophylline   ·Slightly Soluble:
distinct actions in the theophylline       completely absorbed                                 theophylline
airways of patients                        after oral
with reversible                            administration in
obstruction; smooth                        solution or immediate-
muscle relaxation (i.e.,                   release solid oral
bronchodilation) and                       dosage form.
suppression of the                         Undergoes extensive
response of the                            hepatic metabolism.
airways to stimuli                         CL: 0.65 mL/kg/min.
                                           t1/2: 8.7 h. 40% bound
: theophylline                             to plasma proteins. In
                                           adults, about 10% of a
                                           dose of theophylline is
                                           excreted unchanged in
                                           the urine. Vd: 0.45
                                           L/kg (range 0.3-0.7
                                           L/kg).


·Corticosteroid with    ·small molecule:   -                       -   ·430.53: budesonide     ·Practically Insoluble:
mainly glucocorticoid   budesonide                                                             budesonide
activity : budesonide




VLA-4 (alpha 4 beta 1) small molecule      -                       -   -                       -
antagonists
·: undisclosed small   ·small molecule:      -   -   ·: undisclosed small   ·: undisclosed small
molecule·: undisclosed undisclosed small             molecule·: undisclosed molecule·: undisclosed
small molecule         molecule·small                small molecule         small molecule
                       molecule: undisclosed
                       small molecule




-                     -                      -   -   -                      -




-                     small molecule         -   -   -                      -
-                     vaccine           -   -   -   -


ATP is known to affect small molecule   -   -   -   -
several cell types that
play a critical
mechanistic role in
asthma. In particular,
ATP exacerbates the
immune reaction-
induced release of
histamine from human
lung mast cells. We
refer to the proposed
drug that would block
this action of ATP as
Primastrene™  .



-                     small molecule    -   -   -   -
-   -   -   -   -   -
·Beta agonist:             ·small molecule:   Salbutamol:             -   ·239.213:           ·Sparingly Soluble:
albuterol·Corticosteroi    albuterol·small    Salbutamol does not         albuterol·521.04:   albuterol·Practically
d with mainly              molecule:          appear to be                beclomethasone      Insoluble:
glucocorticoid activity:   beclomethasone     metabolised in the          dipropionate        beclomethasone
beclomethasone             dipropionate       lung, therefore its                             dipropionate
dipropionate                                  ultimate metabolism
                                              and excretion following
                                              inhalation depends
                                              upon the delivery
                                              method used, which
                                              determines the
                                              proportion of inhaled
                                              salbutamol relative to
                                              the proportion
                                              inadvertently
                                              swallowed. It has been
                                              suggested that the
                                              majority of an inhaled
                                              dose is swallowed and
                                              absorbed from the gut.
                                              The plasma t1/2 of
                                              salbutamol has been
                                              estimated to range
                                              from 4 - 6 hrs. (REF 1-
                                              (Pubmed id:5081599),
                                              REF 2- (Pubmed
                                              id:974663), REF 3-
                                              (Pubmed id:17520),
                                              REF 4- (Pubmed
                                              id:3790406), REF 5-
                                              (Pubmed id:2687008),
                                              REF 6- (Pubmed
                                              id:2598971), REF 7-
                                              (Pubmed id:1457264),
·Albuterol sulfate, the    ·small molecule:          Salbutamol                -   ·548.24: albuterol   ·Freely Soluble:
racemic form of            albuterol sulfate·small   administered                  sulfate·521.04:      albuterol
albuterol and a            molecule:                 intravenously has a           beclomethasone       sulfate·Practically
relatively selective       beclomethasone            half-life of 4 to 6 hours     dipropionate         Insoluble:
beta 2 -adrenergic         dipropionate              and is cleared partly                              beclomethasone
bronchodilator:                                      renally and partly by                              dipropionate
albuterol                                            metabolism to the
sulfate·Corticosteroid                               inactive 4' - 0-sulphate
with mainly                                          (phenolic sulphate)
glucocorticoid activity:                             which is also excreted
beclomethasone                                       primarily in the urine.
dipropionate                                         The faeces are a
                                                     minor route of
                                                     excretion. The majority
                                                     of a dose of
                                                     salbutamol given
                                                     intravenously, orally or
                                                     by inhalation is
                                                     excreted within 72
                                                     hours. Salbutamol is
                                                     bound to plasma
                                                     proteins to the extent
                                                     of 10%.
                                                     After administration by
                                                     the inhaled route
                                                     between 10 and 20%
                                                     of the dose reaches
                                                     the lower airways.
                                                     Beclomethasone
                                                     dipropionate: When
                                                     administered via
                                                     inhalation (via metered
                                                     dose inhaler) there is
                                                     extensive conversion
·Beta agonist: albuterol ·small molecule:   Salbutamol (albuterol) -     ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          sulfate provides short-                            albuterol
                                            acting (4-6 hour)
                                            bronchodilatation with
                                            a fast onset (within 5
                                            minutes) in reversible
                                            airways obstruction.
                                            Salbutamol is readily
                                            absorbed from the
                                            gastrointestinal tract. It
                                            is subject to first-pass
                                            metabolism in the liver
                                            and possibly in the gut
                                            wall; the main
                                            metabolite is an
                                            inactive sulfate
                                            conjugate. Salbutamol
                                            is rapidly excreted in
                                            the urine as
                                            metabolites and
                                            unchanged drug; there
                                            is some excretion in
                                            the faeces. Salbutamol
                                            does not appear to be
                                            metabolised in the
                                            lung, therefore its
                                            ultimate metabolism
                                            and excretion following
                                            inhalation depends
                                            upon the delivery
                                            method used, which
                                            determines the
                                            proportion of inhaled
                                            salbutamol relative to
·Albuterol sulfate, the   ·small molecule:    Salbutamol                -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   administered                  sulfate              albuterol sulfate
albuterol and a                               intravenously has a
relatively selective                          t1/2 of 4 - 6 hrs and is
beta 2 -adrenergic                            cleared partly renally
bronchodilator:                               and partly by
albuterol sulfate                             metabolism to the
                                              inactive 4'-O-Sulphate
                                              (Phenolic Sulphate)
                                              which is also excreted
                                              primarily in the urine.
                                              The faeces are a
                                              minor route of
                                              excretion. The majority
                                              of a dose of
                                              Salbutamol given
                                              intravenously, orally or
                                              by inhalation is
                                              excreted within 72
                                              hours.Salbutamol is
                                              readily absorbed from
                                              the gastrointestinal
                                              tract. It is subject to
                                              first-pass metabolism
                                              in the liver and
                                              possibly in the gut wall;
                                              the main metabolite is
                                              an inactive sulfate
                                              conjugate.
·Albuterol sulfate, the   ·small molecule:    Salbutamol                -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   administered                  sulfate              albuterol sulfate
albuterol and a                               intravenously has a
relatively selective                          half-life of 4 to 6 hours
beta 2 -adrenergic                            and is cleared partly
bronchodilator:                               renally, and partly by
albuterol sulfate                             metabolism to the
                                              inactive 4'-O-sulphate
                                              (phenolic sulphate)
                                              which is also excreted
                                              primarily in the urine.
                                              The faeces are a
                                              minor route of
                                              excretion. After
                                              administration by the
                                              inhaled route between
                                              10 and 20% of the
                                              dose reaches the
                                              lower airways. The
                                              remainder is retained
                                              in the delivery system
                                              or is deposited in the
                                              oropharynx from
                                              where it is swallowed.
                                              The fraction deposited
                                              in the airways is
                                              absorbed into the
                                              pulmonary tissues and
                                              circulation, but is not
                                              metabolised by the
                                              lung. On reaching the
                                              systemic circulation it
                                              becomes accessible to
                                              hepatic metabolism
·Beta agonist: albuterol ·small molecule:   Albuterol (WHO             -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol          designation is                                       albuterol
                                            salbutamol) is readily
                                            absorbed from the
                                            gastrointestinal tract. It
                                            is subject to first-pass
                                            metabolism in the liver
                                            and possibly in the gut
                                            wall; the main
                                            metabolite is an
                                            inactive sulfate
                                            conjugate.
                                            Approximately 72% of
                                            the inhaled dose is
                                            excreted within 24
                                            hours in the urine, and
                                            consists of 28% as
                                            unchanged drug and
                                            44% as metabolite.;
                                            there is some
                                            excretion in the
                                            faeces.
                                            Albuterol/Salbutamol
                                            does not appear to be
                                            metabolised in the
                                            lung, therefore its
                                            ultimate metabolism
                                            and excretion following
                                            inhalation depends
                                            upon the delivery
                                            method used, which
                                            determines the
                                            proportion of inhaled
                                            salbutamol relative to
·Beta agonist: albuterol ·small molecule:     -                      -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol                                                             albuterol




·Albuterol sulfate, the   ·small molecule:    Cmax of 1.4 - 3.2      -   ·548.24: albuterol    ·Freely Soluble:
racemic form of           albuterol sulfate   ng/mL occurs at 0.5        sulfate               albuterol sulfate
albuterol and a                               hrs. Less than 20% of
relatively selective                          dose absorbed. Short-
beta 2 -adrenergic                            acting (4-6 hour)
bronchodilator:                               bronchodilatation with
albuterol sulfate                             a fast onset (within 5
                                              minutes) in reversible
                                              airways obstruction.
                                              t/1/2 is 4-6 hrs (IV)
·Albuterol sulfate, the   ·small molecule:    Cmax of 1.4 - 3.2       -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   ng/mL occurs at 0.5         sulfate              albuterol sulfate
albuterol and a                               hours. t/1/2 is 4-6 hrs
relatively selective                          (IV). is bound to
beta 2 -adrenergic                            plasma proteins to the
bronchodilator:                               extent of 10%.
albuterol sulfate




·Albuterol sulfate, the   ·small molecule:    Salbutamol (albuterol) -    ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   sulfate provides short-     sulfate              albuterol sulfate
albuterol and a                               acting (4-6 hour)
relatively selective                          bronchodilatation with
beta 2 -adrenergic                            a fast onset (within 5
bronchodilator:                               minutes) in reversible
albuterol sulfate                             airways obstruction.
                                              Undergoes extensive
                                              first pass metabolism.
·Albuterol sulfate, the   ·small molecule:    -   -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate           sulfate              albuterol sulfate
albuterol and a
relatively selective
beta 2 -adrenergic
bronchodilator:
albuterol sulfate
·Albuterol sulfate, the   ·small molecule:    Tmax= is 52 hrs        -   ·548.24: albuterol   ·Freely Soluble:
racemic form of           albuterol sulfate   (longer than CFC           sulfate              albuterol sulfate
albuterol and a                               propellant=0.17 hrs),
relatively selective                          t1/2 is 4.6 hrs.
beta 2 -adrenergic                            Undergoes extensive
bronchodilator:                               first pass metabolism.
albuterol sulfate
·Corticosteroid with      ·small molecule:   -   -   ·538.6: fluticasone   ·Practically Insoluble:
mainly glucocorticoid fluticasone furoate            furoate               fluticasone furoate
activity. It has weak
affinity for the
progesterone receptor,
and virtually no affinity
for the
mineralocorticoid,
estrogen, or androgen
receptors.: fluticasone
furoate




Beta 2 Adrenergic      small molecule        -   -   -                     -
Agonist
·Beta agonist: albuterol ·small molecule:   -   -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol                                        albuterol




·Beta agonist: albuterol ·small molecule:   -   -   ·239.213: albuterol   ·Sparingly Soluble:
                         albuterol                                        albuterol
·Albuterol sulfate, the   ·small molecule:    Salbutamol is readily -      ·548.24: albuterol     ·Freely Soluble:
racemic form of           albuterol sulfate   absorbed from the            sulfate                albuterol sulfate
albuterol and a                               gastrointestinal tract. It
relatively selective                          is subject to first-pass
beta 2 -adrenergic                            metabolism in the liver
bronchodilator:                               and possibly in the gut
albuterol sulfate                             wall; the main
                                              metabolite is an
                                              inactive sulfate
                                              conjugate. BA is about
                                              50%. Salbutamol
                                              administered
                                              intravenously has a
                                              t1/2 of 4 - 6 hrs and is
                                              cleared partly renally
                                              and partly by
                                              metabolism.




·Selective long-acting    ·small molecule:    -                        -   ·344.405: formoterol   ·Slightly Soluble:
(12 hours) ß2-            formoterol                                                              formoterol
adrenergic stimulant
(bronchodilator):
formoterol
·Inhibits the binding of ·antibodies:   After SC                -   ·149000: omalizumab   ·: omalizumab
IgE to the high-affinity omalizumab     administration,
IgE receptor (FceRI)                    Omalizumab is
on the surface of mast                  absorbed with an
cells and basophils.:                   average absolute BA
omalizumab                              of 62%. Following a
                                        single SC dose in adult
                                        and adolescent
                                        patients with asthma,
                                        Omalizumab was
                                        absorbed slowly,
                                        reaching peak serum
                                        concentrations after an
                                        average of 7-8 days.
                                        Vd (SC): 78 ± 32
                                        mL/kg. t1/2: 26 days,
                                        CL: 2.4 ± 1.1
                                        mL/kg/day.

·Inhibits the binding of ·antibodies:   -                       -   ·149000: omalizumab   ·: omalizumab
IgE to the high-affinity omalizumab
IgE receptor (FceRI)
on the surface of mast
cells and basophils.:
omalizumab
·A beta-agonist for the ·small molecule:        There is some          -   ·628.7: levalbuterol   ·Freely Soluble:
treatment of reversible levalbuterol tartrate   systemic absorption of     tartrate               levalbuterol tartrate
bronchospasm.:                                  inhaled
levalbuterol tartrate                           levosalbutamol. It
                                                appears to be
                                                stereochemically
                                                stable in vivo and not
                                                metabolised to S(+)-
                                                salbutamol. After a
                                                single dose
                                                levosalbutamol has a
                                                half-life of 3.3 hours
·A beta-agonist for the ·small molecule:   -   -   ·275.8: levalbuterol   ·Freely Soluble:
treatment of reversible levalbuterol               hydrochloride          levalbuterol
bronchospasm.:          hydrochloride                                     hydrochloride
levalbuterol
hydrochloride
·Active inhibitor of 5- ·small molecule:   Zileuton is rapidly      -   ·236.294: zileuton   ·Practically Insoluble:
lipoxygenase, the       zileuton           absorbed upon oral                                zileuton
enzyme that catalyzes                      administration with a
the formation of                           mean time to peak
leukotrienes from                          plasma concentration
arachidonic acid.:                         (Tmax) of 1.7 hours
zileuton                                   and a mean
                                           peak level (Cmax) of
                                           4.98 &#956;g/mL. The
                                           absolute bioavailability
                                           of ZYFLO is unknown.
                                           Systemic exposure
                                           (mean AUC) following
                                           600 mg
                                           ZYFLO administration
                                           is 19.2 &#956;g.hr/mL.
                                           Plasma concentrations
                                           of zileuton are
                                           proportional to dose,
                                           and steady-state levels
                                           are
                                           predictable from single-
                                           dose pharmacokinetic
                                           data. Administration of
                                           ZYFLO with food
                                           resulted in a small but
                                           statistically
                                           significant
                                           increase (27%) in
                                           zileuton Cmax without
                                           significant changes in
                                           the extent of
                                           absorption (AUC) or
                                           Tmax. Therefore,
·An IL-2 receptor         ·antibodies:   t1/2: 11-38 days. CL:   -   ·142612: daclizumab   ·: daclizumab
antagonist that binds daclizumab         15 mL/hour
with high-affinity to the
Tac subunit of the high-
affinity IL-2 receptor
complex and inhibits IL-
2 binding. : daclizumab




-                        -               -                       -   -                     -
·Histamine H1             ·small molecule:   -   -   ·322.47: mequitazine   ·: mequitazine
antagonists :             mequitazine
mequitazine
·Histamine H1             ·small molecule:   -   -   ·322.47: mequitazine   ·: mequitazine
antagonists :             mequitazine
mequitazine
·Active inhibitor of 5-   ·small molecule:   -   -   ·236.294: zileuton     ·Practically Insoluble:
lipoxygenase, the         zileuton                                          zileuton
enzyme that catalyzes
the formation of
leukotrienes from
arachidonic acid.:
zileuton




Dissociating           -                     -   -   -                      -
glucocorticoid
Protein-free synthetic ·small molecule:      -   -   ·: pumactant           ·: pumactant
lung surfactant made pumactant
from naturally
occurring
phospholipids.···Lung
surfactant: pumactant
·Active inhibitor of 5- ·small molecule:   A three-way crossover -    ·236.294: zileuton   ·Practically Insoluble:
lipoxygenase, the       zileuton           study was conducted                             zileuton
enzyme that catalyzes                      in healthy male and
the formation of                           female subjects (n=24)
leukotrienes from                          with a mean age of 35
arachidonic acid.:                         (range 19-56) following
zileuton                                   multiple doses of 1200
                                           mg (2 x 600 mg)
                                           ZYFLO CR tablets
                                           administered every 12
                                           hours under fasted
                                           and fed conditions,
                                           and 600 mg zileuton
                                           immediate-release
                                           tablets every 6 hours
                                           under fed conditions
                                           until steady state
                                           zileuton levels were
                                           achieved. Food
                                           increased AUC and
                                           Cmin of ZYFLO CR by
                                           43%
                                           and 170%,
                                           respectively, but had
                                           no effect on Cmax.
                                           Therefore, ZYFLO CR
                                           is recommended to be
                                           administered with
                                           food. At steady state,
                                           relative bioavailability
                                           of ZYFLO CR to
                                           zileuton
                                           immediate-release
                                           tablets with respect to
Based on the              peptide          -   -   -   -
proprietary peptide
KL4 (also known as
sinapultide) designed
to precisely mimic the
essential attributes of
human surfactant
protein B (SP-B).


anti YKL40 MAb            antibodies       -   -   -   -

      s
Bruton’ tyrosine          small molecule   -   -   -   -
kinase inhibitor


      s
Bruton’ tyrosine          small molecule   -   -   -   -
kinase inhibitor.


deCODE identified a   small molecule       -   -   -   -
promising compound
targeting the product
of an asthma gene and
developed by another
company for use in a
different indication
Prevents activation of    protein             -   -   -                         -
histamine receptors
including the H4
receptor




·A serine protease        ·protein: alpha-1   -   -   ·: alpha-1 antitrypsin,   ·: alpha-1 antitrypsin,
inhibitor (serpin). It    antitrypsin,                recombinant human         recombinant human
protects tissue from      recombinant human
enzymes from
inflammatory cells,
especially elastase. It
is present in human
blood at 1.5 - 3.5
gram/liter.

: alpha-1 antitrypsin,
recombinant human
Anti-OX40 ligand        antibodies   -   -   -   -
monoclonal antibody
blocks interaction of
OX40 (a TNF
superfamily receptor)
to its ligand
ß-Tryptase inhibitors   -            -   -   -   -
Excipient                How                 DDS Technologies   Physical Chemical   DDS Technology        Approval _
                         Supplied_Administer                    Properties          Owner                 Exclusivity
                         ed

In Phase I trials, the   In Phase 2, doses of  -                -                   Theravance Inc.       -
drug was delivered as    10, 15, and 20
a vapor and as a dry     micrograms once daily
powder trials            were studied. [18699]

DPI formulation. Part -                        -                -                   GlaxoSmithKline Plc   -
of Beyond Advair
collaboration between
Theravance and GSK.

-                        -                     -                -                   GlaxoSmithKline Plc   -


-                        An open-label, single -                -                   -                     -
                         dose study to
                         investigate the safety,
                         tolerability and
                         pharmacokinetics of
                         90mg of GW274150 in
                         adult and elderly RA
                         subjects was
                         completed. trials


-                        -                     -                -                   GlaxoSmithKline Plc   -

-                        -                     -                -                   -                     -


-                        -                     -                -                   GlaxoSmithKline Plc   -
-   Once daily inhaled -        -   GlaxoSmithKline Plc   -
    doses of GW870086X
    administered via
    DISKHALER trials
-   -                  -        -   -                     -


-   It is a once or         -   -   -                     -
    maximally twice daily
    inhalation treatment
-   Once daily treatment    -   -   -                     -


-   Phase II trial          -   -   Argenta Discovery     -
    : administered twice
    daily
Each unit contains a      Supplied as a           -   ·USP 29 (Flunisolide) 3M Health Care   Year of US Approval:
0.24 % w/w solution of    pressurized lined           White to creamy-white,                 2006-01-27
flunisolide hemihydrate   aluminum canister in        crystalline powder.                    Earliest US Market
in 10:90 w/w              boxes of one.               Melts at about 245 ,                   Exclusivity: 2009-01-
ethanol:1,1,1,2-          Adults (age 12 and          with decomposition.                    27
tetrafluoroethane (HFA    older): The                 Practically insoluble in
134a).                    recommended starting        water; soluble in
                          dose is 160 mcg twice       acetone; sparingly
                          daily. The                  soluble in chloroform;
                          maximum dose should         slightly soluble in
                          not exceed 320 mcg          methanol.
                          twice daily.                The octanol: water
                          Children (age 6 to 11):     partition coefficient is
                          The recommended             2.17 at neutral pH.:
                          starting dose is 80         flunisolide
                          mcg twice daily. The
                          maximum dose should
                          not exceed 160 mcg
                          twice daily.




-                         -                       -   -                    -                 -


-                         -                       -   -                    -                 -
Compounds will be        -               -       -   -                -
tested for delivery by
the oral, intravenous or
inhaled route of
administration.




PDDS microspheres of Once-a-day dosing   PDDS™   -   Acusphere Inc.   -
marketed small
molecule. Inhalable
powder in a sustained
release, microparticle
form delivered using
marketed DPI device.
Particles are 3.5 -4.5
microns MMAD.
Acusphere patent
WO2007070851
describes use of
fluticasone propionate
as model drug
delivered with
Cyclohaler device.
-                    -                      AIR Inhaler   ·USP 29 (Albuterol       Alkermes, Inc.          -
                                                          Sulfate) White or
                                                          practically white
                                                          powder. Freely soluble
                                                          in water; slightly
                                                          soluble in alcohol, in
                                                          chloroform, and in
                                                          ether. pKa=9.14.
                                                          Solubility: 24.5% w/v at
                                                          pH 7.: albuterol sulfate



-                    -                      AIR Inhaler   -                       Alkermes, Inc.           -

Inhalation aerosol   maximum of one dose -                -                       Altair Therapeutics Inc. -
(undisclosed         per day, maximum of 6
technology)          doses in 22 days
                     trials.In Phase I trial,
                     30 mg single dose
                     arm; 20 mg multiple
                     doses were
                     administered. [56815]
Taifun inhaler   Phase I dosing:0.025   TAIFUN® DPI   -   Akela Pharma Inc.   -
                 mg to 5 mg. Phase II
                 dosing: 5mg b.i.d.
Excipients: Sucrose,   Available as dry syrup -   ·Pemirolast potassium -     Year of Japan
sodium citrate         including 5 mg             occurs as an odorless,      Approval: 1992-08-01
                       pemirolast potassium       bitter, light yellow
                       per gram. The usual        crystalline powder. It is
                       child dosage for oral      freely soluble in water,
                       use is 0.2 mg/kg of        slightly soluble in
                       pemirolast potassium       methanol and ethanol,
                       for bronchial asthma,      and practically
                       and 0.1 mg/kg or           insoluble in ether.:
                       allergic rhinitis given    pemirolast potassium
                       twice a day after
                       breakfast and at
                       bedtime, dissolved in
                       water before use.
Excipients:Lactose,          Available as yellowish -   ·Pemirolast potassium -              Year of Japan
partly pregelatinized        white, plain, round 5      occurs as an odorless,               Approval: 1991-03-01
starch,                      and 10 mg tablets. The     bitter, light yellow
hydroxypropylcellulose       usual adult dosage for     crystalline powder. It is
, cellulose, silicic acid,   oral use is 10 mg of       freely soluble in water,
magnesium stearate           pemirolast potassium       slightly soluble in
                             for bronchial asthma,      methanol and ethanol,
                             and 5 mg for allergic      and practically
                             rhinitis given twice a     insoluble in ether.:
                             day after breakfast and    pemirolast potassium
                             supper.




Tablet-based vaccine         -                      -   -                       ALK-Abello   -
-   Results from the        -   -   -   -
    Phase 1 trial showed
    that AM103 was safe
    and well-tolerated at
    doses up to 1,000 mg
    per day. The systemic
    exposure of AM103
    increased linearly from
    50 mg to 1,000 mg.
    [27737]
-   -                       -   -   -   -




-   -                       -   -   -   -

-   -                       -   -   -   -




-   -                       -   -   -   -
-                       Once-daily              -                 -            -                      -

Dry powder inhaler      -                       -                 ·: APC 366   Celera Corp.           -
formulation
Captisol formulations   -                           · CAPTISOL®
                                                AERx™             -            Aradigm Corp.          -
delivered in AERX
nebulizer




-                       -                       -                 -            -                      -

-                       -                       -                 -            ISIS Pharmaceuticals   -
                                                                               Inc.


-                       -                       -                 -            -                      -


-                       -                       -                 -            -                      -


-                       -                       -                 -            A-Viral                -

-                       In phase I trial Avac   -                 -            Genesis Research &     -
                        was administered                                       Development Corp.
                        intranasally [43886].
-                       -                       -                 -            Pfizer Inc.            -
-   -   -   -   Pfizer Inc.   -




-   -   -   -   -             -
-   -   -   -   -             -
Decoy ODN              -   Decoy ODN            -               Activaero GmbH   -
Technology delivered       Technology· AKITA® 2
with AKITA 2 nebulizer




-                      -   -                    ·: AWD 12-281   elbion NV        -


-                      -   -                    -               -                -

-                      -   -                    -               -                -
-                      At phase 2 Asthma         -   -   -   -
                       study patients received
                       50 mg, 400 mg and
                       1000 mg AZD1981
                       tablet twice
                       daily(trials). At phase 2
                       COPD study patients
                       received AZD1981
                       tablet twice daily for 4
                       weeks(trials)


-                      -                         -   -   -   -

-                      -                         -   -   -   -

-                      -                         -   -   -   -


-                      -                         -   -   -   -

-                      -                         -   -   -   -
-                      -                         -   -   -   -




-                      -                         -   -   -   -

nasal spray solution   At phase 1 Allergic      -    -   -   -
                       Rhinitis trials 30 or 60
                       mg administered
                       intranasally once
                       weekly for one month.

-                      -                         -   -   -   -
-                     -   -   -                      -                -




HFA MDI formulation   -   -   ·USP 29 (Triazolam)    Sanofi-Aventis   -
                              White to off-white,
                              practically odorless,
                              crystalline powder.
                              Soluble in chloroform;
                              slightly soluble in
                              alcohol; practically
                              insoluble in ether and
                              in water.: triazolam·:
                              reproterol




-                     -   -   -                      -                -
Inactive ingredients:    10 (unflavored) and 20 -   ·A fine white to pale     -   Year of US Approval:
croscarmellose           mg white, round,           yellow amorphous              1996-09-26
sodium, lactose,         biconvex, film-coated      powder, is practically        Earliest US Market
magnesium stearate,      tablets.                   insoluble in water. It is     Exclusivity: 2010-01-
microcrystalline         The recommended            slightly soluble in           01
cellulose, povidone,     dose in adults and         methanol and freely           Earliest Patent
ydroxypropylmethylcell   children 12 years and      soluble in                    Exclusivity: 2010-09-
ulose, and titanium      older is 20 mg twice       tetrahydrofuran,              26
dioxide.                 daily.                     dimethylsulfoxide, and        Year of EU Approval:
                         The recommended            acetone.                      2000-06-01
                         dose of in children 5      : zafirlukast
                         through 11 years of
                         age is 10 mg twice
                         daily.
AccuNeb (albuterol         3 mL in unit-dose low- -   ·USP 29 (Albuterol       DEY L.P.               Year of US Approval:
sulfate) Inhalation        density polyethylene       Sulfate) White or                               2001-04-30
Solution is supplied as    (LDPE) vials. Each unit-   practically white                               Earliest US Market
a 3 mL, clear,             dose LDPE is               powder. Freely soluble                          Exclusivity: 2021-01-
colorless, sterile,        protected in a foil        in water; slightly                              01
preservative-free,         pouch, and each foil       soluble in alcohol, in                          Earliest Patent
aqueous solution in        pouch contains five        chloroform, and in                              Exclusivity: 2021-12-
two different strengths    unit-dose LDPE vials.      ether. pKa=9.14.                                28
(0.63 mg and 1.25 mg)      Each strength of           Solubility: 24.5% w/v at
of albuterol (equivalent   AccuNeb (albuterol         pH 7.: albuterol sulfate
to 0.75 mg of albuterol    sulfate) Inhalation
sulfate or 1.5 mg of       Solution is available in
albuterol sulfate per 3    a shelf carton
mL).                       containing multiple foil
                           pouches.
                           Administered 3 or 4
                           times daily

-                          -                      -   ·USP 29 (Albuterol       Watson                 Year of US Approval:
                                                      Sulfate) White or        Pharmaceuticals Inc.   2007-09-25
                                                      practically white
                                                      powder. Freely soluble
                                                      in water; slightly
                                                      soluble in alcohol, in
                                                      chloroform, and in
                                                      ether. pKa=9.14.
                                                      Solubility: 24.5% w/v at
                                                      pH 7.: albuterol sulfate
-                      -   -         -                       -           -




Mystic EHD nebulizer   -   Mystic™   ·(EP5.0) White or        Ventaira   -
                                     almost white powder.
                                     Practically insoluble in
                                     water, sparingly
                                     soluble in methylene
                                     chloride, slightly
                                     soluble in alcohol.:
                                     fluticasone propionate
Diskus DPI device.      Diskus100/50, 250/50 Diskus/AccuHaler   ·(EP5.0) White or        GlaxoSmithKline Plc   Year of US Approval:
Inactive ingredients:   and 500/50 contain                      almost white powder.                           2000-08-24
lactose                 100mcg/50 mcg, 250                      Practically insoluble in                       Earliest US Market
                        mcg/50 mcg and 500                      water, sparingly                               Exclusivity: 2011-04-
                        mcg/50 mcg of                           soluble in methylene                           30
                        flutacasone/salmeterol                  chloride, slightly                             Earliest Patent
                        respectively. Dosed                     soluble in alcohol.:                           Exclusivity: 2008-02-
                        twice daily                             fluticasone                                    12
                                                                propionate·A white to                          Year of EU Approval:
                                                                off-white powder. It is                        1999-02-01
                                                                freely soluble in                              Year of Japan
                                                                methanol; slightly                             Approval: 2007-04-18
                                                                soluble in ethanol,
                                                                chloroform, and
                                                                isopropanol; and
                                                                sparingly soluble in
                                                                water.

                                                                : salmeterol xinafoate
Each unit contains a     Advair HFA is            -   ·(EP5.0) White or        GlaxoSmithKline Plc   Year of US Approval:
microcrystalline         available in three           almost white powder.                           2006-06-08
suspension of            strengths, Advair HFA        Practically insoluble in                       Earliest US Market
fluticasone propionate   45/21, Advair HFA            water, sparingly                               Exclusivity: 2009-06-
(micronized) and         115/21 and Advair            soluble in methylene                           08
salmeterol xinafoate     HFA 230/21. Each 12-         chloride, slightly                             Earliest Patent
(micronized) in          gram canister of             soluble in alcohol.:                           Exclusivity: 2008-02-
propellant HFA-134a      Advair HFA provides          fluticasone                                    12
(1,1,1,2-                120 metered                  propionate·A white to
tetrafluoroethane). It   inhalations. Dosed           off-white powder. It is
contains no other        twice daily. After           freely soluble in
excipients.              priming, each                methanol; slightly
                         actuation of the inhaler     soluble in ethanol,
                         delivers 50, 125, or         chloroform, and
                         250 mcg of fluticasone       isopropanol; and
                         propionate and 25 mcg        sparingly soluble in
                         of salmeterol in 75 mg       water.
                         of suspension from the
                         valve. Each actuation        : salmeterol xinafoate
                         delivers 45, 115, or
                         230 mcg of fluticasone
                         propionate and 21 mcg
                         of salmeterol from the
                         actuator.
AeRx nebulizer and   -   AERx™   ·USP 29                  Aradigm Corp.   -
APT's proprietary                (Hydroxychloroquine
formulation (US                  Sulfate) White or
6,572,858 )                      practically white,
                                 crystalline powder. Is
                                 odorless, and has a
                                 bitter taste. Its
                                 solutions have a pH of
                                 about 4.5. Exists in two
                                 forms, the usual form
                                 melting at about 240
                                 and the other form
                                 melting at about 198 .
                                 Freely soluble in water;
                                 practically insoluble in
                                 alcohol, in chloroform,
                                 and in ether.:
                                 hydroxychloroquine
                                 sulfate



-                    -   -       -                      -                 -
Developed as an      In Phase II, 60 mg of -    ·: pitrakinra   Aerovance, Inc.   -
inhaled dry powder   the drug was dosed
                     twice daily using an
                     undisclosed nebulizer
                     technology. [14378]
                     In Phase II trials, also
                     25 mgs s.c. once daily
                     for 28 days was
                     studied trials.In Phase
                     IIb study, a single 10
                     mg dose of Aerovant
                     inhalation powder was
                     administered.[44087].I
                     n Phase IIb trial,
                     Aerovant administered
                     at doses 1 mg, 3 mg
                     or 10 mg by inhalation
                     twice daily for 12
                     weeks. [53068]
AEROBID Inhaler is        Each activation           3M MDI Metering   ·USP 29 (Flunisolide) 3M Health Care   Year of US Approval:
delivered in a metered-   delivers approximately Valves               White to creamy-white,                 1984-08-17
dose aerosol system       250 mcg of flunisolide                      crystalline powder.                    Earliest US Market
containing a              to the patient. One                         Melts at about 245 ,                   Exclusivity: 2007-01-
microcrystalline          AEROBID Inhaler                             with decomposition.                    01
suspension of             System is designed to                       Practically insoluble in               Earliest Patent
flunisolide as the        deliver at least 100                        water; soluble in                      Exclusivity: 2007-06-
hemihydrate in            metered inhalations.                        acetone; sparingly                     12
propellants               Dose is two inhalations                     soluble in chloroform;
(trichloromonofluorom     twice daily. The                            slightly soluble in
ethane,                   maximum daily dose                          methanol.
dichlorodifluoromethan    should not exceed 4                         The octanol: water
e and                     inhalations twice a day                     partition coefficient is
dichlorotetrafluoroetha   for a total daily dose of                   2.17 at neutral pH.:
ne) with sorbitan         2 mg.                                       flunisolide
trioleate as a
dispersing agent.
AEROBID-M also
contains menthol as a
flavoring agent.
-   -   AeroDose™   ·USP 29 (Albuterol)      Nektar Therapeutics   -
                    White, crystalline
                    powder. Soluble in
                    alcohol, sparingly
                    soluble in water. Melts
                    at about 156 oC. n-
                    Octanol/Water
                    Partition Coefficient is
                    1.7 x 10 -3 at pH 7.
                    pKa=9.14. : albuterol
-   -   Aeroneb® Pro   ·Budesonide is a white Nektar Therapeutics   -
                       to off-white, odorless
                       powder that is
                       practically insoluble in
                       water and in heptane,
                       sparingly soluble in
                       ethanol, and freely
                       soluble in chloroform.
                       Its partition coefficient
                       between octanol and
                       water at pH 5 is 1.6 x
                       10.3 : budesonide
Inactive ingredients:   250 and 500   -           ·: ipratropium bromide Arrow                  -
sodium chloride,        microgram                 anhydrous              Pharmaceuticals Ltd.
hydrochloric acid




-                       -             AeroCell™   -                     AerovectRx Corp.        -
The product uses the   125, 250, 375, 500 mg Microcaps®·           ·USP 29                  Eurand N.V.   -
Company's              capsules              Diffucaps/Surecaps®   (Theophylline) White,
Microcaps® and                                                     odorless, crystalline
Diffucaps/Surecaps®                                                powder, having a bitter
tehnologies.                                                       taste. Is stable in air.
                                                                   Slightly soluble in
                                                                   water, but more
                                                                   soluble in hot water;
                                                                   freely soluble in
                                                                   solutions of alkali
                                                                   hydroxides and in
                                                                   ammonia; sparingly
                                                                   soluble in
                                                                   alcohol, in chloroform,
                                                                   and in ether.:
                                                                   theophylline

Each actuation         -                    -                      ·USP 29 (Albuterol)      GenPharm      -
contains 90 mcg                                                    White, crystalline
albuterol and CFC                                                  powder. Soluble in
propellants.                                                       alcohol, sparingly
                                                                   soluble in water. Melts
                                                                   at about 156 oC. n-
                                                                   Octanol/Water
                                                                   Partition Coefficient is
                                                                   1.7 x 10 -3 at pH 7.
                                                                   pKa=9.14. : albuterol
Microcrystalline         17 g canister for 200   -   ·USP 29 (Albuterol)      Teva Pharmaceutical   Year of US Approval:
albuterol, CFC           inhalations                 White, crystalline       Industries Ltd.       1995-12-28
propellants, and oleic                               powder. Soluble in
acid                                                 alcohol, sparingly
                                                     soluble in water. Melts
                                                     at about 156 oC. n-
                                                     Octanol/Water
                                                     Partition Coefficient is
                                                     1.7 x 10 -3 at pH 7.
                                                     pKa=9.14. : albuterol
Generic for Proventil   200 dose inhaler   -   ·USP 29 (Albuterol       Martec Pharmaceutical -
                                               Sulfate) White or        Inc.
                                               practically white
                                               powder. Freely soluble
                                               in water; slightly
                                               soluble in alcohol, in
                                               chloroform, and in
                                               ether. pKa=9.14.
                                               Solubility: 24.5% w/v at
                                               pH 7.: albuterol sulfate
Each actuation           Each canister provides -   ·USP 29 (Albuterol)      Barr Pharmaceuticals   Year of US Approval:
contains 90 mcg          200 inhalations.           White, crystalline       Inc.                   1996
microcrystalline         Dosed as two               powder. Soluble in
albuterol, oleic acid,   inhalations four times     alcohol, sparingly
and CFC propellants      daily                      soluble in water. Melts
                                                    at about 156 oC. n-
                                                    Octanol/Water
                                                    Partition Coefficient is
                                                    1.7 x 10 -3 at pH 7.
                                                    pKa=9.14. : albuterol
Mystic EHD nebulizer   -   Mystic™   ·USP 29 (Albuterol)      Ventaira   -
                                     White, crystalline
                                     powder. Soluble in
                                     alcohol, sparingly
                                     soluble in water. Melts
                                     at about 156 oC. n-
                                     Octanol/Water
                                     Partition Coefficient is
                                     1.7 x 10 -3 at pH 7.
                                     pKa=9.14. : albuterol
Generic for Proventil   -   -   ·USP 29 (Albuterol       DEY L.P.         Year of US Approval:
and Ventolin                    Sulfate) White or                         1992-02-21
                                practically white
                                powder. Freely soluble
                                in water; slightly
                                soluble in alcohol, in
                                chloroform, and in
                                ether. pKa=9.14.
                                Solubility: 24.5% w/v at
                                pH 7.: albuterol sulfate



Generic for Proventil   -   -   ·USP 29 (Albuterol       Wockhardt Ltd.   Year of US Approval:
and Ventolin                    Sulfate) White or                         1999-11-22
                                practically white
                                powder. Freely soluble
                                in water; slightly
                                soluble in alcohol, in
                                chloroform, and in
                                ether. pKa=9.14.
                                Solubility: 24.5% w/v at
                                pH 7.: albuterol sulfate
Generic for Proventil   Albuterol Sulfate          -   ·USP 29 (Albuterol       Nephron               Year of US Approval:
and Ventolin            Inhalation Solution,           Sulfate) White or        Pharmaceuticals Corp. 1997-09-17
                        0.042% is supplied as          practically white
                        a prediluted 3 mL,             powder. Freely soluble
                        clear, colorless, sterile,     in water; slightly
                        preservative-free,             soluble in alcohol, in
                        aqueous solution,              chloroform, and in
                        containing 1.25 mg of          ether. pKa=9.14.
                        albuterol (equivalent to       Solubility: 24.5% w/v at
                        1.5 mg albuterol               pH 7.: albuterol sulfate
                        sulfate in 3 mL), in unit-
                        dose lowdensity
                        polyethylene (LDPE)
                        vials. Each unit-dose
                        LDPE vial is protected
                        in a foil pouch.The
                        usual starting dosage
                        for patients 2 to 12
                        years of age is 1.25
                        mg of albuterol
                        administered 3 or 4
                        times daily by
                        nebulization.
-   Standard 0.5%           Aria   ·USP 29 (Albuterol       Chrysalis            -
    solution delivered with        Sulfate) White or        Technologies
    Aria device. MMAD              practically white
    approximately 3                powder. Freely soluble
    microns. (AAPS 2006            in water; slightly
    poster)                        soluble in alcohol, in
                                   chloroform, and in
                                   ether. pKa=9.14.
                                   Solubility: 24.5% w/v at
                                   pH 7.: albuterol sulfate



-   -                       -      -                      -                      -

-   10 and 20 mg tablets.   -      ·Water solubility 38 -                        -
                                   mg/mL (Sigma Aldrich
                                   catalog): epinastine
                                   hydrochloride

-   -                       -      ·: eculizumab          -                      -




-   -                       -      ·: eculizumab          Alexion                -
                                                          Pharmaceuticals Inc.
Excipients:              30, 60, 120 and 180     -   ·Fexofenadine             -   Year of US Approval:
croscarmellose           mg tablets.                 hydrochloride is a            2000-02-25
sodium, magnesium        Adults and Children 12      white to off-white            Earliest US Market
stearate,                Years and Older: The        crystalline powder. It is     Exclusivity: 2006-11-
microcrystalline         recommended dose is         freely soluble in             12
cellulose, and           60 mg twice daily, or       methanol and ethanol,         Earliest Patent
pregelatinized starch.   180 mg once daily.          slightly soluble in           Exclusivity: 2012-05-
The aqueous tablet       Children 6 to 11 Years.     chloroform and water,         11
film coating is made     The recommended             and insoluble in
from hydroxypropyl       dose is 30 mg twice         hexane.
methylcellu-lose, iron   daily.                      Fexofenadine
oxide blends,                                        hydrochloride is a
polyethylene glycol,                                 racemate and exists
povidone, silicone                                   as a zwitterion in
dioxide, and titanium                                aqueous media at
dioxide.                                             physiological pH.:
                                                     fexofenadine
                                                     hydrochloride
Aerosol formulation   -   -            -                     Allergica   -




-                     -   Novolizer®   ·A white, odourless,  Almirall    -
                                       hygroscopic,
                                       crystalline powder.
                                       Soluble in water;
                                       insoluble in alcohol
                                       and in chloroform.:
                                       sodium cromoglycate·:
                                       reproterol
The following not     Four times daily two   -          ·A white, odourless,  Meda AB         -
effective components spraying impacts.                  hygroscopic,
are contained in the                                    crystalline powder.
medicine: Apafluran,                                    Soluble in water;
Dentomint pH 799959,                                    insoluble in alcohol
Ethanol, Macrogol-25-                                   and in chloroform.:
glyceroltrioleat,                                       sodium cromoglycate·:
Saccharin sodium.                                       reproterol
(translated from
German). CFC-free




Established active     -                     PADD DPI   -                   Britannia         -
pharmaceutical                                                              Pharmaceuticals
ingredient delivered
with PADD inhaler
-   -   -   ·: alpha1-proteinase   -   -
            inhibitor, human
3M MDI Metering          Each inhalation         3M MDI Metering   ·USP 29                3M Health Care   Year of US Approval:
Valves technology.       delivers 650 mcg        Valves            (Metaproterenol                         1973-07-31
Inactive ingredients:    micronozed                                Sulfate) White to off-
sorbitan trioleate and   metaproterenol.                           white, crystalline
CFC propellants.         Available in 100 and                      powder. Freely soluble
                         200 inhalation                            in water.:
                         configurations.                           metaproterenol
                         Single dose is two or                     sulphate
                         three inhalations. With
                         repetitive dosing,
                         inhalation should
                         usually not be
                         repeated more often
                         than about every three
                         to four hours. Total
                         dosage per day should
                         not exceed 12
                         inhalations.
pH adjusted aqueous     10 mL or 30 mL         -   ·USP 29                Boehringer Ingelheim   Year of US Approval:
solution containing     bottles. Dosed every 4     (Metaproterenol                               1983-06-30
benzalkonium chloride   hours. Dose                Sulfate) White to off-
and edetate disodium    dependent on age.          white, crystalline
as preservatives.                                  powder. Freely soluble
                                                   in water.:
                                                   metaproterenol
                                                   sulphate
Generic for Alupent.   -   -   ·USP 29                DEY L.P.   Year of US Approval:
                               (Metaproterenol                   1987-08-17
                               Sulfate) White to off-
                               white, crystalline
                               powder. Freely soluble
                               in water.:
                               metaproterenol
                               sulphate
Generic for Alupent   -   -   ·USP 29                Wockhardt Ltd.   Year of US Approval:
                              (Metaproterenol                         2002-05-30
                              Sulfate) White to off-
                              white, crystalline
                              powder. Freely soluble
                              in water.:
                              metaproterenol
                              sulphate
Generic for Alupent   -   -   ·USP 29                Nephron               Year of US Approval:
                              (Metaproterenol        Pharmaceuticals Corp. 1988-07-14
                              Sulfate) White to off-
                              white, crystalline
                              powder. Freely soluble
                              in water.:
                              metaproterenol
                              sulphate
Clear and colourless    Once daily               3M MDI Metering         ·Ciclesonide is a white 3M Health Care         Market Launch Date
solution containing     solution.160 ug as       Valves· HFA-MDI         to yellow-white                                US: 2008-09-08Year
Norflurane (HFA-134a)   starting dose and dose   Ethanol Formulations·   powder, practically                            of US Approval: 2008-
and Ethanol,            can be reduced to 80     AEROCOUNT               insoluble in water and                         01-15
anhydrous.              ug.                                              freely                                         Year of EU Approval:
                                                                         soluble in ethanol and                         2004-04-16
                                                                         acetone: ciclesonide                           Year of Japan
                                                                                                                        Approval: 2007-04-18


-                       -                        -                       ·Ciclesonide is a white Nycomed                -
                                                                         to yellow-white
                                                                         powder, practically
                                                                         insoluble in water and
                                                                         freely
                                                                         soluble in ethanol and
                                                                         acetone:
                                                                         ciclesonide·White to
                                                                         yellow crystal slightly
                                                                         soluble in water.:
                                                                         formoterol
-                       -                        -                       -                      -                       -

MPDDS: controlled       75 and 120 mg            MPDDS                   ·(EP5.0) White or        Themis Laboratories   -
release pellets in      capsules. Once daily                             yellowish crystalline    Private Ltd.
capsules                                                                 powder. Sparingly
                                                                         soluble in water,
                                                                         soluble in methanol,
                                                                         practically insoluble in
                                                                         methylene chloride.:
                                                                         ambroxol
                                                                         hydrochloride
Formulated as dry   12 out-patients were     -   ·: andolast   Rottapharm   -
powder for          treated with a single
inhalation.         dose of andolast of 2,
                    4 and 8 mg by
                    inhalation using the
                    MIAT Monohaler
                    device (Ref 1).




-                   -                        -   -             -            -


-                   -                        -   -             -            -




-                   -                        -   -             -            -
Inhaled mannitol as a   Two FEV1 readings        -   ·USP 29 (Mannitol)       Pharmaxis Ltd.   -
biomarker for airway    are taken at the             White, crystalline
inflammation            beginning of the test        powder or free-flowing
                        and the average is           granules. Is odorless
                        recorded as the              and has a sweet taste.
                               s
                        patient’ BASELINE            Freely soluble in water;
                        FEV1. The patient will       soluble in alkaline
                        then be instructed to        solutions; slightly
                        use a simple dry             soluble in pyridine;
                        powder inhaler to            very slightly soluble in
                        inhale progressively         alcohol; practically
                        higher doses of dry          insoluble: mannitol
                        mannitol. After each
                        step the patient waits
                        for one minute and
                        then performs two
                        FEV1measurements.
                        The test is stopped
                        when a patient has a
                        greater than 10 per
                        cent drop in
                        FEV1compared to
                        their BASELINE FEV1.
                        This is a positive test,
                        which indicates the
                        presence of active
                        airway inflammation.
                        On average, the
                        procedure takes 10
                        minutes plus recovery
                        time for a positive test
                        and 25 minutes for a
                        negative test.
-   Features offer the     -   ·USP 29 (Zileuton)       -   -
    opportunity to develop     White to off-white
    a product candidate        powder.
    with a reduced tablet      It is a racemic mixture
    size or less frequent      (50:50) of R(+) and S(-
    dose administration        ) enantiomers. Zileuton
                               is a practically
                               odorless, white,
                               crystalline powder that
                               is soluble in methanol
                               and ethanol, slightly
                               soluble in acetonitrile,
                               and practically
                               insoluble in water and
                               hexane.: zileuton
Each metered             The initial dose for  Clickhaler   ·(EP5.0) A white or      Vectura Group Plc   -
actuation of 1.3 mg      patients with mild                 almost white,
contains 50 mcg of       asthma is 200 to 400               crystalline powder,
drug and delivers 45     micrograms per day;                practically insoluble in
mcg of drug. For other   this may be increased              water, freely soluble in
strengths of 100 mcg     to 800 micrograms per              acetone, sparingly
and 250 mcg, same        day if required.                   soluble in alcohol.
ratios hold.                                                It melts at about 210
Formulations contain                                        °C, with
lactose monohydrate                                         decomposition.:
                                                            beclomethasone
                                                            dipropionate




-                        -                     -            -                      -                     -
TwistHaler DPI.         Each delivered dose     TwistHaler   ·USP 29 (Mometasone Schering-Plough Corp.   Year of US Approval:
Inactive ingredients:   contains 200 or 400                  Furoate) White to off-                      2005-03-30
lactose anhydrous.      micrograms                           white powder. Melts at                      Earliest US Market
                        mometasone furoate.                  about 220, with                             Exclusivity: 2008-03-
                        Available in 14, 30, 60              decomposition.                              30
                        multiple dose                        Soluble in acetone and                      Earliest Patent
                        configurations. The                  in methylene chloride.:                     Exclusivity: 2012-06-
                        only approved dose for               mometasone furoate                          25
                        children 4 to 11 is 110
                        mcg (1 puff)
                        administered once
                        daily in the evening.
Clickhaler technology.     Each metered            Clickhaler   ·USP 29 (Albuterol)      Vectura Group Plc   Year of EU Approval:
95 mcg of drug in          actuation of 3 mg of                 White, crystalline                           1997-05-09
lactose monohydrate        inhalation powder                    powder. Soluble in
is delivered. Dose is 1-   contains 114                         alcohol, sparingly
2 puffs three to four      micrograms of                        soluble in water. Melts
times daily.               salbutamol sulphate                  at about 156 oC. n-
                           (95 micrograms                       Octanol/Water
                           salbutamol base) and                 Partition Coefficient is
                           delivers 110                         1.7 x 10 -3 at pH 7.
                           micrograms of                        pKa=9.14. : albuterol
                           salbutamol sulphate
                           (90 micrograms of
                           salbutamol base). er.

                           The maximum
                           recommended dose is
                           two inhalations three
                           or four times a day.
The inhaler             -   Asmair® /Assist        -   Bang and Olufsen     -
incorporates a single       Actuated Inhaler(TM)       Medicom AS
increment dose
counter which counts
back from 199 doses,
allowing the user to
track each single dose
taken. The device is
also equipped with a
special lever
mechanism requiring
50% less force to
release a dose, this is
especially important
for the elderly and
young children.



-                       -   Clickhaler             -   Vectura Group Plc    -

As a part of the        -   Eiffel SCF Technology· -   Telesso Technologies -
program, Eiffel             Xcelovair
Technologies supplies
a re-engineered and
modified asthma drug
to Meridica for testing
with their inhalation
device.


-                       -   -                      -   -                    -

-                       -   -                      -   -                    -

Mycobacterium vaccae -      -                      -   -                    -
technology
-   -   -   -   -   -
-   -   -   ·(EP5.0) A white,        -   -
            crystalline powder,
            very soluble in water,
            soluble in alcohol.
            Melting point: 134 °C
            to 136 °C.:
            proxyphylline·(EP5.0)
            White, crystalline
            powder or colourless
            crystals. Freely soluble
            in water, soluble in
            alcohol. mp: about 219
            °C.: ephedrine
            hydrochloride·USP 29
            (Phenobarbital) White,
            odorless, glistening,
            small crystals, or
            white, crystalline
            powder, which may
            exhibit polymorphism.
            Is stable in air. Its
            saturated solution has
            a pH of about 5. Very
            slightly soluble in
            water; soluble in
            alcohol, in ether, and
            in solutions of fixed
            alkali hydroxides and
            carbonates; sparingly
            soluble in chloroform.:
            phenobarbital
-   60 mL bottle          -   ·Procaterol               -   -
    containing 25 mcg/5       hydrochloride occurs
    mL procaterol HCl.        as white to pale yellow-
                              white crystals or
                              crystalline powder. It is
                              soluble in water, formic
                              acid and methanol,
                              slightly soluble in
                              ethanol (95), and
                              practically insoluble in
                              diethyl ether. The pH
                              of its aqueous solution
                              (1&#8594;100) is 4.0-
                              5.0. It
                              gradually changes in
                              color when exposed to
                              light. Its aqueous
                              solution (1&#8594;20)
                              shows no optical
                              rotation: procaterol
                              hydrochloride
-   25 and 50 mcg         -   ·Procaterol               -   -
    procaterol HCl            hydrochloride occurs
    containing tablets.       as white to pale yellow-
                              white crystals or
                              crystalline powder. It is
                              soluble in water, formic
                              acid and methanol,
                              slightly soluble in
                              ethanol (95), and
                              practically insoluble in
                              diethyl ether. The pH
                              of its aqueous solution
                              (1&#8594;100) is 4.0-
                              5.0. It
                              gradually changes in
                              color when exposed to
                              light. Its aqueous
                              solution (1&#8594;20)
                              shows no optical
                              rotation: procaterol
                              hydrochloride
Drug in capsule         Dark olive/light olive AeroHaler   ·White to off-white      Boehringer Ingelheim   Year of EU Approval:
containing glucose as   opaque size 3 hard                 crystalline substance,                          2006-01-13
carroer. Delivered by   gelatin capsules.                  freely soluble in water
Aeohaler device.        packaged in                        and lower alcohols. It
Capsule shell:          PVC/Aluminium blister              is a quaternary
Titanium dioxide        packs containing 30,               ammonium compound
(E171), Indigo          50, 60, 90, 100, 120,              and thus exists in an
Carmine (E132), Iron    180, 240, 300 or 360               ionized state in
Oxide Yellow (E172),    AEROCAPS. 1                        aqueous solutions. It is
Iron Oxide Black        capsule three or four              relatively insoluble in
(E172), Gelatin.        times daily. This dose             non-polar media.. The
                        may be doubled safely              pH of a 1% solution in
                        in patients who are                water is 5.0 to 7.5. :
                        less responsive. A                 ipratropium bromide
                        total daily dose of 8              hydrate
                        capsules should not be
                        exceeded.
3M MDI Metering         Each actuation meters 3M MDI Metering   ·White to off-white      3M Health Care   Year of US Approval:
Valves technology.      21 mcg of ipratropium Valves            crystalline substance,                    1986-12-29
Inactive ingredients:   bromide from the valve                  freely soluble in water                   Earliest US Market
soya lectin and CFC     and delivers 18 mcg of                  and lower alcohols. It                    Exclusivity: 2007-11-
propellants.            ipratropium bromide                     is a quaternary                           17
                        from the mouthpiece.                    ammonium compound                         Earliest Patent
                        Each 14.7 gram                          and thus exists in an                     Exclusivity: 2009-11-
                        canister provides                       ionized state in                          28
                        sufficient medication                   aqueous solutions. It is
                        for 200 inhalations.                    relatively insoluble in
                        Dosed in two                            non-polar media.. The
                        inhalations, four times                 pH of a 1% solution in
                        daily                                   water is 5.0 to 7.5. :
                                                                ipratropium bromide
                                                                hydrate
Atrovent Inhalation        Atrovent® (ipratropium -   ·White to off-white      Boehringer Ingelheim   Year of US Approval:
Solution is                bromide) Inhalation        crystalline substance,                          1993
administered by oral       Solution Unit Dose Vial    freely soluble in water                         Year of EU Approval:
inhalation with the aid    is                         and lower alcohols. It                          2003-03-01
of a nebulizer. It         supplied as a 0.02%        is a quaternary
contains ipratropium       clear, colorless           ammonium compound
bromide 0.02%              solution containing 2.5    and thus exists in an
(anhydrous basis) in a     ml with 5 Unit Dose        ionized state in
sterile, isotonic saline   Vials per pouch, 5         aqueous solutions. It is
solution, pH adjusted      pouches per carton         relatively insoluble in
to 3.4 (3 to 4) with       (NDC 0597-0080-62).        non-polar media.. The
hydrochloric acid.         The usual dosage of        pH of a 1% solution in
                           Atrovent® (ipratropium     water is 5.0 to 7.5. :
                           bromide) Inhalation        ipratropium bromide
                           Solution is 500 mcg (1     hydrate
                           Unit-Dose Vial)
                           administered three to
                           four times a day by
                           oral nebulization, with
                           doses 6 to 8 hours
                           apart.
-                    -   -   -                       -                 -




-                    -   -   -                       -                 -


-                    -   -   -                       -                 -

HFA formulation in   -   -   ·USP 29                  Sanofi-Aventis   -
MDI device with              (Triamcinolone
electronic dose              Acetonide) White to
counter                      cream-colored,
                             crystalline powder,
                             having not more than a
                             slight odor. Practically
                             insoluble in water;
                             sparingly soluble in
                             dehydrated alcohol, in
                             chloroform, and in
                             methanol.:
                             triamcinolone
                             acetonide
Microcrystalline         Device delivers 200      -   ·USP 29                  Abbott Laboratories   Year of US Approval:
suspension of drug       micrograms from valve        (Triamcinolone           Inc.                  1982-04-23
with                     and 75 micrograms            Acetonide) White to
dichlorofluoromethane    from mouthpiece after        cream-colored,
propellant and           initial prime of two         crystalline powder,
dehydrated alcohol 1%    actuations.                  having not more than a
w/w. each canister       Administered two             slight odor. Practically
contains 60 mg of drug   inhalations three to         insoluble in water;
capable of delivering    four times daily or four     sparingly soluble in
up to 240 actuations.    inhalations twice daily.     dehydrated alcohol, in
                                                      chloroform, and in
                                                      methanol.:
                                                      triamcinolone
                                                      acetonide
Modulite® technology      The usual starting    Modulite® technology   ·(EP5.0) A white or      Chiesi Farmaceutici   Year of EU Approval:
MDI CFC free              dose for 50                                  almost white,            SpA                   2006-06-29
propellant/formulation    micrograms, 100                              crystalline powder,
system based on the       micrograms & 200                             practically insoluble in
use of HFA                micrograms of BDP                            water, freely soluble in
propellants.Suspensio     Modulite is 200                              acetone, sparingly
n contains excipients :   micrograms twice                             soluble in alcohol.
ethanol, glycerol,        daily.For 250                                It melts at about 210
norflurane                micrograms of BDP                            °C, with
                          Modulate the usual                           decomposition.:
                          administration dosage                        beclomethasone
                          is 1000 micrograms                           dipropionate
                          daily, which may be
                          increased to 2000
                          micrograms daily.For
                          detailed information
                          please see EU label.
-                  inhalation solution     Respimat   -   Boehringer Ingelheim   -
                   delivered by the
                   Respimat,
                   administered once
                   daily as doses 50 µg,
                   100 µg and 200 µg in
                   phase 2 trials
-                  administered as         -          -   -                      -
                   subcutaneously
-                  inhalation solution     Respimat   -   Boehringer Ingelheim   -
                   delivered once daily as
                   5 and 10 mcg doses
                   by the Respimat in
                   phase 3 trials

Hard Capsule for   administered as 30mg HandiHaler    -   Boehringer Ingelheim   -
HandiHaler         twice daily in phase 2
                   trials
-                  At phase 2 trials      -           -   -                      -
                   patients received 0.1
                   mg/kg and 1.0 mg/kg
                   IV MEDI-563 on Study
                   Days 0 and 56.

-                  -                       -          -   -                      -
-                      -                 -                      -                        -          -




Lactose monohydrate;   10 and 20 mg      -                      ·(EP5.0) A white or      -          -
maize starch;          tablets.                                 almost white,
povidone;              Once daily                               crystalline powder,
microcrystalline       administration.                          freely soluble in water,
cellulose; magnesium                                            soluble in alcohol. It
stearate; water,                                                shows polymorphism.:
purified.                                                       bambuterol
                                                                hydrochloride




Drug nanoparticles     -                 Eiffel SCF Technology· -                        Ventaira   -
produced by                              Mystic™
Supercritical Fluid
(SCF) technology to be
tested with
BattellePharma’ s
MysticTM inhalation
delivery technology
Oleic Acid,            Each inhalation         Easi-Breathe   ·(EP5.0) A white or      Teva Pharmaceutical   Year of EU Approval:
dichlorodifluoromethan delivers 50, 100, or                   almost white,            Industries Ltd.       2000-09-28
e, and                 250 mcg of drug.                       crystalline powder,
trichlorofluoromethane                                        practically insoluble in
formualtion in Easi-                                          water, freely soluble in
breathe inhaler.                                              acetone, sparingly
                                                              soluble in alcohol.
                                                              It melts at about 210
                                                              °C, with
                                                              decomposition.:
                                                              beclomethasone
                                                              dipropionate


A mixture of 400       Double-foil disks        Diskhaler     ·(EP5.0) A white or      GlaxoSmithKline Plc   Year of EU Approval:
micrograms             comprising eight                       almost white,                                  2003-03-14
beclomethasone         regularly spaced                       crystalline powder,
dipropionate (as the   blisters each delivering               practically insoluble in
monohydrate) and       a mixture of 400                       water, freely soluble in
lactose, used in a     micrograms                             acetone, sparingly
Diskhaler device.      beclomethasone                         soluble in alcohol.
                       dipropionate (as the                   It melts at about 210
                       monohydrate) and                       °C, with
                       lactose                                decomposition.:
                                                              beclomethasone
                                                              dipropionate
EasyHaler DPI.        100 or 200 mcg/dose. EasyHaler   ·(EP5.0) A white or      Orion Corp.           -
Lactose monohydrate                                    almost white,
                                                       crystalline powder,
                                                       practically insoluble in
                                                       water, freely soluble in
                                                       acetone, sparingly
                                                       soluble in alcohol.
                                                       It melts at about 210
                                                       °C, with
                                                       decomposition.:
                                                       beclomethasone
                                                       dipropionate


-                     -                   CycloHaler   ·(EP5.0) A white or      Teva Pharmaceutical   -
                                                       almost white,            Industries Ltd.
                                                       crystalline powder,
                                                       practically insoluble in
                                                       water, freely soluble in
                                                       acetone, sparingly
                                                       soluble in alcohol.
                                                       It melts at about 210
                                                       °C, with
                                                       decomposition.:
                                                       beclomethasone
                                                       dipropionate
Oleic Acid,               50, 100 or 200          -   ·(EP5.0) A white or      Orion Corp.   Year of EU Approval:
dichlorodifluoromethan    micrograms                  almost white,                          1999-03-04
e,                        Beclometasone               crystalline powder,
trichlorofluoromethane.   Dipropionate BP per         practically insoluble in
                          actuation. Each             water, freely soluble in
                          canister delivers 80 or     acetone, sparingly
                          200 actuations.             soluble in alcohol.
                          Adults (including the       It melts at about 210
                          elderly): The usual         °C, with
                          starting dose is 200        decomposition.:
                          micrograms twice a          beclomethasone
                          day.                        dipropionate
                          Children: The usual
                          starting dose is 100
                          micrograms twice
                          daily
Respimat nebulizer    Each single dose unit Respimat   · A 4% solution in          Boehringer Ingelheim   Year of EU Approval:
device. Excipients:   contains Fenoterol               water has a pH of 4.2                              1993-06-09
Sodium chloride,      Hydrobromide Ph.Eur.             to 5.2. Protect from
Hydrochloric acid,    1.25 mg and                      light.
Purified water.       Ipratropium Bromide              (EP5.0) White,
                      Ph.Eur. 0.5 mg.                  crystalline powder.
                      The recommended                  Soluble in water and in
                      dose for adults and              alcohol.: fenoterol
                      children over 14 years           hydrobromide·White to
                      is one vial (4 ml) to be         off-white crystalline
                      nebulised immediately            substance, freely
                      upon presentation.               soluble in water and
                      Repeat dosing may be             lower alcohols. It is a
                      given at the discretion          quaternary ammonium
                      of the treating                  compound and thus
                      physician, up to a               exists in an ionized
                      maximum of 4 vials in            state in aqueous
                      24 hours.                        solutions. It is relatively
                                                       insoluble in non-polar
                                                       media.. The pH of a
                                                       1% solution in water is
                                                       5.0 to 7.5. :
                                                       ipratropium bromide
                                                       hydrate
Fenoterol solution in     0.625 and 0.25 mg/mL -    · A 4% solution in      Boehringer Ingelheim   -
20 mL bottles contains    vials, each mL of         water has a pH of 4.2
preservatives             aqueous solution          to 5.2. Protect from
(benzalkonium             contains 0.625 mg and     light.
chloride and edetate      0.25 mg fenoterol HBr     (EP5.0) White,
disodium) The 2 mL        repectively.              crystalline powder.
unit dose vial does not                             Soluble in water and in
contain preservatives.                              alcohol.: fenoterol
Nonmedicinal                                        hydrobromide
ingredients:
benzalkonium chloride
and edetate disodium
in an aqueous solution.
Sodium:




Berotec (100 µg) and      Berotec (100 µg) and -    · A 4% solution in      Boehringer Ingelheim   -
Berotec forte (200 µg)    Berotec forte (200 µg).   water has a pH of 4.2
are metered dose          The 100 ug cannister      to 5.2. Protect from
aerosol systems which     contains 200 doses        light.
contain a suspension      and the 200ug             (EP5.0) White,
of fenoterol HBr in       cannister(Forte)          crystalline powder.
fluorocarbon              contains 100 doses.       Soluble in water and in
propellants               Non-CFC versions          alcohol.: fenoterol
(difluorodichlorometha    available in many         hydrobromide
ne,                       countries
monofluorotrichlorome
thane,
tetrafluorodichloroetha
ne) with sorbitan
trioleate as a
dispersing agent.
CLICTM Lipids.          -       Lipids
                            CLIC™        -                     Inovio BioMedical      -
                                                               Corp.




P20-MTS recombinant -       -            -                     -                      -
fusion protein.




BiOral cochleate        -   Bioral       ·USP 29 (Amphotericin BioDelivery Sciences   -
technology. This is not                  B) Yellow to orange     International Inc.
SinuNase.                                powder; odorless or
                                         practically so.
                                         Insoluble in water, in
                                         anhydrous alcohol, in
                                         ether, in benzene, and
                                         in toluene; soluble in
                                         dimethylformamide, in
                                         dimethyl sulfoxide, and
                                         in propylene glycol;
                                         slightly soluble in
                                         methanol.:
                                         amphotericin B



-                       -   -            ·: mepolizumab        -                      -
Each milliliter of          1 mg/mL ampuls.      -       ·USP 29 (Terbutaline -     Year of US Approval:
solution contains 1 mg      The usual                    Sulfate) White to gray-    1981
of terbutaline sulfate      subcutaneous dose of         white, crystalline
USP (0.82 mg of the         Brethine is 0.25 mg.         powder. Is odorless or
free base), sodium                                       has a faint odor of
chloride for isotonicity,                                acetic acid. Soluble in
and hydrochloric acid                                    water and in 0.1 N
for adjustment to a                                      hydrochloric acid;
target pH of 4.                                          slightly soluble in
                                                         methanol; insoluble in
                                                         chloroform.: terbutaline
                                                         sulfate


-                           2.5 and 5 mg tablets.    -   ·USP 29 (Terbutaline -     Year of US Approval:
                            The usual dose is 5          Sulfate) White to gray-    1976
                            milligrams taken at          white, crystalline
                            approximately 6-hour         powder. Is odorless or
                            intervals, 3 times per       has a faint odor of
                            day during waking            acetic acid. Soluble in
                            hours.                       water and in 0.1 N
                                                         hydrochloric acid;
                                                         slightly soluble in
                                                         methanol; insoluble in
                                                         chloroform.: terbutaline
                                                         sulfate
Terbutaline (0.25 mg),      0.25mg/dose. One or -               ·USP 29 (Terbutaline AstraZeneca Plc   Year of US Approval:
sorbitan trioleate, CFC     two inhalations as                  Sulfate) White to gray-                1985-03-19
11,12, and 14. For          required, with a short              white, crystalline                     Year of EU Approval:
use with Bricanyl           interval between each               powder. Is odorless or                 2002-06-04
Inhaler, Bricanyl           inhalation at 6 hourly              has a faint odor of
Spacer Inhaler and          intervals. Discontinued             acetic acid. Soluble in
Nebuhaler                   in US (0.2 mg/INH)                  water and in 0.1 N
                                                                hydrochloric acid;
                                                                slightly soluble in
                                                                methanol; insoluble in
                                                                chloroform.: terbutaline
                                                                sulfate


Breath actuated             One inhalation (0.5mg) Turbuhaler   ·USP 29 (Terbutaline AstraZeneca Plc   Year of US Approval:
metered dose powder         as required. Not more               Sulfate) White to gray-                1985-03-19
inhaler. Each dose          than 4 inhalations                  white, crystalline                     Year of EU Approval:
contains 0.5 mg             should be required in               powder. Is odorless or                 2002-06-04
terbutaline sulphate        any 24-hour period.                 has a faint odor of
delivered using                                                 acetic acid. Soluble in
Turbohaler technology.                                          water and in 0.1 N
Each inhaler contains                                           hydrochloric acid;
100 doses. No                                                   slightly soluble in
additives, lubricants, or                                       methanol; insoluble in
preservatives added.                                            chloroform.: terbutaline
                                                                sulfate


-                           40 and 80 mg tablets.   -           ·: seratrodast       -                 -
                            Once daily.
Auto-Jethaler   -   Auto-Jethaler®   ·Budesonide is a white Pulmotec   Year of EU Approval:
                                     to off-white, odorless            2005
                                     powder that is
                                     practically insoluble in
                                     water and in heptane,
                                     sparingly soluble in
                                     ethanol, and freely
                                     soluble in chloroform.
                                     Its partition coefficient
                                     between octanol and
                                     water at pH 5 is 1.6 x
                                     10.3 : budesonide


Jethaler DPI.   -   Jethaler®        ·Budesonide is a white Pulmotec   -
                                     to off-white, odorless
                                     powder that is
                                     practically insoluble in
                                     water and in heptane,
                                     sparingly soluble in
                                     ethanol, and freely
                                     soluble in chloroform.
                                     Its partition coefficient
                                     between octanol and
                                     water at pH 5 is 1.6 x
                                     10.3 : budesonide
-   -   Airmax/Spriomax   ·Budesonide is a white Teva Pharmaceutical   -
                          to off-white, odorless Industries Ltd.
                          powder that is
                          practically insoluble in
                          water and in heptane,
                          sparingly soluble in
                          ethanol, and freely
                          soluble in chloroform.
                          Its partition coefficient
                          between octanol and
                          water at pH 5 is 1.6 x
                          10.3 : budesonide


-   -   Clickhaler        ·Budesonide is a white Vectura Group Plc     Year of EU Approval:
                          to off-white, odorless                       2005
                          powder that is
                          practically insoluble in
                          water and in heptane,
                          sparingly soluble in
                          ethanol, and freely
                          soluble in chloroform.
                          Its partition coefficient
                          between octanol and
                          water at pH 5 is 1.6 x
                          10.3 : budesonide
-                      -                      CycloHaler   ·Budesonide is a white Teva Pharmaceutical   -
                                                           to off-white, odorless Industries Ltd.
                                                           powder that is
                                                           practically insoluble in
                                                           water and in heptane,
                                                           sparingly soluble in
                                                           ethanol, and freely
                                                           soluble in chloroform.
                                                           Its partition coefficient
                                                           between octanol and
                                                           water at pH 5 is 1.6 x
                                                           10.3 : budesonide


A highly efficient      Supplied as a 120      SkyeFine    ·Budesonide is a white SkyePharma Plc        -
formulation involving a dose canister with 200             to off-white, odorless
70%(in vitro) increase ug per puff.                        powder that is
of fine particles                                          practically insoluble in
compared to the                                            water and in heptane,
currently marketed                                         sparingly soluble in
CFC-MDI. The                                               ethanol, and freely
formulation includes                                       soluble in chloroform.
HFA227/134a                                                Its partition coefficient
propellants,                                               between octanol and
budesonide, surfactant                                     water at pH 5 is 1.6 x
and CO2. Skyefine                                          10.3 : budesonide
Technology
Generic Pulmicort        0.25 mg/2 mL and 0.5 -            ·Budesonide is a white Teva Pharmaceutical   Market Launch Date
Respules                 mg/2 mL indicated for             to off-white, odorless Industries Ltd.       US: 2008-11-19Year
                         twice daily                       powder that is                               of US Approval: 2008-
                                                           practically insoluble in                     11-19
                                                           water and in heptane,
                                                           sparingly soluble in
                                                           ethanol, and freely
                                                           soluble in chloroform.
                                                           Its partition coefficient
                                                           between octanol and
                                                           water at pH 5 is 1.6 x
                                                           10.3 : budesonide


MMX matrix controlled    Cosmo is presently          MMX   ·Budesonide is a white Cosmo                 -
release delays           conducting two phase              to off-white, odorless Pharmaceuticals
absorption of drug for   III clinical trials, one in       powder that is            S.p.A.
colonic delivery         the Americas and one              practically insoluble in
                         in the EU. The US trial           water and in heptane,
                         is testing efficacy and           sparingly soluble in
                         safety of new oral                ethanol, and freely
                         Budesonide MMX™        9          soluble in chloroform.
                         mg and 6 mg extended-             Its partition coefficient
                         release tablet                    between octanol and
                         formulations                      water at pH 5 is 1.6 x
                         (CB-01-02) in patients            10.3 : budesonide
                         with mild or moderate,
                         active Ulcerative
                         Colitis.
Modulite technology      0.2 mg drug dose per   Modulite® technology   ·Budesonide is a white Chiesi Farmaceutici   Year of EU Approval:
uses HFA propellants actuation                                         to off-white, odorless SpA                   2003
in a drug solution with                                                powder that is
optimized particle size.                                               practically insoluble in
                                                                       water and in heptane,
                                                                       sparingly soluble in
                                                                       ethanol, and freely
                                                                       soluble in chloroform.
                                                                       Its partition coefficient
                                                                       between octanol and
                                                                       water at pH 5 is 1.6 x
                                                                       10.3 : budesonide
Mystic EHD nebulizer   -   Mystic™       ·Budesonide is a white Ventaira           -
                                         to off-white, odorless
                                         powder that is
                                         practically insoluble in
                                         water and in heptane,
                                         sparingly soluble in
                                         ethanol, and freely
                                         soluble in chloroform.
                                         Its partition coefficient
                                         between octanol and
                                         water at pH 5 is 1.6 x
                                         10.3 : budesonide


Powder-whirl           -   PowderWhirl   ·Budesonide is a white Direct-Haler A/S   -
                                         to off-white, odorless
                                         powder that is
                                         practically insoluble in
                                         water and in heptane,
                                         sparingly soluble in
                                         ethanol, and freely
                                         soluble in chloroform.
                                         Its partition coefficient
                                         between octanol and
                                         water at pH 5 is 1.6 x
                                         10.3 : budesonide
Inactive ingredients:   200 mcg salbutamol      Pulvinal   ·USP 29 (Albuterol)      Chiesi Farmaceutici   Year of EU Approval:
lactose monohydrate.    (albuterol) per dose.              White, crystalline       SpA                   2001
                        Dose not to exceed 4               powder. Soluble in
Dose not to exceed 4    per day.                           alcohol, sparingly
per day                                                    soluble in water. Melts
                                                           at about 156 oC. n-
                                                           Octanol/Water
                                                           Partition Coefficient is
                                                           1.7 x 10 -3 at pH 7.
                                                           pKa=9.14. : albuterol
Inactive ingredients:   (salbutamol           -   ·USP 29 (Albuterol)      Orion Corp.   -
lactose monohydrate     inhalation powder 100     White, crystalline
                        and 200 mcg/dose          powder. Soluble in
                                                  alcohol, sparingly
                                                  soluble in water. Melts
                                                  at about 156 oC. n-
                                                  Octanol/Water
                                                  Partition Coefficient is
                                                  1.7 x 10 -3 at pH 7.
                                                  pKa=9.14. : albuterol


-                       At phase 1 study, 150 -   -                       -              -
                        mg and 300 mg
                        subcutaneous
                        administration
                        compared with 150 mg
                        IV administration
                        (trials). Phase 2
                        dosing: 1 mg/kg CAT-
                        354 on Day 0, 28, and
                        56 5 mg/kg CAT-354
                        on Day 0, 28, and 56
                        10 mg/kg CAT-354 on
                        Day 0, 28, and
                        56(trials)
-                  Phase 2 trials used      -                    ·: apremilast   -                     -
                   doses varied between
                   10, 20, 30, 40 mg
                   tablets, once or twice a
                   day.
                   The pilot, open-label,
                   single arm phase II
                   study enrolled 19
                   patients with 15
                   patients having
                   complete sets of
                   evaluable biopsies and
                   17 patients evaluable
                   for complete efficacy
                   assessments. CC-
                   10004 at 20mg was
                   administered daily for
                   29 days with an
                   additional 28-day
                   observational follow-up
                   period to monitor
                   safety [6764].


-                  -                        -                    -               -                     -


Modulite HFA MDI   Phase 2 trials dosage; Modulite® technology   ·: carmoterol   Chiesi Farmaceutici   -
                   carmoterol 1.0                                                SpA
                   &#956;g, 2.0 &#956;g,
                   4.0 &#956;g once a
                   day, in the morning
-                        -                       -   ·:                        Chiesi Farmaceutici   -
                                                     carmoterol·Budesonid SpA
                                                     e is a white to off-
                                                     white, odorless powder
                                                     that is practically
                                                     insoluble in water and
                                                     in heptane, sparingly
                                                     soluble in ethanol, and
                                                     freely soluble in
                                                     chloroform. Its partition
                                                     coefficient between
                                                     octanol and water at
                                                     pH 5 is 1.6 x 10.3 :
                                                     budesonide


Inhalation formulation   -                       -   -                       -                       -


Inactive ingredient:     It is supplied as white -   ·Fudosteine is white to -                       Year of Japan
Corn starch, talc,       film-coated tablet.         pale yellow white                               Approval: 2001-12-01
magnesium stearate,      Usually 400 mg as           crystal                                         Market Launch Date
hydroxypropylmethylce    fudosteine is orally        or crystalline powder. It                       Japan: 2001-12-01
llulose,                 administered to adults      is very soluble in
titanium oxide,          3 times a day after         formic
macrogol                 meals.                      acid, freely soluble in
                                                     water, slightly soluble
                                                     4 Mitsubishi Pharma
                                                     Corporation in acetic
                                                     acid (100), very slightly
                                                     soluble in ethanol (95)
                                                     and practically
                                                     insoluble in
                                                     diethylether.:
                                                     fudosteine
A novel modified oral -                      Collegium Liquid   -                     Collegium             -
formulation (liquid,                         Modified Release                         Pharmaceuticals
extended release) of a
product used for the
treatment of asthma.

-                     Dry powder formula for -                  ·: tofimilast         Pfizer Inc.           -
                      inhalation

LVT derivative of     -                      Lipid Vector       ·USP 29                 Clavis Pharma ASA   -
betamethasone                                Technology (LVT)   (Betamethasone)
                                                                White to practically
                                                                white, odorless,
                                                                crystalline powder.
                                                                Melts at about 240 ,
                                                                with some
                                                                decomposition.
                                                                Insoluble in water;
                                                                sparingly soluble in
                                                                acetone, in alcohol, in
                                                                dioxane, and in
                                                                methanol; very slightly
                                                                soluble in chloroform
                                                                and in ether.:
                                                                betamethasone
LVT derivative of   -                      Lipid Vector       ·USP 29                 Clavis Pharma ASA   -
prednisolone                               Technology (LVT)   (Prednisolone) White
                                                              to practically white,
                                                              odorless, crystalline
                                                              powder. Melts at about
                                                              235, with some
                                                              decomposition. Very
                                                              slightly soluble in
                                                              water; soluble in
                                                              methanol
                                                              and in dioxane;
                                                              sparingly soluble in
                                                              acetone and in alcohol;
                                                              slightly soluble in
                                                              chloroform.
                                                              (EP5.0) It shows
                                                              polymorphism.:
                                                              prednisolone


-                   Compound's             -                  -                     -                     -
                    pharmacokinetic
                    properties allow once-
                    a-day oral dosing.




-                   -                      -                  -                     -                     -

-                   -                      -                  -                     -                     -
-   Novel once-nightly     -   ·USP 29                 CombinatoRx Inc.   -
    modified release co-       (Prednisolone) White
    formulation capsule        to practically white,
                               odorless, crystalline
                               powder. Melts at about
                               235, with some
                               decomposition. Very
                               slightly soluble in
                               water; soluble in
                               methanol
                               and in dioxane;
                               sparingly soluble in
                               acetone and in alcohol;
                               slightly soluble in
                               chloroform.
                               (EP5.0) It shows
                               polymorphism.:
                               prednisolone·:
                               nortriptyline
-   -   -   ·USP 29                 -   -
            (Prednisolone) White
            to practically white,
            odorless, crystalline
            powder. Melts at about
            235, with some
            decomposition. Very
            slightly soluble in
            water; soluble in
            methanol
            and in dioxane;
            sparingly soluble in
            acetone and in alcohol;
            slightly soluble in
            chloroform.
            (EP5.0) It shows
            polymorphism.:
            prednisolone·:
            nortriptyline
-   -                      -   ·Bromelain is a mixture -   -
                               of sulfur-containing
                               protein-digesting
                               enzymes—  called
                               proteolytic enzymes or
                                          and
                               proteases— several
                               other substances in
                               smaller quantities. The
                               two main enzymes are:
                               stem bromelain and
                               fruit bromelain:
                               bromelains




-   CVT-6883, a selective, -   -                       -   -
    potent and orally
    available A2B-
    adenosine receptor
    antagonist, intended to
    treat asthma with once
    a day dosing [20373]
-   In a phase IIa pilot    -   -   -   -
    study the 10 patients
    received 6 weekly
    injections of 300
    &#956;g CYT003-
    QbG10 [9187]
-   Product is the           -   -   -   -
    combination of 300µg
    QbG10 with an
    approved allergen
    extract. In open-label,
    single arm phase IIa
    study, at the first two
    weekly visits, the
    allergen was injected
    subcutaneously and up-
    titrated. Thereafter, at
    the next 4
    weekly visits, allergen
    was further up-titrated,
    but now co-
    administered
    subcutaneously with
    300 &#956;g CYT005-
    AllQbG10. Finally, at
    an additional two
    biweekly visits, 300
    &#956;g CYT005-
    AllQbG10 were
    coadministered
    with the highest
    targeted allergen dose
    [20410]
1mg and 30mg tablets:    1, 6 and 30 mg tablets. -                  ·: deflazacort        -                       Year of EU Approval:
Microcrystalline         For acute disorders,                                                                     2008-08-06
cellulose, lactose,      up to 120 mg/day
maize starch and         deflazacort may need
magnesium stearate.      to be given initially.
6mg tablets:             Maintenance doses in
Microcrystalline         most conditions are
cellulose, lactose,      within the range 3 - 18
sucrose, maize starch    mg/day.
and magnesium
stearate.




Contain 2-10%            The solution is         CAPTISOL®· eFlow   ·Budesonide is a white CyDex                  -
Captisol. Doses of 60,   nebulized with a                           to off-white, odorless Pharmaceuticals, Inc
120 and 240              modified Pari e-flow                       powder that is
microgram per 0.5 mL     nebulizer.                                 practically insoluble in
delivered in Pahse I.                                               water and in heptane,
US2007197487                                                        sparingly soluble in
                                                                    ethanol, and freely
                                                                    soluble in chloroform.
                                                                    Its partition coefficient
                                                                    between octanol and
                                                                    water at pH 5 is 1.6 x
                                                                    10.3 : budesonide
-   -   -   -   -   -




-   -   -   -   -   -
-   -   -   -   -   -




-   -   -   -   -   -

-   -   -   -   -   -
Inactive ingredients:      400 mg and 600 mg      -   ·USP 29 (Oxtriphylline) Pfizer Inc.       Year of US Approval:
carnauba wax,              extended release           White, crystalline                        1983-05-24
hydrogenated soybean       tablets. One 400 or        powder, having an
oil, magnesium             600 mg tablet every 12     amine-like odor. A
stearate and sugar;        hours.                     solution (1 in 100) has
coating: candelilla wax,                              a pH of about 10.3.
hydroxypropyl                                         Freely soluble in water
cellulose, opaseal,                                   and in alcohol; very
opaspray pink and talc.                               slightly soluble in
                                                      chloroform.:
                                                      oxtriphylline




-                          400 mg and 600 mg      -   ·: choline theophylline   Galenica S.A.   -
                           sustained release
                           tablets.

-                          -                      -   ·Ciclesonide is a white Nycomed           -
                                                      to yellow-white
                                                      powder, practically
                                                      insoluble in water and
                                                      freely
                                                      soluble in ethanol and
                                                      acetone: ciclesonide
-   -   -   ·: cintredekin   NeoPharm Inc.   -
            besudotox
Nanosteroids are a       -                       LTT PLA         -                       LTT Bio-Pharma Co      -
drug delivery system in                          Nanoparticles                           Ltd
which steroids are
inserted into a
polylactic acid particle
with a width of only
150 nanometres.

Pulvinal technology.     100, 200, 400 mcg       Pulvinal        ·(EP5.0) A white or      Chiesi Farmaceutici   Year of EU Approval:
Inactive ingredients:    beclomethasone                          almost white,            SpA                   2006-06-29
lactose monohydrate,     dipropionate. Dosed                     crystalline powder,
magnesium stearate.      two to four times daily                 practically insoluble in
                                                                 water, freely soluble in
                                                                 acetone, sparingly
                                                                 soluble in alcohol.
                                                                 It melts at about 210
                                                                 °C, with
                                                                 decomposition.:
                                                                 beclomethasone
                                                                 dipropionate
Combivent Inhalation      Two inhalations four   -   ·White to off-white      Boehringer Ingelheim   Year of US Approval:
Aerosol contains a        times a day.               crystalline substance,                          1996-10-24
microcrystalline          Combivent® Inhalation      freely soluble in water                         Earliest US Market
suspension of             Aerosol is supplied as     and lower alcohols. It                          Exclusivity: 2015-01-
ipratropium bromide       a metered-dose             is a quaternary                                 01
and albuterol             inhaler with a white       ammonium compound                               Earliest Patent
sulfate in a              mouthpiece which has       and thus exists in an                           Exclusivity: 2015-06-
pressurized metered-      a clear, colorless         ionized state in                                09
dose aerosol unit for     sleeve and an orange       aqueous solutions. It is                        Year of EU Approval:
oral inhalation           protective cap.            relatively insoluble in                         1994-03-22
administration. The                                  non-polar media.. The
200 inhalation unit has                              pH of a 1% solution in
a net weight of 14.7                                 water is 5.0 to 7.5. :
grams. Each actuation                                ipratropium bromide
meters 21 mcg of                                     hydrate·USP 29
ipratropium bromide                                  (Albuterol Sulfate)
and 120 mcg of                                       White or practically
albuterol sulfate from                               white powder. Freely
the valve and delivers                               soluble in water;
18 mcg of ipratropium                                slightly soluble in
bromide and 103 mcg                                  alcohol, in chloroform,
of albuterol sulfate                                 and in ether.
(equivalent to 90 mcg                                pKa=9.14. Solubility:
albuterol base) from                                 24.5% w/v at pH 7.:
the mouthpiece. The                                  albuterol sulfate
excipients are
dichlorodifluoromethan
e,
dichlorotetrafluoroetha
ne, and
trichloromonofluorome
thane as propellants
and soya lecithin.
Formoterol 12µg and     -   -            ·White to yellow crystal Novartis AG   -
24µg delivered by a                      slightly soluble in
new inhalation device                    water.: formoterol
(Concept1) (source:
clinicaltrials.gov
NCT00443482)
-                       -   Contramid®   ·Levosalbutamol, the Labopharm Inc.    -
                                         R(-)-enantiomer of
                                         salbutamol. It is a
                                         white to off-white,
                                         crystalline solid, with a
                                         melting point of
                                         approximately 187° C
                                         and solubility of
                                         approximately 180
                                         mg/mL in water.
                                         Levalbuterol is the (R)-
                                         enantiomer of the drug
                                         substance racemic
                                         albuterol.

                                         : levalbuterol
                                         hydrochloride
PARI's eFlow           -   eFlow   ·USP 29 (Lidocaine)      Pari Pharma GmbH   -
electronic nebulizer               White or slightly
(Ventaira's Mystic was             yellow, crystalline
also studied)                      powder. Has a
                                   characteristic odor and
                                   is stable in air.
                                   Practically insoluble in
                                   water; very soluble in
                                   alcohol and in
                                   chloroform; freely
                                   soluble in benzene and
                                   in ether. Dissolves in
                                   oils.
                                   (EP5.0) Melting point:
                                   66 °C to 70 °C,
                                   determined without
                                   previous drying.:
                                   lidocaine
-   5 mg/dose   Easi-Breathe   ·Cromolyn Sodium:          Teva Pharmaceutical   -
                               White, odorless,           Industries Ltd.
                               crystalline powder. Is
                               tasteless at first, with a
                               slightly bitter after
                               taste. Is hygroscopic.
                               Soluble in water;
                               insoluble in alcohol
                               and in chloroform.
                               (Cromolyn Sodium for
                               Inhalation) White to
                               creamy white,
                               odorless, hygroscopic,
                               and very finely divided
                               powder.: cromolyn
                               sodium
Utilizes one of the   -    -         ·Cromolyn Sodium:          Durect Corporation   -
Company's proprietary                White, odorless,
biodegradable drug                   crystalline powder. Is
delivery platforms                   tasteless at first, with a
                                     slightly bitter after
                                     taste. Is hygroscopic.
                                     Soluble in water;
                                     insoluble in alcohol
                                     and in chloroform.
                                     (Cromolyn Sodium for
                                     Inhalation) White to
                                     creamy white,
                                     odorless, hygroscopic,
                                     and very finely divided
                                     powder.: cromolyn
                                     sodium




Mystic EHD nebulizer   -   Mystic™   ·Cromolyn sodium is a Ventaira                  -
                                     water soluble,
                                     odorless, white,
                                     hydrated crystalline
                                     powder. It is tasteless
                                     at first, but leaves a
                                     slightly bitter
                                     aftertaste.: cromolyn
-                      -                      -            -                      -                   -

-                      -                      -            -                      -                   -

-                      -                      -            -                      Dr. Reddys          -
                                                                                  Laboratories Ltd.
-                      -                      -            -                      -                   -




-                      In the RECORD study -               ·: roflumilast         -                   -
                       patients were treated
                       for 24 weeks with
                       either placebo or
                       250µg or 500 µg
                       Roflumilast. Once
                       daily. [11395]
Diffutab based.          100, 200, 350 mg once Diffutab®   ·USP 29                  Eurand N.V.       -
Excipients: HPMC and a day tablets                         (Theophylline) White,
shellac, calcium                                           odorless, crystalline
phosphate dibasic,                                         powder, having a bitter
calcium phosphate                                          taste. Is stable in air.
tribasic, magnesium                                        Slightly soluble in
stearate, precipitated                                     water, but more
silica. (translated from                                   soluble in hot water;
Italian)                                                   freely soluble in
                                                           solutions of alkali
                                                           hydroxides and in
                                                           ammonia; sparingly
                                                           soluble in
                                                           alcohol, in chloroform,
                                                           and in ether.:
                                                           theophylline
-   -   -   -   -   -
Each white film-coated   For oral use, the usual -   ·Ozagrel hydrochloride -    Year of Japan
tablets 100 mg and       adult dosage is 400         occurs as in the form       Approval: 1992-06-01
200 mg DOMENAN           mg of ozagrel               of white crystals or a
Tablets contains 100     hydrochloride (four 100     crystalline powder. It is
mg and 200 mg of         mg tablets or two 200       odorless but has an
ozagrel hydrochloride.   mg tablets) in two          acidic and bitter taste.
For 100 mg tablet        divided doses (after        It is freely soluble in
Lactose,                 breakfast and before        methanol, soluble in
Microcrystalline         bed-time). The              water, sparingly
cellulose,               dosage                      soluble in ethanol (95),
Hydroxypropyl            may be adjusted             and practically
cellulose,Magnesium      according to the            insoluble in acetone or
stearate, Macrogol,             s
                         patient’ age and            diethyl ether.: ozagrel
Polyoxyethylene          symptoms                    hydrochloride
polyoxypropylene
glycol, for 200 mg
tablet Lactose,
Microcrystalline
cellulose,
Hydroxypropyl
cellulose,
Magnesium
stearate,
Hydroxypropylmethylc
ellulose,
Polyoxyethylene
polyoxypropylene
glycol are inactive
ingredients.
-                    -   -                      -   -                     -




Undisclosed fixed    -   DuoHaler(C200)         -   Vectura Group Plc     -
dose comination in
DuoHaler device
Undisclosed fixed    -   DuoHaler(C200)         -   Vectura Group Plc     -
dose comination in
DuoHaler device
-                    -   Modulite® technology   -   Chiesi Farmaceutici   -
                                                    SpA




-                    -   -                      -   Enanta                -
                                                    Pharmaceuticals
-   -            -   -                      Enanta                  -
                                            Pharmaceuticals




-   once daily   -   ·This entery is used as Epigenesis             -
                     a place holder in the   Pharmaceuticals Inc.
                     database for NCE or
                     undisclosed small
                     molecules. It is
                     required to be used in
                     some cases (e.g.
                     combination products)
                     in order for charts and
                     statistics to function
                     properly.: undisclosed
                     small molecule·This
                     entery is used as a
                     place holder in the
                     database for NCE or
                     undisclosed small
                     molecules. It is
                     required to be used in
                     some cases (e.g.
                     combination products)
                     in order for charts and
                     statistics to function
                     properly.: undisclosed
                     small molecule
-                       Oral treatment   -                      -   -                    -




As part of the program, -                Eiffel SCF Technology· -   Telesso Technologies -
Eiffel Technologies                      Oriel DPI
supplies a
reengineered and
modified asthma drug
to Oriel for testing with
their inhalation device.
Eligen technology   -   Eligen&#8482   ·Cromolyn Sodium:          Emisphere            -
                                       White, odorless,           Technologies, Inc.
                                       crystalline powder. Is
                                       tasteless at first, with a
                                       slightly bitter after
                                       taste. Is hygroscopic.
                                       Soluble in water;
                                       insoluble in alcohol
                                       and in chloroform.
                                       (Cromolyn Sodium for
                                       Inhalation) White to
                                       creamy white,
                                       odorless, hygroscopic,
                                       and very finely divided
                                       powder.: cromolyn
                                       sodium
Epinephrine Mist is         Delivers 0.22 mg        -   ·USP 29 (Epinephrine) Amphastar                  Year of US Approval:
generic and National        epinephrine per             White to practically      Pharmaceuticals Inc.   1984-05-23
Brand Equivalent            inhalation. Epinephrine     white, odorless,
(NBE) product to            Mist products are           microcrystalline
Primatene Mist®.            available in a ½ fl oz      powder or granules,
Inactive ingredients:       (15mL) Kit (with            gradually darkening on
alcohol 34%, ascorbic       mouthpiece), and ½ fl       exposure to light and
acid, fluorocarbons         oz (15mL) refill            air. With acids, it forms
(propellant),               (without mouthpiece).       salts that are readily
hydrochloric acid, nitric                               soluble in water, and
acid, water.                                            the base may be
                                                        recovered by the
                                                        addition of ammonia
                                                        water or alkali
                                                        carbonates. Its
                                                        solutions are alkaline
                                                        to litmus. Very slightly
                                                        soluble in water and in
                                                        alcohol; insoluble in
                                                        ether, in chloroform,
                                                        and in fixed and
                                                        volatile oils.
                                                        (Epinephrine Injection)
                                                        Practically colorless,
                                                        slightly acid liquid.
                                                        Gradually turns dark
                                                        on exposure to light
                                                        and air.
                                                        (Epinephrine Inhalation
                                                        Solution) Practically
                                                        colorless, slightly acid
                                                        liquid. Gradually turns
                                                        dark on exposure to
                                                        light and air.
Euphyllin Retard® is a   It is supplied as light  -   ·USP 29                  Nycomed   -
delayed release          blue, convex, oblong,        (Theophylline) White,
formulation of           scored, film coated          odorless, crystalline
anhydrous theophylline   tablets.                     powder, having a bitter
                         Adults: Generally, one       taste. Is stable in air.
                         tablet taken twice a         Slightly soluble in
                         day (every 10-12             water, but more
                         hours) after meals,          soluble in hot water;
                         preferably with some         freely soluble in
                         water. Depending             solutions of alkali
                         upon the effect              hydroxides and in
                         achieved and in severe       ammonia; sparingly
                         cases one tablet can         soluble in
                         be administered 3            alcohol, in chloroform,
                         times a day (at              and in ether.:
                         intervals of 8 hours, or     theophylline
                         half tablets can be
                         added to the dosage.
                         As a general guideline
                         the average daily
                         dosage can be given
                         as 10-14 mg/kg body
                         mass/day.
-                      Once daily intravenous -   ·USP 29                  -   -
                       administration             (Theophylline) White,
                                                  odorless, crystalline
                                                  powder, having a bitter
                                                  taste. Is stable in air.
                                                  Slightly soluble in
                                                  water, but more
                                                  soluble in hot water;
                                                  freely soluble in
                                                  solutions of alkali
                                                  hydroxides and in
                                                  ammonia; sparingly
                                                  soluble in
                                                  alcohol, in chloroform,
                                                  and in ether.:
                                                  theophylline

Alchemia's proprietary -                      -   -                        -   -
VAST™ drug discovery
technology with
Euroscreen's expertise
in GPCR screening



-                      -                      -   -                        -   -
-   -   -   -   -   -




-   -   -   -   -   -
Fixed dose            -   Modulite® technology   ·(EP5.0) A white or      Chiesi Farmaceutici   Year of EU Approval:
combination product                              almost white,            SpA                   2006
using Modulite HFA                               crystalline powder,
MDI technology                                   practically insoluble in
                                                 water, freely soluble in
                                                 acetone, sparingly
                                                 soluble in alcohol.
                                                 It melts at about 210
                                                 °C, with
                                                 decomposition.:
                                                 beclomethasone
                                                 dipropionate· A white
                                                 or almost white or
                                                 slightly yellow powder.
                                                 Slightly soluble in
                                                 water and in isopropyl
                                                 alcohol; practically
                                                 insoluble in
                                                 acetonitrile; soluble in
                                                 methyl alcohol. A 0.1%
                                                 solution in water has a
                                                 pH of 5.5 to 6.5.
                                                 Protect from light.:
                                                 formoterol fumarate




-                     -   -                      -                       -                      -
Each double foil          50, 100, 250 and 500   Diskhaler   ·(EP5.0) White or        GlaxoSmithKline Plc   Year of EU Approval:
rotadisk contains 4       mcg flutacasone                    almost white powder.                           1993-02-25
blisters with 50, 100,    propionate blended                 Practically insoluble in
250 and 500 mcg           with lactose to a                  water, sparingly
flutacasone propionate    weight of 25 mg.                   soluble in methylene
blended with lactose to   Administered twice                 chloride, slightly
a weight of 25 mg.        daily.                             soluble in alcohol.:
Contents are inhaled                                         fluticasone propionate
twice daily using
DiskHaler.



NonSpil(TM) liquid    5 mg/5 mL and 15     -                 ·USP 29 (Prednisolone Taro Pharmaceutical      Year of US Approval:
drug delivery system, mg/5 mL prednisolone                   Acetate) White to        Industries Ltd.       2008-01-22
taste masking formula solution                               practically white,
has a cherry flavor.                                         odorless, crystalline
                                                             powder. Melts at about
                                                             235, with some
                                                             decomposition.
                                                             Practically insoluble in
                                                             water; slightly soluble
                                                             in
                                                             acetone, in alcohol,
                                                             and in chloroform.:
                                                             prednisolone acetate
Pressurized, metered-      44, 110 and 220 mcg    -                  ·(EP5.0) White or        GlaxoSmithKline Plc   Year of US Approval:
dose aerosol units         inhalation aerosols.                      almost white powder.                           1996-03-27
intended for oral          Twice daily                               Practically insoluble in
inhalation only. Each      administration.                           water, sparingly
unit contains a                                                      soluble in methylene
microcrystalline                                                     chloride, slightly
suspension of                                                        soluble in alcohol.:
fluticasone propionate                                               fluticasone propionate
(micronized) in CFC
propellants It contains
no other excipients.



Specially designed         Flovent diskus 0.05,   Diskus/AccuHaler   ·(EP5.0) White or        GlaxoSmithKline Plc   Year of US Approval:
plastic devices            0.1, 0.25 mg.                             almost white powder.                           2000-09-29
containing a double foil   Administered twice                        Practically insoluble in                       Earliest US Market
blister. Each blister      daily.                                    water, sparingly                               Exclusivity: 2011-01-
contains 50, 100, 250                                                soluble in methylene                           01
mcg of drug blended                                                  chloride, slightly                             Earliest Patent
with lactose to a                                                    soluble in alcohol.:                           Exclusivity: 2011-03-
weight of 12.5 mg.                                                   fluticasone propionate                         01
Contents are inhaled
twice daily using
DISKUS device. 50
mcg inhaler supplied
with a dose counter.
Pressurised inhalation,    44 micrograms, 110  -   ·(EP5.0) White or        GlaxoSmithKline Plc   Year of US Approval:
suspensions,               micrograms, and 220     almost white powder.                           2004-05-14
delivering either 44,      micrograms inhalers     Practically insoluble in                       Earliest US Market
110 or 220                 dosed twice daily       water, sparingly                               Exclusivity: 2009-02-
micrograms of                                      soluble in methylene                           28
fluticasone per                                    chloride, slightly                             Earliest Patent
actuation, respectively.                           soluble in alcohol.:                           Exclusivity: 2012-12-
                                                   fluticasone propionate                         04
HFA 134a propellant.                                                                              Year of EU Approval:
44 mcg dose is                                                                                    2000-06-27
available with a dose
counter.
-                       -   -            ·: fluasterone          -           -




Miat-Haler, multidose   -   Miat-Haler   ·(EP5.0) White or        Miat Spa   -
DPI.                                     almost white powder.
                                         Practically insoluble in
                                         water, sparingly
                                         soluble in methylene
                                         chloride, slightly
                                         soluble in alcohol.:
                                         fluticasone propionate
HFA based MDI            -                       Skyepharma HFA        ·White to yellow crystal SkyePharma Plc   Company Estimated
formulation of fixed                             Formulations· SkyeDry slightly soluble in                       Launch Date: 2010-01-
dose formoterol and                                                    water.:                                   01
fluticasone. Product                                                   formoterol·(EP5.0)
includes a dose                                                        White or almost white
counter.                                                               powder. Practically
                                                                       insoluble in water,
                                                                       sparingly soluble in
                                                                       methylene chloride,
                                                                       slightly soluble in
                                                                       alcohol.: fluticasone
                                                                       propionate




Foradil Aerolizer is a   Individual capsules     -                     · A white or almost      Novartis AG      Year of US Approval:
single-dose dry          packaged in foil                              white or slightly yellow                  2001-02-16
powder inhaler. Each     blisters. Taken twice                         powder. Slightly                          Earliest US Market
capsule contains 12      daily (morning and                            soluble in water and in                   Exclusivity: 2006-02-
mcg of formoterol and    evening)                                      isopropyl alcohol;                        16
25 mg of lactose for                                                   practically insoluble in                  Earliest Patent
use with Aerolizer                                                     acetonitrile; soluble in                  Exclusivity: 2019-03-
inhaler. (US6488027).                                                  methyl alcohol. A 0.1%                    08
                                                                       solution in water has a                   Year of EU Approval:
                                                                       pH of 5.5 to 6.5.                         2003-03-20
                                                                       Protect from light.:
                                                                       formoterol fumarate
AirMax DPI   -   Airmax/Spriomax   · A white or almost      Teva Pharmaceutical   -
                                   white or slightly yellow Industries Ltd.
                                   powder. Slightly
                                   soluble in water and in
                                   isopropyl alcohol;
                                   practically insoluble in
                                   acetonitrile; soluble in
                                   methyl alcohol. A 0.1%
                                   solution in water has a
                                   pH of 5.5 to 6.5.
                                   Protect from light.:
                                   formoterol fumarate
Certihaler is a novel,     FORADIL®                SkyeHaler DPI·   · A white or almost      SkyePharma Plc   Year of US Approval:
breath-activated multi-    CERTIHALER®             SkyeProtect™     white or slightly yellow                  2006-12-15
dose dry powder            contains a powder                        powder. Slightly                          Earliest US Market
inhaler technology         formulation of                           soluble in water and in                   Exclusivity: 2009-12-
developed by               formoterol fumarate                      isopropyl alcohol;                        15
SkyePharma. Contains       intended for oral                        practically insoluble in                  Year of EU Approval:
60 doses. The device       inhalation only. Each                    acetonitrile; soluble in                  2004
provides patients          actuation of FORADIL                     methyl alcohol. A 0.1%
confirmation that the      CERTIHALER delivers                      solution in water has a
full dose has been         approximately 8.5 mcg                    pH of 5.5 to 6.5.
administered.              of formoterol fumarate                   Protect from light.:
Embodies two               from the mouthpiece                      formoterol fumarate
proprietary                (based on in vitro
SkyePharma                 testing at 60 L/min for
technologies, the          2 sec), corresponding
SKYEHALER breath-          to a metered dose of
actuated multi-dose        10 mcg of formoterol
dry powder inhaler         fumarate. Twice daily
device and                 administration
SKYEPROTECT, a
powder formulation
that protects the drug
from atmospheric
moisture to ensure
product stability and
dose-to-dose
reproducibility. Foradil
currently marketed as
a single dose DPI.
Excipients: Lactose
monohydrate (which
contains trace levels of
milk proteins) and
magnesium stearate.
NOVOLIZER         6 and 12 microgram   Novolizer®     ·White to yellow crystal Almirall         -
technology        doses                               slightly soluble in
                                                      water.: formoterol




Skyeprotect HFA   -                    SkyeProtect™   · A white or almost      SkyePharma Plc   -
formulation                                           white or slightly yellow
                                                      powder. Slightly
                                                      soluble in water and in
                                                      isopropyl alcohol;
                                                      practically insoluble in
                                                      acetonitrile; soluble in
                                                      methyl alcohol. A 0.1%
                                                      solution in water has a
                                                      pH of 5.5 to 6.5.
                                                      Protect from light.:
                                                      formoterol fumarate
Modulite HFA MDI   each actuation        Modulite® technology   · A white or almost      Chiesi Farmaceutici   Year of EU Approval:
                   provides 12 microgram                        white or slightly yellow SpA                   2004
                   drug                                         powder. Slightly
                                                                soluble in water and in
                                                                isopropyl alcohol;
                                                                practically insoluble in
                                                                acetonitrile; soluble in
                                                                methyl alcohol. A 0.1%
                                                                solution in water has a
                                                                pH of 5.5 to 6.5.
                                                                Protect from light.:
                                                                formoterol fumarate



Powderwhirl        -                     PowderWhirl            · A white or almost      Direct-Haler A/S      -
                                                                white or slightly yellow
                                                                powder. Slightly
                                                                soluble in water and in
                                                                isopropyl alcohol;
                                                                practically insoluble in
                                                                acetonitrile; soluble in
                                                                methyl alcohol. A 0.1%
                                                                solution in water has a
                                                                pH of 5.5 to 6.5.
                                                                Protect from light.:
                                                                formoterol fumarate



-                  -                     -                      ·White to yellow crystal Miat Spa              -
                                                                slightly soluble in
                                                                water.: formoterol
NEXT DPI   Phase II trials daily   NEXT DPI   ·(EP5.0) A white or      Chiesi Farmaceutici   -
           dosages are 400/24                 almost white,            SpA
           µg and 100/6 µg                    crystalline powder,
                                              practically insoluble in
                                              water, freely soluble in
                                              acetone, sparingly
                                              soluble in alcohol.
                                              It melts at about 210
                                              °C, with
                                              decomposition.:
                                              beclomethasone
                                              dipropionate· A white
                                              or almost white or
                                              slightly yellow powder.
                                              Slightly soluble in
                                              water and in isopropyl
                                              alcohol; practically
                                              insoluble in
                                              acetonitrile; soluble in
                                              methyl alcohol. A 0.1%
                                              solution in water has a
                                              pH of 5.5 to 6.5.
                                              Protect from light.:
                                              formoterol fumarate
Miat-Haler, multidose    -          Miat-Haler   ·Budesonide is a white Miat Spa               -
DPI                                              to off-white, odorless
                                                 powder that is
                                                 practically insoluble in
                                                 water and in heptane,
                                                 sparingly soluble in
                                                 ethanol, and freely
                                                 soluble in chloroform.
                                                 Its partition coefficient
                                                 between octanol and
                                                 water at pH 5 is 1.6 x
                                                 10.3 : budesonide


-                        -          -            -                       -                     -


Phase II studies utilize -          -            ·: oglemilast           -                     -
a once-daily-dosing
regimen.

-                        -          -            -                       -                     -




Pulmonary delivery       -          -            -                       GlaxoSmithKline Plc   -


Undisclosed inhalation Once daily   -            ·It has a beige solid   Theravance Inc.       -
technology (DPI or                               appearance.: MABA
MDI)
Novel dry powder     The long duration of   -                       ·: darotropium bromide GlaxoSmithKline Plc    -
inhaler (Source:     action of GSK233705
clinicaltrials.gov   when administered via
NCT00783003)         inhalation in animal
                     models supports the
                     potential for use as a
                     once-daily
                     bronchodilator for
                     chronic obstructive
                     pulmonary disease.
                     trials


-                    -                        -                     -                      Theravance Inc.        -


DPI assumed to be    In Phase II study           Diskus/AccuHaler   ·Fluticasone furoate is GlaxoSmithKline Plc   -
Diskus inhaler       started October 2008,                          a white powder with a
                     GW685698X is being                             molecular weight of
                     dosed 200mcg once                              538.6, and the
                     daily or 100mcg twice                          empirical
                     daily. (clinicaltrials.gov,                    formula is
                     NCT00766090).In                                C27H29F3O6S. It is
                     Phase 2b trial, a range                        practically insoluble in
                     of eight doses (25 ?                           water.: fluticasone
                     800 mcg)of                                     furoate
                     GW685698X was
                     administered.[51771]
GW642444M and          In separate phase 2b -    ·Fluticasone furoate is GlaxoSmithKline Plc   -
GW685698X will be      studies assessing         a white powder with a
simultaneously co-     efficacy and safety of    molecular weight of
administered from a          s
                       GSK’ inhaled              538.6, and the
single device trials   corticosteroid (ICS)      empirical
                       fluticasone furoate (FF   formula is
                       or GW685698) eight        C27H29F3O6S. It is
                       doses (25 – 800 mcg) in   practically insoluble in
                       over 1,800 patients       water.: fluticasone
                       with mild, moderate       furoate
                       and severe asthma
                       were treated [51747].




-                      -                     -   -                      -                      -
-                      -                     -   -                     -             -


Generic for Atrovent   250 mcg/mL. Supplied -    ·White to off-white      GenPharm   -
                       as a 20 mL clear          crystalline substance,
                       colorless solution        freely soluble in water
                       containing 0.025%         and lower alcohols. It
                       ipratropium bromide in    is a quaternary
                       isotonic solution         ammonium compound
                       preserved with            and thus exists in an
                       benzalkonium chloride     ionized state in
                       0.025% and disodium       aqueous solutions. It is
                       edetate 0.05% in an       relatively insoluble in
                       amber glass bottle with   non-polar media.. The
                       screw cap.                pH of a 1% solution in
                                                 water is 5.0 to 7.5. :
                                                 ipratropium bromide
                                                 hydrate
Ipratropium nebules.   1 or 2 mL of clear       -   ·White to off-white      GenPharm   -
Generic for Atrovent   colorless solution           crystalline substance,
                       containing 0.025%            freely soluble in water
                       ipratropium bromide in       and lower alcohols. It
                       isotonic solution,           is a quaternary
                       presented in plastic         ammonium compound
                       single use vial. Each        and thus exists in an
                       vial contains,               ionized state in
                       respectively, a total of     aqueous solutions. It is
                       250 or 500 mcg               relatively insoluble in
                       ipratropium bromide.         non-polar media.. The
                                                    pH of a 1% solution in
                                                    water is 5.0 to 7.5. :
                                                    ipratropium bromide
                                                    hydrate
Generic for Ventolin   5 mg/mL in bottles of   -   ·USP 29 (Albuterol       GenPharm   -
Resp. Solution         10 mL.                      Sulfate) White or
                                                   practically white
                                                   powder. Freely soluble
                                                   in water; slightly
                                                   soluble in alcohol, in
                                                   chloroform, and in
                                                   ether. pKa=9.14.
                                                   Solubility: 24.5% w/v at
                                                   pH 7.: albuterol sulfate



Generic for Ventolin   2.5 or 5 mg solution    -   ·USP 29 (Albuterol       GenPharm   -
Nebules                supplied in 2.5 mL          Sulfate) White or
                       translucent nebules.        practically white
                                                   powder. Freely soluble
                                                   in water; slightly
                                                   soluble in alcohol, in
                                                   chloroform, and in
                                                   ether. pKa=9.14.
                                                   Solubility: 24.5% w/v at
                                                   pH 7.: albuterol sulfate



-                      -                       -   -                     -             -
-   -   -   ·Budesonide is a white Apotex   Year of US Approval:
            to off-white, odorless          2009-03-30
            powder that is
            practically insoluble in
            water and in heptane,
            sparingly soluble in
            ethanol, and freely
            soluble in chloroform.
            Its partition coefficient
            between octanol and
            water at pH 5 is 1.6 x
            10.3 : budesonide
Equivalent to   100 mcg drug twice   -   ·Budesonide is a white Orion Corp.   -
Turbohaler      daily.                   to off-white, odorless
                                         powder that is
                                         practically insoluble in
                                         water and in heptane,
                                         sparingly soluble in
                                         ethanol, and freely
                                         soluble in chloroform.
                                         Its partition coefficient
                                         between octanol and
                                         water at pH 5 is 1.6 x
                                         10.3 : budesonide
-   -   EasyHaler   ·Budesonide is a white Orion Corp.   -
                    to off-white, odorless
                    powder that is
                    practically insoluble in
                    water and in heptane,
                    sparingly soluble in
                    ethanol, and freely
                    soluble in chloroform.
                    Its partition coefficient
                    between octanol and
                    water at pH 5 is 1.6 x
                    10.3 :
                    budesonide·White to
                    yellow crystal slightly
                    soluble in water.:
                    formoterol
-   -   Novolizer®   ·USP 29                  Almirall         -
                     (Glycopyrrolate) White,
                     odorless, crystalline
                     powder. Soluble in
                     water and in alcohol;
                     practically insoluble in
                     chloroform and in
                     ether. Unlike atropine,
                     glycopyrrolate is
                     completely ionized at
                     physiological pH
                     values. The partition
                     coefficient of
                     glycopyrrolate in a n-
                     octanol/water system
                     is 0.304 (log10 P= -
                     1.52) at ambient room
                     temperature (24°C).:
                     glycopyrrolate bromide




-   -   -            -                        Genentech Inc.   -
-                      -   -           -                       -           -




HFA formulation of a   -   Inyx MDIs   ·This entery is used as Inyx Inc.   -
corticosteroid and a                   a place holder in the
beta-2-agonist.                        database for NCE or
                                       undisclosed small
                                       molecules. It is
                                       required to be used in
                                       some cases (e.g.
                                       combination products)
                                       in order for charts and
                                       statistics to function
                                       properly.: undisclosed
                                       small molecule·This
                                       entery is used as a
                                       place holder in the
                                       database for NCE or
                                       undisclosed small
                                       molecules. It is
                                       required to be used in
                                       some cases (e.g.
                                       combination products)
                                       in order for charts and
                                       statistics to function
                                       properly.: undisclosed
                                       small molecule
-   -   -   -   -   -


-   -   -   -   -   -
Each HOKUNALIN          HOKUNALIN Tapes          -   ·Tulobuterol occurs as Nitto Denko Corp.   Year of Japan
Tapes 0.5mg, 1 mg       are drug-in-adhesive         white crystals or                          Approval: 1998-12-01
and 2 mg contains 0,5   patches containing           crystalline powder. It is
mg , 1 mg and 2 mg of   0.5, 1 and 2 mg              odorless. It is very
tulobuterol             tulobuterol for              soluble in methanol,
respectively.           transdermal delivery to      freely soluble in
Polyisobutylene,        be worn before use.          ethanol (95), acetic
Polybutene, Alicyclic   It is attached on the        acid (100), diethylether
saturated hydrocarbon   skin of chest, back or       or isopropylether,
resin are excipients.   upper arm once a day.        sparingly soluble in
                        For adults,                  hexane and practically
                        HOKUNALIN Tape               insoluble in water. It
                        2mg (2mg of                  has no optical rotation:
                        tulobuterol) is applied.     tulobuterol
                        For children from 6
                        months to less than 3
                        years of age,
                        HOKUNALIN Tape
                        0.5mg (0.5mg of
                        tulobuterol) is applied.
                        For children from 3 to
                        less than 9 years of
                        age, HOKUNALIN
                        Tape 1mg (1mg of
                        tulobuterol) is applied.
                        For children of 9 years
                        of age and older,
                        HOKUNALIN Tape
                        2mg (2mg of
                        tulobuterol) is applied.




-                       -                        -   -                     -                    -
-   -   -   -   -   -


-   -   -   -   -   -


-   -   -   -   -   -


-   -   -   -   -   -


-   -   -   -   -   -




-   -   -   -   -   -
IL13-PE38QQR is a          IL13-PE38QQR is          NeoPharm Tumor   ·: cintredekin   NeoPharm Inc.   -
targeted molecule          administered directly to Targeting        besudotox
composed of two            brain tumors through
parts: a tumor-            positive-pressure
targeting molecule         convection-enhanced
(IL13) and a cytotoxic     delivery. The
agent (PE38). IL13         anticancer agent is
receptors are found on     delivered continuously
malignant glioma cells,    by infusion (0.25
but not to any             ug/mL or 0.5 ug/mL)
measurable degree, if      infused over 96 hours.
at all, on healthy brain
cells. Cintredekin
besudotox is designed
to bind to IL13
receptors on the
tumor.




-                          -                     -                   -                -               -

-                          -                     -                   -                -               -
-   -               -   ·: anrukinzumab         -                  -


-   -               -   ·USP 29 (Nadolol)        Inverseon, Inc.   -
                        White to off-white,
                        practically odorless,
                        crystalline powder.
                        Freely soluble in
                        alcohol and in
                        methanol; soluble in
                        water at pH 2; slightly
                        soluble in chloroform,
                        in methylene chloride,
                        in isopropyl alcohol,
                        and in water (between
                        pH 7 and pH 10);
                        insoluble in acetone, in
                        benzene, in ether, in
                        hexane, and in
                        trichloroethane.:
                        nadolol



-   50 and 100 mg   -   ·: suplatast tosilate   -                  -
    capsules
-   5% dry syrup            -   ·: suplatast tosilate   -                     -




-   Phase IIb dosing: 20    -   -                       -                     -
    mg once daily [5070].




-   -                       -   -                       -                     -




-   -                       -   ·Soluble in water :     Shire Pharmaceuticals -
                                icatibant               Group PLC




-   -                       -   -                       -                     -
-                  administered as doses -                      ·Budesonide is a white Boehringer Ingelheim   -
                   of 400mcg                                    to off-white, odorless
                                                                powder that is
                                                                practically insoluble in
                                                                water and in heptane,
                                                                sparingly soluble in
                                                                ethanol, and freely
                                                                soluble in chloroform.
                                                                Its partition coefficient
                                                                between octanol and
                                                                water at pH 5 is 1.6 x
                                                                10.3 : budesonide


Nektar pulmonary   -                     Nektar Pulmonary      -                        Nektar Therapeutics   -
delivery system                          Inhaler
-                  -                     Next Safety Pulmonary ·USP 29 (Albuterol       Next Safety, Inc.     -
                                         Delivery              Sulfate) White or
                                                               practically white
                                                               powder. Freely soluble
                                                               in water; slightly
                                                               soluble in alcohol, in
                                                               chloroform, and in
                                                               ether. pKa=9.14.
                                                               Solubility: 24.5% w/v at
                                                               pH 7.: albuterol sulfate



-                  -                     -                      -                      Dynavax Technologies -
                                                                                       Corp.
Inactive ingredient:   20 mg/ml metered-        -   ·Cromolyn Sodium:          Astellas Pharma Inc.   Year of Japan
Povidone               dose spray type              White, odorless,                                  Approval: 2000-09-01
Macrogol 600           aerosol unit.                crystalline powder. Is
1,1,1,2,3,3,3,-        Inhale a dose of two         tasteless at first, with a
heptafluoropropane     sprays (2 mg as              slightly bitter after
(HFA-227)              sodium                       taste. Is hygroscopic.
                       cromoglicate)                Soluble in water;
                       four times daily             insoluble in alcohol
                       (morning, noon,              and in chloroform.
                       evening and at               (Cromolyn Sodium for
                       bedtime).                    Inhalation) White to
                       When the symptoms            creamy white,
                       have been alleviated,        odorless, hygroscopic,
                       the dosage should            and very finely divided
                       be reduced to two to         powder.: cromolyn
                       three times daily under      sodium
                       careful observation
                                     s
                       of the patient’ clinical
                       condition.
-   20 mg light orange     -   ·Cromolyn Sodium:          -   Year of Japan
    transparent/colorless      White, odorless,               Approval: 1971-06-01
    transparent, hard          crystalline powder. Is
    capsules.                  tasteless at first, with a
    Bronchial asthma: The      slightly bitter after
    product should be          taste. Is hygroscopic.
    inhaled in a dose of 1     Soluble in water;
    capsule                    insoluble in alcohol
    (20 mg as sodium           and in chloroform.
    cromoglicate), 3 to 4      (Cromolyn Sodium for
    times daily                Inhalation) White to
    (morning, noon and         creamy white,
    before sleeping, or        odorless, hygroscopic,
    morning,                   and very finely divided
    noon, evening and          powder.: cromolyn
    before sleeping) with      sodium
    an inhaling
    instrument for the
    exclusive use of this
    product.
    When the symptoms
    have been alleviated,
    the dosage
    should be reduced to 2
    to 3 capsules daily
    under
    careful observation of
                s
    the patient’ clinical
    condition.
    Allergic rhinitis: The
    product should be
    inhaled to each nasal
    cavity in
    a dose of 1 capsule
HFA based MDI   -   Inyx MDIs   ·Cromolyn Sodium:          Inyx Inc.   -
                                White, odorless,
                                crystalline powder. Is
                                tasteless at first, with a
                                slightly bitter after
                                taste. Is hygroscopic.
                                Soluble in water;
                                insoluble in alcohol
                                and in chloroform.
                                (Cromolyn Sodium for
                                Inhalation) White to
                                creamy white,
                                odorless, hygroscopic,
                                and very finely divided
                                powder.: cromolyn
                                sodium
Inactive ingredients:   Each dose contains 5 -    ·Cromolyn Sodium:          3M Health Care   Year of US Approval:
sorbitan trioleate,     mg cromolyn sodium.       White, odorless,                            1985-12-05
macrogal 600, CFC       Each 8.1 g canister       crystalline powder. Is
propellants.            delivers at least 112     tasteless at first, with a
                        metered inhalations       slightly bitter after
                        (56 doses); each 14.2     taste. Is hygroscopic.
                        g canister delivers at    Soluble in water;
                        least 200 metered         insoluble in alcohol
                        inhalations (100          and in chloroform.
                        doses). Two               (Cromolyn Sodium for
                        inhalations, four times   Inhalation) White to
                        daily                     creamy white,
                                                  odorless, hygroscopic,
                                                  and very finely divided
                                                  powder.: cromolyn
                                                  sodium
Clear, colorless (or     Each 2 mL ampule        -   ·Cromolyn Sodium:          Sanofi-Aventis   Year of US Approval:
very pale), sterile      contains 20 mg              White, odorless,                            1982-05-28
solution for             cromolyn sodium,            crystalline powder. Is                      Year of Japan
nebulization. Contains   USP, in purified water.     tasteless at first, with a                  Approval: 1982-11-01
1% w/w active and        Dose four times daily.      slightly bitter after
purified water.                                      taste. Is hygroscopic.
                                                     Soluble in water;
                                                     insoluble in alcohol
                                                     and in chloroform.
                                                     (Cromolyn Sodium for
                                                     Inhalation) White to
                                                     creamy white,
                                                     odorless, hygroscopic,
                                                     and very finely divided
                                                     powder.: cromolyn
                                                     sodium
Generic for Intal       2 mL vials containing   -   ·Cromolyn Sodium:          DEY L.P.   Year of US Approval:
inhalation Solutions.   20 mg drug                  White, odorless,                      1994-04-26
Drug in purified water.                             crystalline powder. Is
                                                    tasteless at first, with a
                                                    slightly bitter after
                                                    taste. Is hygroscopic.
                                                    Soluble in water;
                                                    insoluble in alcohol
                                                    and in chloroform.
                                                    (Cromolyn Sodium for
                                                    Inhalation) White to
                                                    creamy white,
                                                    odorless, hygroscopic,
                                                    and very finely divided
                                                    powder.: cromolyn
                                                    sodium
Generic for Intal      10 mg/mL   -   ·Cromolyn Sodium:          Morton Grove           Year of US Approval:
inhalation Solutions                  White, odorless,           Pharmaceuticals Inc.   1999-10-25
                                      crystalline powder. Is
                                      tasteless at first, with a
                                      slightly bitter after
                                      taste. Is hygroscopic.
                                      Soluble in water;
                                      insoluble in alcohol
                                      and in chloroform.
                                      (Cromolyn Sodium for
                                      Inhalation) White to
                                      creamy white,
                                      odorless, hygroscopic,
                                      and very finely divided
                                      powder.: cromolyn
                                      sodium
20 mg of micronized       Sodium Cromoglicate   SpinHaler   ·Cromolyn Sodium:          Sanofi-Aventis   Year of EU Approval:
cromyln sodium in         20.0 mg. The normal               White, odorless,                            1997-05-30
hard gelatin capsule      dose is one Spincap               crystalline powder. Is
for use in Spinhaler or   four times daily                  tasteless at first, with a
other capsule based                                         slightly bitter after
DPI device.                                                 taste. Is hygroscopic.
                                                            Soluble in water;
                                                            insoluble in alcohol
                                                            and in chloroform.
                                                            (Cromolyn Sodium for
                                                            Inhalation) White to
                                                            creamy white,
                                                            odorless, hygroscopic,
                                                            and very finely divided
                                                            powder.: cromolyn
                                                            sodium
Inactive ingredients:   Each dose contains    -   ·Cromolyn Sodium:          Sanofi-Aventis   -
povidone, macrogal      5mg cromolyn sodium.      White, odorless,
600, heptafluro         Two inhalations, four     crystalline powder. Is
propane non-CFC         times daily.              tasteless at first, with a
propellant.                                       slightly bitter after
                                                  taste. Is hygroscopic.
                                                  Soluble in water;
                                                  insoluble in alcohol
                                                  and in chloroform.
                                                  (Cromolyn Sodium for
                                                  Inhalation) White to
                                                  creamy white,
                                                  odorless, hygroscopic,
                                                  and very finely divided
                                                  powder.: cromolyn
                                                  sodium
-   -   CycloHaler   ·White to off-white      Teva Pharmaceutical   -
                     crystalline substance, Industries Ltd.
                     freely soluble in water
                     and lower alcohols. It
                     is a quaternary
                     ammonium compound
                     and thus exists in an
                     ionized state in
                     aqueous solutions. It is
                     relatively insoluble in
                     non-polar media.. The
                     pH of a 1% solution in
                     water is 5.0 to 7.5. :
                     ipratropium bromide
                     hydrate
-   250 micrograms/ ml,         -   ·White to off-white      Galen Limited   -
    500 micrograms /                crystalline substance,
    2ml.                            freely soluble in water
                                    and lower alcohols. It
    20 or 40 micrograms             is a quaternary
    three or four times             ammonium compound
    daily is the usual UK           and thus exists in an
    dose and it may be up           ionized state in
    to 80 micrograms as a           aqueous solutions. It is
    single dose. The daily          relatively insoluble in
    dose should not                 non-polar media.. The
    exceed 216                      pH of a 1% solution in
    micrograms (12                  water is 5.0 to 7.5. :
    inhalations). In children       ipratropium bromide
    aged 6 to 12 years the          hydrate
    usual dose is 20 or 40
    micrograms three
    times daily, and below
    6 years the usual dose
    is 20 micrograms three
    times daily.
-   1% isotonic solution           eFlow   ·A white, odourless,   Pari Pharma GmbH   -
                                           hygroscopic,
                                           crystalline powder.
                                           Soluble in water;
                                           insoluble in alcohol
                                           and in chloroform.:
                                           sodium cromoglycate




-   -                              -       -                      -                  -

-   -                              -       -                      -                  -




-   In the phase II/III            -       ·: tipelukast          -                  -
    interstitial cystitis trial,
    patients were given
    500mg MN-001 once
    or twice a day for 8
    weeks [15029].

    In the Phase III
    Asthma trial patients
    were to receive
    placebo or MN-001
    (750 mg BID, 500 mg
    TID) for 12 weeks.
ICS/LABA               -   KOS MDI technology   ·This entery is used as Abbott Laboratories   -
Combination                                     a place holder in the   Inc.
                                                database for NCE or
                                                undisclosed small
                                                molecules. It is
                                                required to be used in
                                                some cases (e.g.
                                                combination products)
                                                in order for charts and
                                                statistics to function
                                                properly.: undisclosed
                                                small molecule·This
                                                entery is used as a
                                                place holder in the
                                                database for NCE or
                                                undisclosed small
                                                molecules. It is
                                                required to be used in
                                                some cases (e.g.
                                                combination products)
                                                in order for charts and
                                                statistics to function
                                                properly.: undisclosed
                                                small molecule




ICS molecule in Aero   -   KOS MDI technology   -                      Abbott Laboratories    -
Device MDI                                                             Inc.
-                      -   -                    -                      -                      -


-                      -   -                    -                      -                      -
-   -                        -   -                        -   -

-   In the Phase Ib clinical -   ·: bedoradrine sulfate   -   -
    trial volunteers
    received a single-dose
    intravenous infusion
    regimen of MN-221,
    consisting of two
    consecutive rounds of
    a 15-minute priming
    and a 105-minute
    maintenance infusion
    to deliver 294
    micrograms of MN-221
    over four hours.
    [23946]
    The Phase IIa study
    for treatment of status
    asthmaticus achieved
    statistical significance
    in its primary endpoint
    of mean change in
    FEV1 (forced
    expiratory volume in 1
    second) from baseline
    at 15 minutes (the end
    of the infusion) at
    doses of 10, 16, 30
    and 60
    micrograms/min of MN-
    221 (p less than or
    equal to 0.0006).
    [26230]
    In Phase II trial, MN-
    221 administered 16
    micrograms/min for 15
-                      -                      -          -                       -               -




-                      10 mg capsules.        -          ·White crystalline      -               Year of Japan
                       Asthma: 10 mg twice               powder, Odorless.                       Approval: 1989-05-01
                       daily. Cerebrovascular            Very soluble in
                       disorders: 10 mg three            methanol or
                       times daily.                      chloroform, freely
                                                         soluble in acetic
                                                         anhydride or ethanol or
                                                         ether and very slightly
                                                         soluble in water.:
                                                         ibudilast
-                      -                      -          -                       Endacea, Inc.   -

-                      -                      -          -                       -               -

-                      -                      -          -                       -               -

-                      -                      Genuair®   -                       Almirall        -

Almirall intends to     Once daily            Genuair®   -                       Almirall        -
further develop this
compound with the
same proprietary
inhaler device used for
aclidinium bromide
(Genuair device).
[35230]
-                      -                      -          -                       -               -
-   Supplied as 0.25 gram -   -   -   -
    tablets

-   -                     -   -   -   -
Geoclock formulation. 1 mg, 2 mg, and 5 mg Geolock   ·USP 29 (Prednisone) SkyePharma Plc   Year of EU Approval:
          is
Lodotra™ comprised tablets                           White to practically                  2009-01-07
of an active core                                    white, odorless,                      Company Estimated
containing prednisone,                               crystalline powder.                   Launch Date: 2009-04-
which is encapsulated                                Melts at about 230,                   01
by an inactive porous                                with some
shell. The inactive                                  decomposition. Very
shell acts as a barrier                              slightly soluble in
between the product’   s                             water; slightly soluble
active core and a                                    in alcohol, in
patient’s                                            chloroform, in dioxane,
gastrointestinal fluids.                             and in methanol.
Following ingestion of                               (EP5.0) It shows
Lodotra™ , water in the                              polymorphism.:
digestive tract diffuses                             prednisone
through the shell to the
active core which
expands, leading to a
weakening and
breakage of the shell
allowing a release of
prednisone from the
core tablet. This
proprietary technology
is able to define the
period of delay
between ingestion and
dissolution of the
active core by the
patient’s
gastrointestinal fluids.
In the case of Lodotra™  ,
this period is
approximately four
-                          -               -         -                   -                 -
-   In a single-center,    -   ·Loteprednol etabonate Meda AB   -
    double-blind, placebo-     is a white to off-white
    controlled, parallel-      powder.: loteprednol
    group trial 165            etabonate
    subjects with SAR to
    grass pollen received
    daily single doses of
    either 100, 200, 400
    &#956;g LE nasal
    spray, or placebo for
    14 days [REF 1 -
    (Pubmed
    id:15679722)] .
Novolizer   -   Novolizer®   ·Loteprednol etabonate Almirall   -
                             is a white to off-white
                             powder.: loteprednol
                             etabonate
Magnesium stearate,   200 mg and 400 mg       -   ·(EP5.0) A white,        -   Year of US Approval:
microcrystalline      tablets dosed every 6       crystalline powder,          1976-08-16
cellulose.            hours                       freely soluble in water,
                                                  slightly soluble in
                                                  alcohol. Melting point:
                                                  160 °C to 165 °C.:
                                                  diphylline
Idec's Primatized®      -   -                     ·: lumiliximab   -                    -
antibody technology




-                       -   -                     -                -                    -




Eiffel SCF technology   -   Eiffel SCF Technology -                Telesso Technologies -
Eiffel ASES SCF           Phase II trial evaluated Eiffel SCF Technology·   ·Budesonide is a white Telesso Technologies -
particle technology to    two doses of             Tempo                    to off-white, odorless
manufacture               MAP0005, 104/5.4                                  powder that is
steroid/beta agonist      mcg and 312/16.2 mcg                              practically insoluble in
combinations. Patent      of                                                water and in heptane,
describes                 budesonide/formoterol.                            sparingly soluble in
formoterol/budesonide,    [34683]                                           ethanol, and freely
salmeterol                                                                  soluble in chloroform.
xinafoate/fluticasone                                                       Its partition coefficient
propionate, formoterol                                                      between octanol and
fumarate/fluticasone                                                        water at pH 5 is 1.6 x
propionate, and                                                             10.3 :
salmeterol xinafoate                                                        budesonide·White to
/budesonide as                                                              yellow crystal slightly
potential combinations.                                                     soluble in water.:
The drugs are                                                               formoterol
combined at micron or
submicron level rather
than separate particles
which can improve
dose efficiency and
consistency.




-                         -                      -                          -                     -                     -
-   In Phase II trials       -   -   -   -
    escalating multiple SC
    doses (0.3 mg/kg, 1
    mg/kg, 3 mg/kg) of
    MEDI-528 were
    administred. In Phase
    IIA trials MEDI-528
    was administred as a
    Subcutaneous
    injection twice weekly
    for 4 weeks (total of 8
    doses) at Day 0
    through Day 24. In
    another Phase IIA
    trials the patients
    received MEDI-528
    (9.0 mg/kg) as a single
    IV infusion. In Phase II
    trials patients received
    single IV dose of MEDI-
    528.


-   In the Phase 2a trial,   -   -   -   -
    600 mg of MEM 1414
    was administered.
Dehydrated ethanol,     Each gram of MEPTIN -     ·Procaterol               Otsuka           Year of Japan
oleic acid, and         Air 10 &#956;g            hydrochloride occurs Pharmaceutical Co.,   Approval: 2003-11-01
1,1,1,2,3,3,3-          contains 143 &#956;g      as white to pale yellow- Ltd.
heptafluoropropane      of                        white crystals or
(HFA-227) are used as   procaterol                crystalline powder. It is
inactive                hydrochloride, and a      soluble in water, formic
ingredients.            single puff delivers 10   acid and methanol,
                        &#956;g                   slightly soluble in
                        of the active             ethanol (95), and
                        ingredient. Each          practically insoluble in
                        container contains 5      diethyl ether. The pH
                        mL of                     of its aqueous solution
                        the drug suspension       (1&#8594;100) is 4.0-
                        and provides about        5.0. It
                        100 puffs.                gradually changes in
                        MEPTIN Air 10             color when exposed to
                        &#956;g is delivered      light. Its aqueous
                        as a mist, when           solution (1&#8594;20)
                        shaken                    shows no optical
                        well and sprayed          rotation: procaterol
                        through anadapter.        hydrochloride
                        The usual adult dose
                        is 20 &#956;g (2 puffs)
                        of procaterol
                        hydrochloride. For
                        children the amount
                        should be reduced to
                        10 &#956;g (1 puff) of
                        procaterol
                        hydrochloride.
Inactive                 MEPTIN Drysyrup            -   ·Procaterol               -   Year of Japan
ingredients: sucrose,    0.005% is a white              hydrochloride occurs          Approval: 2004-09-01
ascorbic acid,           odorless powder or             as white to pale yellow-
anhydrous citric acid,   granules with a sweet          white crystals or
and light anhydrous      taste.                         crystalline powder. It is
silicic acid.                                           soluble in water, formic
                         The usual adult dose           acid and methanol,
                         is 50 &#956;g of               slightly soluble in
                         procaterol                     ethanol (95), and
                         hydrochloride (1 g             practically insoluble in
                         of MEPTIN Drysyrup             diethyl ether. The pH
                         0.005%) once daily (at         of its aqueous solution
                         bedtime) or                    (1&#8594;100) is 4.0-
                         twice daily (in the            5.0. It
                         morning and at                 gradually changes in
                         bedtime) by the oral           color when exposed to
                         route.                         light. Its aqueous
                         MEPTIN Drysyrup                solution (1&#8594;20)
                         0.005% is prepared             shows no optical
                         into a solution at the         rotation: procaterol
                         time of use.                   hydrochloride
                         The dose for children 6
                         years of age or older is
                         25 &#956;g of
                         procaterol
                         hydrochloride (0.5 g of
                         MEPTIN Drysyrup
                         0.005%) once daily (at
                         bedtime) or twice daily
                         (in the
                         morning and at
                         bedtime) by the oral
                         route.
Inactive ingredients: D-   MEPTIN Granules are -      ·Procaterol               -   Year of Japan
mannitol, purified         white odorless             hydrochloride occurs          Approval: 1984-06-01
sucrose, corn starch,      granules with a sweet      as white to pale yellow-
crystalline cellulose,     taste. Each gram of        white crystals or
and anhydrous citric       MEPTIN Granules            crystalline powder. It is
acid.                      contains 100 &#956;g       soluble in water, formic
                           of                         acid and methanol,
                           procaterol                 slightly soluble in
                           hydrochloride.             ethanol (95), and
                                                      practically insoluble in
                           The usual adult dose       diethyl ether. The pH
                           is 50 &#956;g of           of its aqueous solution
                           procaterol                 (1&#8594;100) is 4.0-
                           hydrochloride (0.5         5.0. It
                           g of MEPTIN                gradually changes in
                           Granules) once daily       color when exposed to
                           (at bedtime) or twice      light. Its aqueous
                           daily                      solution (1&#8594;20)
                           (in the morning and at     shows no optical
                           bed time) by the oral      rotation: procaterol
                           route.                     hydrochloride
                           The dose for children 6
                           years of age or older is
                           25 &#956;g of
                           procaterol
                           hydrochloride (0.25 g
                           of MEPTIN
                           Granules)
                           once daily (at bedtime)
                           or twice daily (in the
                           morning
                           and at bedtime) by the
                           oral route.
                           The dose for children
Inactive ingredients:     100 &#956;g of         -   ·Procaterol               Otsuka           Year of Japan
Anhydrous citric acid,    procaterol                 hydrochloride occurs Pharmaceutical Co.,   Approval: 1987-10-01
sodium hydroxide (pH      hydrochloride/mL.          as white to pale yellow- Ltd.
adjuster), purified       Clear, colorless           white crystals or
water. Additionally, 30   liquids. They have no      crystalline powder. It is
mL/bottle includes        odor.                      soluble in water, formic
benzalkonium              The usual adult dose       acid and methanol,
chloride solution.        is 30-50 &#956;g of        slightly soluble in
                          procaterol                 ethanol (95), and
                          hydrochloride              practically insoluble in
                          (0.3-0.5 mL of             diethyl ether. The pH
                          MEPTIN Inhalation          of its aqueous solution
                          Solution) via a            (1&#8594;100) is 4.0-
                          nebulizer                  5.0. It
                          with deep breathing.       gradually changes in
                          For children, the          color when exposed to
                          amount should be           light. Its aqueous
                          reduced to 10-30           solution (1&#8594;20)
                          &#956;g of procaterol      shows no optical
                          hydrochloride (0.1-0.3     rotation: procaterol
                          mL of                      hydrochloride
                          the drug).
Inactive ingredients:   MEPTIN Kid Air 5       -   ·Procaterol               Otsuka           Year of Japan
Dehydrated ethanol,     &#956;g is delivered       hydrochloride occurs Pharmaceutical Co.,   Approval: 2003-12-01
oleic acid, and         as a mist, when            as white to pale yellow- Ltd.
1,1,1,2,3,3,3-          shaken                     white crystals or
heptafluoropropane      well and sprayed           crystalline powder. It is
(HFA-227).              through an adapter.        soluble in water, formic
                        Each gram of MEPTIN        acid and methanol,
                        Kid Air 5 &#956;g          slightly soluble in
                        contains 143 &#956;g       ethanol (95), and
                        of                         practically insoluble in
                        procaterol                 diethyl ether. The pH
                        hydrochloride, and a       of its aqueous solution
                        single puff delivers 5     (1&#8594;100) is 4.0-
                        &#956;g of                 5.0. It
                        the active ingredient.     gradually changes in
                        Each container             color when exposed to
                        contains 2.5 mL of         light. Its aqueous
                        the drug suspension        solution (1&#8594;20)
                        and provides about         shows no optical
                        100 puffs.                 rotation: procaterol
                                                   hydrochloride
                        The usual adult dose
                        is 20 &#956;g (4 puffs)
                        of procaterol
                        hydrochloride. For
                        children the amount
                        should be reduced to
                        10 &#956;g (2 puffs) of
                        procaterol
                        hydrochloride.
Inactive ingredients:    MEPTIN Syrup is a          -   ·Procaterol               -   Year of Japan
Ethyl                    colorless, clear, slightly     hydrochloride occurs          Approval: 1984-03-01
parahydroxybenzoate,     viscous liquid.                as white to pale yellow-
butyl                    It has an orange odor          white crystals or
parahydroxybenzoate,     and sweet taste.               crystalline powder. It is
                         pH: 3.5 - 4.5.                 soluble in water, formic
sodium benzoate,         Each mL of MEPTIN              acid and methanol,
flavor, purified         Syrup contains 5               slightly soluble in
sucrose, ethanol,        &#956;g of procaterol          ethanol (95), and
anhydrous citric acid,   hydrochloride.                 practically insoluble in
sodium citrate, and      The usual adult                diethyl ether. The pH
purified water.          dosage is 50 &#956;g           of its aqueous solution
                         of procaterol                  (1&#8594;100) is 4.0-
                         hydrochloride                  5.0. It
                         (10 mL of MEPTIN               gradually changes in
                         Syrup) once daily (at          color when exposed to
                         bed time) or twice             light. Its aqueous
                         daily (in the morning          solution (1&#8594;20)
                         and at bed time) by the        shows no optical
                         oral route.                    rotation: procaterol
                         The dose for children 6        hydrochloride
                         years of age or older is
                         25 &#956;g of
                         procaterol
                         hydrochloride (5 mL of
                         MEPTIN Syrup) once
                         daily
                         (at bed time) or twice
                         daily (in the morning
                         and at bed time) by
                         the oral route.
                         The dose for children
                         younger than 6 years
                         of age is 1.25 &#956;g
Inactive ingredients:   MEPTIN Tablets are       -   ·Procaterol               -   Year of Japan
D-mannitol, corn        white compressed             hydrochloride occurs          Approval: 1980-12-01
starch, crystalline     tablets scored on one        as white to pale yellow-
cellulose,              side. Each MEPTIN            white crystals or
hydroxypropylmethylce   Tablets contains 50          crystalline powder. It is
llulose,                &#956;g of procaterol        soluble in water, formic
and magnesium           hydrochloride.               acid and methanol,
stearate.                                            slightly soluble in
                        The usual adult dose         ethanol (95), and
                        of MEPTIN Tablets is         practically insoluble in
                        50 &#956;g of                diethyl ether. The pH
                        procaterol                   of its aqueous solution
                        hydrochloride (one           (1&#8594;100) is 4.0-
                        tablet) once daily (at       5.0. It
                        bedtime) or twice            gradually changes in
                        daily (in the morning        color when exposed to
                        and at bedtime) by the       light. Its aqueous
                        oral route.                  solution (1&#8594;20)
                                                     shows no optical
                                                     rotation: procaterol
                                                     hydrochloride
Inactive ingredients:   MEPTIN-Mini Tablets -      ·Procaterol               -   Year of Japan
D-mannitol, corn        are white compressed       hydrochloride occurs          Approval: 1984-06-01
starch, crystalline     tablets scored on one      as white to pale yellow-
cellulose,              side. Each MEPTIN-         white crystals or
hydroxypropylmethylce   Mini Tablet contains       crystalline powder. It is
llulose, and            25 &#956;g of              soluble in water, formic
magnesium stearate.     procaterol                 acid and methanol,
                        hydrochloride.             slightly soluble in
                                                   ethanol (95), and
                        The usual adult dose       practically insoluble in
                        of MEPTIN Mini Tablet      diethyl ether. The pH
                        is 50 &#956;g of           of its aqueous solution
                        procaterol                 (1&#8594;100) is 4.0-
                        hydrochloride (two         5.0. It
                        tablets) once daily (at    gradually changes in
                        bedtime)                   color when exposed to
                        or twice daily (in the     light. Its aqueous
                        morning and at             solution (1&#8594;20)
                        bedtime) by the oral       shows no optical
                        route.                     rotation: procaterol
                        The dose for children 6    hydrochloride
                        years of age or older is
                        25 &#956;g (one
                        tablet) once daily (at
                        bedtime) or twice daily
                        (in the morning and at
                        bedtime) by the oral
                        route.
-                      Phase 2 Asthma trial   -   ·: etoricoxib   -                     -
                       dosage was 5mg po
                       qd.trials
                       Phase 2
                       Atherosclerosis and
                       COPD trial dosage
                       was 100mg. trials
-                      -                      -   -               -                     -




-                      -                      -   -               -                     -


-                      -                      -   ·: tipelukast   Kyorin Pharmaceutical -


-                      -                      -   -               -                     -

Aerosol formulation or -                      -   -               AnGes MG Inc.         -
nebulizable powder




-                      -                      -   -               -                     -
MAXAIR AUTOHALER            200 mcg/inh. Each       3M MDI Metering   ·Pirbuterol acetate is a 3M Health Care   Year of US Approval:
is a pressurized            14.0 g canister         Valves            white, crystalline                        1992-11-30
metered-dose aerosol        provides 400                              racemic mixture of two
unit for oral inhalation.   inhalations and each                      optically active
It provides a fine-         2.8 g canister provides                   isomers. It is powder.:
particle suspension of      80 inhalations.                           pirbuterol acetate
pirbuterol acetate in       The usual dose for
the propellant mixture      adults and children 12
of trichioro-               years and older is two
monofluoromethane           inhalations (400 mcg)
and                         repeated every 4-6
dichlorodifluoromethan      hours. A total daily
e, with sorbitan            dose of 12 inhalations
trioleate. Each             should not be
actuation delivers 253      exceeded.
mcg of drug from the
valve and 200 mcg of
drug from the
mouthpiece. The unit
is breath-actuated
such that the
medication is delivered
automatically during
inspiration without the
need for the patient to
coordinate actuation
with inspiration.
Clickhaler technology    The usual adult dose Clickhaler      ·Procaterol               Vectura Group Plc   Year of EU Approval:
                         is 20 &#956;g (2 puffs)              hydrochloride occurs                          2005
                         of procaterol                        as white to pale yellow-                      Year of Japan
                         hydrochloride. For                   white crystals or                             Approval: 2005-09-01
                         children the amount                  crystalline powder. It is
                         should be reduced to                 soluble in water, formic
                         10 &#956;g (1 puff) of               acid and methanol,
                         procaterol                           slightly soluble in
                         hydrochloride.                       ethanol (95), and
                                                              practically insoluble in
                                                              diethyl ether. The pH
                                                              of its aqueous solution
                                                              (1&#8594;100) is 4.0-
                                                              5.0. It
                                                              gradually changes in
                                                              color when exposed to
                                                              light. Its aqueous
                                                              solution (1&#8594;20)
                                                              shows no optical
                                                              rotation: procaterol
                                                              hydrochloride




Combinations             -                    Miat-Haler      -                       Miat Spa              -
delivered in Miat-Haler,
multidose DPI
-                        -                    Microdose DPI   -                       MicroDose Therapeutx -
AirMax DPI   -   Airmax/Spriomax   ·Budesonide is a white Teva Pharmaceutical   -
                                   to off-white, odorless Industries Ltd.
                                   powder that is
                                   practically insoluble in
                                   water and in heptane,
                                   sparingly soluble in
                                   ethanol, and freely
                                   soluble in chloroform.
                                   Its partition coefficient
                                   between octanol and
                                   water at pH 5 is 1.6 x
                                   10.3 : budesonide
Mometasone               -   -   ·USP 29 (Mometasone Schering-Plough Corp. -
Furoate/Formoterol               Furoate) White to off-
Fumarate 200/10mcg               white powder. Melts at
or 400/10 mcg BID                about 220, with
delivered by                     decomposition.
pressurized metered-             Soluble in acetone and
dose Inhaler (source:            in methylene chloride.:
clinical trials.gov).            mometasone
Product combines                 furoate·White to yellow
Novartis’ Foradil®               crystal slightly soluble
(formoterol fumarate),           in water.: formoterol
a selective, long-acting
beta2-agonist, with
Schering-Plough’   s
Asmanex®
(mometasone furoate),
an inhaled
corticosteroid.
-                        Phase 3; Intravenous    -   ·Montelukast sodium is -                 -
                         single administration       a hygroscopic,
                         trials                      optically active, white
                                                     to off-white powder.
                                                     Montelukast sodium is
                                                     freely soluble in
                                                     ethanol, methanol, and
                                                     water and practically
                                                     insoluble in
                                                     acetonitrile. :
                                                     montelukast sodium
Inhalation into the lung -                       -   ·: sodium pyruvate     EmphyCorp, Inc.   -
by a nebulizer.
Sodium Pyruvate in
0.9% sodium chloride
solution in phase 2 trial
(trials)
A proprietary nebulized -                       -        -                      N30 Pharma             -
formulation of s-
nitrosoglutathione
[31530]

3 day patch             -                       -        -                         NAL Pharmaceuticals -
                                                                                   Ltd.
1 day patch             -                       -        ·Tulobuterol occurs as NAL Pharmaceuticals -
                                                         white crystals or         Ltd.
                                                         crystalline powder. It is
                                                         odorless. It is very
                                                         soluble in methanol,
                                                         freely soluble in
                                                         ethanol (95), acetic
                                                         acid (100), diethylether
                                                         or isopropylether,
                                                         sparingly soluble in
                                                         hexane and practically
                                                         insoluble in water. It
                                                         has no optical rotation:
                                                         tulobuterol



NexACT in               -                       NexACT   -                      NexMed, Inc.           -
transdermal patch
Nasal drops             -                       -        -                      Hisamitsu              -
                                                                                Pharmaceutical Co.
                                                                                Inc.
Tablets                 In Phase II trials      -        -                      -                      -
                        patients were given 4
                        mg and/or 8 mg NM-
                        702 twice a day (BID)
-   Once daily       -   -   Epigenesis             -
    administration           Pharmaceuticals Inc.
Inactive ingredients:   250 mg in 10 mL       -   ·USP 29                 -   Market Launch Date
Ethylenediamine         ampules. Administered     (Aminophylline) May         Japan: 1950-10-01
                        intravenously once to     have a faint
                        twice daily. If           ammoniacal odor. It
                        necessary, it             contains 84.0 to 87.4%
                        should be                 of anhydrous
                        administrated by          theophylline and 13.5
                        intravenous drip-         to 15.0% of anhydrous
                        infusion                  ethylenediamine. A
                                                  white or slightly
                                                  yellowish powder,
                                                  sometimes granular.
                                                  Freely soluble in water
                                                  (the solution becomes
                                                  cloudy through
                                                  absorption of carbon
                                                  dioxide); practically
                                                  insoluble in dehydrated
                                                  alcohol.: aminophylline
Each gram of white to     Each gram of white to -   ·USP 29                 -   Market Launch Date
pale yellow granules or   pale yellow granules or   (Aminophylline) May         Japan: 1950-10-01
powder contains 1 g of    powder contains 1 g of    have a faint
aminophylline, JP.        aminophylline, JP. The    ammoniacal odor. It
                          usual adult dosage for    contains 84.0 to 87.4%
                          oral use is 300 to 400    of anhydrous
                          mg of aminophylline       theophylline and 13.5
                          daily in three to four    to 15.0% of anhydrous
                          divided doses.            ethylenediamine. A
                                        s
                          The children’ dosage      white or slightly
                          for oral use is 2-4       yellowish powder,
                          mg/kg of aminophylline    sometimes granular.
                          three to four times       Freely soluble in water
                          daily.                    (the solution becomes
                                                    cloudy through
                                                    absorption of carbon
                                                    dioxide); practically
                                                    insoluble in dehydrated
                                                    alcohol.: aminophylline
Inactive ingredients:    100 mg white plain       -   ·USP 29                 -   Market Launch Date
carmellose calcium,      tablet. The usual adult      (Aminophylline) May         Japan: 1950-10-01
calcium stearate, corn   dosage is 3 to 4             have a faint
starch,                  tablets (300 to 400 mg       ammoniacal odor. It
hydroxypropylcellulose   of aminophylline) daily      contains 84.0 to 87.4%
and povidone K30.        in three to four divided     of anhydrous
                         doses. The children’  s      theophylline and 13.5
                         dosage is 2-4 mg/kg of       to 15.0% of anhydrous
                         aminophylline three to       ethylenediamine. A
                         four times daily.            white or slightly
                                                      yellowish powder,
                                                      sometimes granular.
                                                      Freely soluble in water
                                                      (the solution becomes
                                                      cloudy through
                                                      absorption of carbon
                                                      dioxide); practically
                                                      insoluble in dehydrated
                                                      alcohol.: aminophylline
-   -   -   ·: nepadutant    -   -




-   -   -   -                -   -




-   -   -   ·: neutrazumab   -   -
Inactive ingredients: D- Each 1 g of white fine -   ·Lysozyme                 -   Year of Japan
mannitol                 granules contains 200      hydrochloride occurs          Approval: 1981-09-01
                         mg (potency) of            as white crystals,
                         lysozyme                   crystalline powder or
                         hydrochloride,             amorphous powder. It
                         administered three         is soluble in water and
                         times daily.               practically insoluble in
                                                    ethanol (99.5). It is
                                                    hygroscopic. The pH
                                                    of an aqueous solution
                                                    (3 in 200) is 3.0 to 5.0.
                                                    The molecular weight
                                                    is about 14,400
                                                    Dalton.

                                                    : lysozyme
                                                    hydrochloride
Inactive ingredients:   Each 1 g of white     -   ·Lysozyme                 -   Year of Japan
corn starch, povidone   granules contains 100     hydrochloride occurs          Approval: 1968-01-01
K30 and D-mannitol      mg (potency) of           as white crystals,
                        lysozyme                  crystalline powder or
                        hydrochloride,            amorphous powder. It
                        administered three        is soluble in water and
                        times daily.              practically insoluble in
                                                  ethanol (99.5). It is
                                                  hygroscopic. The pH
                                                  of an aqueous solution
                                                  (3 in 200) is 3.0 to 5.0.
                                                  The molecular weight
                                                  is about 14,400
                                                  Dalton.

                                                  : lysozyme
                                                  hydrochloride
Inactive ingredients:    30 and 90 mg white,   -   ·Lysozyme                 -   Year of Japan
calcium stearate,        plain tablets,            hydrochloride occurs          Approval: 1967-08-01
hydroxypropylcellulose   administered three        as white crystals,
and D-mannitol           times daily.              crystalline powder or
                                                   amorphous powder. It
                                                   is soluble in water and
                                                   practically insoluble in
                                                   ethanol (99.5). It is
                                                   hygroscopic. The pH
                                                   of an aqueous solution
                                                   (3 in 200) is 3.0 to 5.0.
                                                   The molecular weight
                                                   is about 14,400
                                                   Dalton.

                                                   : lysozyme
                                                   hydrochloride




-                        -                     -   -                         -   -
-                       -                      -              -                      -          -




Novolizer technology.   One metered dose         Novolizer®   ·Budesonide is a white Almirall   Year of EU Approval:
200 µg and 400 µg       contains 200                          to off-white, odorless            2000
budesonide. Inactive    micrograms of                         powder that is
ingredients: lactose    budesonide. Adults:                   practically insoluble in
monohydrate             Initial recommended                   water and in heptane,
                        dose: 200 - 400 mcg                   sparingly soluble in
                        once or twice daily;                  ethanol, and freely
                        max. recommended                      soluble in chloroform.
                        dose: 800 mcg twice                   Its partition coefficient
                        daily. Children: Initial              between octanol and
                        recommended dose:                     water at pH 5 is 1.6 x
                        200 mcg twice or 200 -                10.3 : budesonide
                        400 mcg once daily;
                        max. recommended
                        dose: 400 mcg twice
                        daily
Excipients: Lactose Ph   175 and 250 mg            -   ·USP 29                  Meda AB   -
Eur, Cellulose Acetate   prolonged release             (Theophylline) White,
Phthalate Ph Eur,        tablets. 1 to 2 tablets       odorless, crystalline
Magnesium Stearate       twice daily.                  powder, having a bitter
Ph Eur                                                 taste. Is stable in air.
                                                       Slightly soluble in
                                                       water, but more
                                                       soluble in hot water;
                                                       freely soluble in
                                                       solutions of alkali
                                                       hydroxides and in
                                                       ammonia; sparingly
                                                       soluble in
                                                       alcohol, in chloroform,
                                                       and in ether.:
                                                       theophylline




-                        Once daily.               -   -                      -           -

-                        -                         -   -                      -           -


-                        In Phase II, patients  -      -                      -           -
                         are given OX914 in
                         doses of 15 or 50 mg
                         for two weeks. [42449]

-                        -                         -   -                      -           -
Program contains non- -   -   -   -   -
steroid anti-
inflammatory
substances that have
shown favorable
effects in preclinical
asthma models.
-                     -   -   -   -   -




-                     -   -   -   -   -
-                       In Phase II Clinical       -          -   -                  -
                        Trials, patients with
                        seasonal allergic
                        rhinitis will be treated
                        with a placebo or
                        OX914 in dosages of
                        15 or 50 mg for two
                        weeks in a double-
                        blind, three-way
                        cross-over study.
                        company report
                        page:5


MicroAir nebulizer to   -                          MicroAir   -   Omron HealthCare   -
deliver marketed
nebulizer solutions
Each ONON®               White - yellowish white -   ·Pranlukast hydrate      -   Year of EU Approval:
Capsules contains        opaque hard 112.5 mg        occurs as a white to         1995
112.5 mg of              capsules.The usual          light yellow crystalline     Year of Japan
Pranlukast hydrate and   adult dosage for oral       powder. It is odourless      Approval: 2006-06-01
Macrogol 4000,           use is 450 mg of            and tasteless. It is
magnesium stearate,      pranlukast hydrate (4       soluble in
lactose hydrate          capsules) daily in two      dimethylsulfoxide or
(Capsules containing     divided doses after         N,N-
gelatin, macrogol        each meal                   dimethylformamide,
4000, sodium lauryl      in the morning and          very slightly soluble in
sulfate and titanium     evening.                    ethanol (99.5), and
oxide) as inactive                                   practically insoluble in
ingredients.                                         water, acetonitrile,
                                                     dichloromethane or
                                                     diethyl ether.:
                                                     pranlukast hydrate
Each gram of ONON®       White to light yellow   -   ·Pranlukast hydrate      -                    Year of EU Approval:
Dry Syrup 10%            granules,100 mg dry         occurs as a white to                          1999
contains 100 mg          syrup. The usual            light yellow crystalline                      Year of Japan
Pranlukast hydrate and   childhood dosage for        powder. It is odourless                       Approval: 2006-01-01
Corn starch,             oral use is 7 mg/kg of      and tasteless. It is
Hydroxypropylcellulose   pranlukast hydrate (70      soluble in
, sucrose as inactive    mg/kg of dry syrup)         dimethylsulfoxide or
ingredients.             daily in 2 divided          N,N-
                         doses after each meal       dimethylformamide,
                         in the morning and          very slightly soluble in
                         evening, preparing a        ethanol (99.5), and
                         suspension each time.       practically insoluble in
                         The dosage may be           water, acetonitrile,
                         adjusted according to       dichloromethane or
                         the patient's age and       diethyl ether.:
                         symptoms. The               pranlukast hydrate
                         maximum daily dose is
                         10 mg/kg of pranlukast
                         hydrate (100 mg/kg of
                         dry syrup). It should
                         not exceed the usual
                         adult daily dose of 450
                         mg/day of pranlukast
                         hydrate (4.5 g/day of
                         dry syrup).




Sterile, topical product -                       -   -                        OPTIME Therapeutics, -
                                                                              Inc.
Taste masked, oral        Oral solution          -   ·(EP5.0) A white or    Biomarin              Year of US Approval:
liquid solution           containing 20.2 mg (15     almost white,          Pharmaceutical Inc.   2000-12-14
containing alcohol,       mg free base) drug in      crystalline powder,
fructose, glycerin,       5 mL. Dosing ranges        hygroscopic, freely
monoammonium              from 5 mg - 60 mg of       soluble in water, very
glycyrrhizinate,          free base per day.         slightly soluble in
povidone, sodium          Doses vary between         alcohol.: prednisolone
benzoate, sorbitol, and   subjects and need to       sodium phosphate
grape flavor.             be individualized.
Grape flavored tablet     White, flat faced,      OraSolv®   ·(EP5.0) A white or    CIMA LABS             Year of US Approval:
containing citric acid,   beveled 13.4 mg, 20.2              almost white,                                2006-06-01
colloidal silicon         mg, and 40.3 mg                    crystalline powder,
dioxide, grape flavor,    (equivalent to 10 mg,              hygroscopic, freely
hypromellose,             15 mg, and 30 mg                   soluble in water, very
magnesium stearate,       prednisolone base)                 slightly soluble in
mannitol, methacrylate    tablets in blisters                alcohol.: prednisolone
copolymer,                containing 48 tablets              sodium phosphate
microcrstalline           per carton. Each card
cellulose, sodium         contains 6 tablets.
bicarbonate, sucralose    Doses are
and sucrose. Orapred      individualized with
ODT is taste-masked,      initial dose of 10-60
and non-refrigerated      mg daily. Up to 200
formulation of            mg per day may be
prednisolone.             used in treatment of
                          exacerbations of
                          multiple sclerosis. The
                          standard regimen for
                          treatment of nephrotic
                          syndrome in pediatric
                          patients is 60 mg/m2
                          in three divided doses
                          for four weeks followed
                          by 40 mg/m2of a
                          single dose alternate
                          day for four weeks



HFA formulation,          -                     -            ·Ciclesonide is a white Ranbaxy Laboratories -
generic for Alvesco                                          to yellow-white         Ltd.
HFA                                                          powder, practically
                                                             insoluble in water and
                                                             freely
                                                             soluble in ethanol and
                                                             acetone: ciclesonide
-                       -                        -          -                      -                   -




Delivers 9 mcg or 4.5   9 micrograms           Turbuhaler   · A white or almost      AstraZeneca Plc   Year of EU Approval:
mcg of drug. Inactive   formoterol fumarate                 white or slightly yellow                   1997-03-26
ingredients: lactose    dihydrate. Dosed 1or 2              powder. Slightly
monohydrate             actuations once or                  soluble in water and in
                        twice daily.                        isopropyl alcohol;
                                                            practically insoluble in
                                                            acetonitrile; soluble in
                                                            methyl alcohol. A 0.1%
                                                            solution in water has a
                                                            pH of 5.5 to 6.5.
                                                            Protect from light.:
                                                            formoterol fumarate



-                       -                        -          -                      -                   -




-                       Phase 1 trial: Oral, two -          -                      -                   -
                        doses 12 hours apart
                        trials
-                     In a Phase 2a study of -   -               -             -
                      Single Oral Doses of
                      PF-04191834 to
                      determine the
                      bronchodilatory effects
                      of PF-04191834
                      compared with zileuton
                      in patients with
                      asthma, single dose
                      30, 100 and 2000 mg
                      PF-04191834 will be
                      administered trials.


-                     -                      -   -               Pfizer Inc.   -

-                     -                      -   -               -             -


Capsule formulation   In the upcoming Phase -    ·: giripladib   -             -
                      II osteoarthritis trial,
                      subjects will be
                      randomized to 1 of 6
                      treatment groups: PLA-
                      695 50 mg, 200 mg, or
                      400 mg QD, PLA-695
                      200 mg BID, placebo,
                      or naproxen 500 mg
                      BID.



-                     -                      -   -               -             -
Bespak MDI Metering     Cannister containing    Bespak MDI Metering ·USP 29 (Albuterol       3M Health Care   Year of US Approval:
Valve technology.       200 doses. 0.108 mg     Valve               Sulfate) White or                         2004-10-29
Microcrystalline        (0.09 mg base) per                          practically white                         Earliest US Market
suspension of drug in   inhalation. Dosed two                       powder. Freely soluble                    Exclusivity: 2007-10-
ethanol and HFA 134a.   inhalations every 4-6                       in water; slightly                        29
                        hours                                       soluble in alcohol, in                    Earliest Patent
                                                                    chloroform, and in                        Exclusivity: 2009-11-
                                                                    ether. pKa=9.14.                          28
                                                                    Solubility: 24.5% w/v at
                                                                    pH 7.: albuterol sulfate
-                       -                       -        -   Pieris AG             -




-                       In phase 2 psoriasis    -        -   -                     -
                        trials 10 mg capsules
                        given orally,in phase 2
                        asthma trials 30 mg
                        capsules given once
                        daily,in COPD phase 2
                        trials 1mg,10mg
                        capsules given 3 times
                        daily.


-                       -                       -        -   -                     -


PW3101 was a            -                       TIMERx   -   Penwest               -
reformulation of a                                           Pharmaceuticals Co.
branded product that is
marketed for oral
asthma.
-                       -                       -        -   Pharmaxis Ltd.        -




-                       -                       -        -   -                     -
New version of             -                     -   -                     Pharmaxis Ltd.         -
PXS25, called PXS64
delivers PXS25 more
effectively to the site of
action when
administered orally
-                          -                     -   -                     -                      -
-                          -                     -   -                     -                      -


Excipients:              225 mg matrix tablet.   -   ·Ph. Eur. 5.2           Napp Pharmaceuticals Year of EU Approval:
Hydroxyethylcellulose,                               (Theophylline-          Ltd.                 1989-07-07
Povidone [K25],                                      ethylenediamine
Cetostearyl alcohol,                                 Hydrate; Aminophylline
Purified talc,                                       Hydrate BP 2004). It
Magnesium stearate,                                  contains 84.0 to 87.4%
Hypromellose (E464),                                 of anhydrous
Macrogol 400,                                        theophylline and 13.5
Industrial methylated                                to 15.0% of anhydrous
spirit, Titanium dioxide                             ethylenediamine. A
(E171), Iron oxide                                   white or slightly
(E172)                                               yellowish powder,
                                                     sometimes granular.
                                                     Freely soluble in water
                                                     and practically
                                                     insoluble in dehydrated
                                                     alcohol.: aminophylline
                                                     dihydrate
Excipients:              350 mg matrix tablet.   -   ·Ph. Eur. 5.2           Napp Pharmaceuticals Year of EU Approval:
Hydroxyethylcellulose,                               (Theophylline-          Ltd.                 1983-08-17
Povidone [K25],                                      ethylenediamine
Cetostearyl alcohol,                                 Hydrate; Aminophylline
Purified talc,                                       Hydrate BP 2004). It
Magnesium stearate,                                  contains 84.0 to 87.4%
Hypromellose (E464),                                 of anhydrous
Macrogol 400,                                        theophylline and 13.5
Industrial methylated                                to 15.0% of anhydrous
spirit, Titanium dioxide                             ethylenediamine. A
(E171), Iron oxide                                   white or slightly
(E172)                                               yellowish powder,
                                                     sometimes granular.
                                                     Freely soluble in water
                                                     and practically
                                                     insoluble in dehydrated
                                                     alcohol.: aminophylline
                                                     dihydrate
-   100 mg controlled   -   ·Ph. Eur. 5.2           United            -
    release tablets         (Theophylline-          Pharmaceuticals
                            ethylenediamine
                            Hydrate; Aminophylline
                            Hydrate BP 2004). It
                            contains 84.0 to 87.4%
                            of anhydrous
                            theophylline and 13.5
                            to 15.0% of anhydrous
                            ethylenediamine. A
                            white or slightly
                            yellowish powder,
                            sometimes granular.
                            Freely soluble in water
                            and practically
                            insoluble in dehydrated
                            alcohol.: aminophylline
                            dihydrate




-   -                   -   -                     -                   -




-   -                   -   -                     -                   -
-   Given as an oral       -   ·: pleconaril   -   -
    solution (2-5 mg/kg,
    also 200 and 400 mg
    doses) to reduce food
    effect in clinical
    studies. In some
    clinical studies
    pleconaril 400 mg 3
    times/day for 5-7 days
    given within 24-36
    hours of symptom
    onset decreases the
    duration and severity
    of the common cold
1.8 cm cherry flavored 3.3 mg lozenges          -   ·USP 29                 Cobalis Corp.   -
lozenge                administered under the       (Cyanocobalamin)
                       tongue twice daily 2-3       Dark red crystals or
                       weeks prior to allergy       amorphous or
                       season and an                crystalline red powder.
                       additional three weeks       In the anhydrous form,
                       into the allergy season.     it is very hygroscopic
                       (website and                 and when exposed to
                       EP1128835)                   air it may absorb about
                                                    12% of water.
                                                    Sparingly soluble in
                                                    water; soluble in
                                                    alcohol; insoluble in
                                                    acetone, in chloroform,
                                                    and in ether.:
                                                    cyanocobalamin
-   -   PremaireTM Metered   ·USP 29 (Albuterol       Sheffield             -
        Solution Inhaler     Sulfate) White or        Pharmaceuticals Inc
                             practically white
                             powder. Freely soluble
                             in water; slightly
                             soluble in alcohol, in
                             chloroform, and in
                             ether. pKa=9.14.
                             Solubility: 24.5% w/v at
                             pH 7.: albuterol sulfate



-   -   PremaireTM Metered   ·Budesonide is a white Sheffield               -
        Solution Inhaler     to off-white, odorless Pharmaceuticals Inc
                             powder that is
                             practically insoluble in
                             water and in heptane,
                             sparingly soluble in
                             ethanol, and freely
                             soluble in chloroform.
                             Its partition coefficient
                             between octanol and
                             water at pH 5 is 1.6 x
                             10.3 : budesonide
-   -   PremaireTM Metered   ·A white, odourless,   Sheffield             -
        Solution Inhaler     hygroscopic,           Pharmaceuticals Inc
                             crystalline powder.
                             Soluble in water;
                             insoluble in alcohol
                             and in chloroform.:
                             sodium cromoglycate
Inactive ingredients:       Delivers 0.22 mg          -   ·USP 29 (Epinephrine) Wyeth   Year of US Approval:
ascorbic acid,              epinephrine per               White to practically          1967-11-08
dehydrated alcohol          inhalation. Available in:     white, odorless,
(34%),                      1/2 fl oz (15 mL) with        microcrystalline
dichlorodifluoromethan      mouthpiece (actuator),        powder or granules,
e (CFC 12),                 1/2 fl oz (15 mL) refill      gradually darkening on
dichlorotetrafluoroetha     and 3/4 fl oz (22.5 mL)       exposure to light and
ne (CFC 114),               refill.                       air. With acids, it forms
hydrochloric acid, nitric                                 salts that are readily
acid, purified water                                      soluble in water, and
                                                          the base may be
                                                          recovered by the
                                                          addition of ammonia
                                                          water or alkali
                                                          carbonates. Its
                                                          solutions are alkaline
                                                          to litmus. Very slightly
                                                          soluble in water and in
                                                          alcohol; insoluble in
                                                          ether, in chloroform,
                                                          and in fixed and
                                                          volatile oils.
                                                          (Epinephrine Injection)
                                                          Practically colorless,
                                                          slightly acid liquid.
                                                          Gradually turns dark
                                                          on exposure to light
                                                          and air.
                                                          (Epinephrine Inhalation
                                                          Solution) Practically
                                                          colorless, slightly acid
                                                          liquid. Gradually turns
                                                          dark on exposure to
                                                          light and air.
Breath actuated       -              Easi-Breathe   ·USP 29 (Albuterol       Teva Pharmaceutical   -
inhalation based on                                 Sulfate) White or        Industries Ltd.
Easi-breathe                                        practically white
technology.                                         powder. Freely soluble
                                                    in water; slightly
                                                    soluble in alcohol, in
                                                    chloroform, and in
                                                    ether. pKa=9.14.
                                                    Solubility: 24.5% w/v at
                                                    pH 7.: albuterol sulfate



-                     1 mg tablets   -              ·(EP5.0) White to          -                   -
                                                    brownish-yellow, fine,
                                                    crystalline powder.
                                                    Sparingly soluble in
                                                    water, slightly soluble
                                                    in methanol, very
                                                    slightly soluble in
                                                    acetonitrile.: ketotifen
                                                    fumarate
-                      -   -   -                      -                      -




CFC-MDI. Replaced      -   -   ·USP 29 (Albuterol       Schering-Plough Corp. Year of US Approval:
with HFA formulation           Sulfate) White or                              1981-05-01
                               practically white
                               powder. Freely soluble
                               in water; slightly
                               soluble in alcohol, in
                               chloroform, and in
                               ether. pKa=9.14.
                               Solubility: 24.5% w/v at
                               pH 7.: albuterol sulfate
3M MDI Metering          Each actuation          3M MDI Metering        ·USP 29 (Albuterol       3M Health Care   Year of US Approval:
Valvesand HFA-MDI        delivers 120 mcg of     Valves· HFA-MDI        Sulfate) White or                         1996-08-15
Ethanol Formulations     microcrystallized drug. Ethanol Formulations   practically white                         Earliest US Market
technologies. Inactive   Each canister provides                         powder. Freely soluble                    Exclusivity: 2009-01-
components: ethanol,     200 inhalations.                               in water; slightly                        01
oleic acid and non-      Dosed in two                                   soluble in alcohol, in                    Earliest Patent
CFC propellant.          inhalations every 4-6                          chloroform, and in                        Exclusivity: 2009-11-
                         hrs.                                           ether. pKa=9.14.                          28
                                                                        Solubility: 24.5% w/v at
                                                                        pH 7.: albuterol sulfate
SkyePharma will use      -                   Skyepharma HFA   ·Budesonide is a white SkyePharma Plc    Year of EU Approval:
HFA as propellant to                         Formulations     to off-white, odorless                   2006-02-15
replace CFC's in the                                          powder that is
currently marketed                                            practically insoluble in
MDIs. Product                                                 water and in heptane,
developed for                                                 sparingly soluble in
territories outside of                                        ethanol, and freely
the US.                                                       soluble in chloroform.
                                                              Its partition coefficient
                                                              between octanol and
                                                              water at pH 5 is 1.6 x
                                                              10.3 : budesonide


Busedonide (200          200 mcg/dose. Dosed -                ·Budesonide is a white AstraZeneca Plc   Year of EU Approval:
mcg/dose), sorbitam      twice daily.                         to off-white, odorless                   2002-08-12
trioleate, CFC 11, 12,   Can be used with                     powder that is
114.                     Nebuhaler and                        practically insoluble in
                         Nebuchamber.                         water and in heptane,
                                                              sparingly soluble in
                                                              ethanol, and freely
                                                              soluble in chloroform.
                                                              Its partition coefficient
                                                              between octanol and
                                                              water at pH 5 is 1.6 x
                                                              10.3 : budesonide
Pulmicort Respules is    0.5 mg and 1 mg        -   ·Budesonide is a white AstraZeneca Plc      Year of US Approval:
a sterile suspension     nebuliser suspension,      to off-white, odorless                      2000-08-08
for inhalation via jet   Budesonide 0.25            powder that is                              Earliest US Market
nebulizer and contains   mg/ml and 0. 5 mg/ml       practically insoluble in                    Exclusivity: 2006-01-
micronized               respectively.              water and in heptane,                       01
budesonide (0.25 mg      Administered usually 1     sparingly soluble in                        Earliest Patent
and 0.5 mg per 2 mL),     2
                         – mg twice daily.          ethanol, and freely                         Exclusivity: 2006-02-
disodium edetate,                                   soluble in chloroform.                      27
sodium chloride,                                    Its partition coefficient                   Year of EU Approval:
sodium citrate, citric                              between octanol and                         2002-06-11
acid, polysorbate 80,                               water at pH 5 is 1.6 x
and water for                                       10.3 : budesonide
injection.
Pari-LC-Jet plus
Nebulizer/Pari master
compressor system
technology.


Generic for Pulmicort    0.25 mg/2 mL and 0.5 -     ·Budesonide is a white Par Pharmaceutical   Market Launch Date
Respules                 mg/2 mL indicated for      to off-white, odorless Companies Inc.       US: 2008-11-19Year
                         twice daily                powder that is                              of US Approval: 2008-
                                                    practically insoluble in                    11-19
                                                    water and in heptane,
                                                    sparingly soluble in
                                                    ethanol, and freely
                                                    soluble in chloroform.
                                                    Its partition coefficient
                                                    between octanol and
                                                    water at pH 5 is 1.6 x
                                                    10.3 : budesonide
Micronized budesonide 100 mcg and 400 mcg -                        ·Budesonide is a white AstraZeneca Plc         Year of EU Approval:
(200 mcg/dose)         strengths. Dosed                            to off-white, odorless                         2002-06-18
delivered using        twice daily.                                powder that is
Turbuhaler technology.                                             practically insoluble in
                                                                   water and in heptane,
                                                                   sparingly soluble in
                                                                   ethanol, and freely
                                                                   soluble in chloroform.
                                                                   Its partition coefficient
                                                                   between octanol and
                                                                   water at pH 5 is 1.6 x
                                                                   10.3 : budesonide


PulmoSphere™  particle -                       PulmoSpheres®       ·USP 29 (Albuterol)      Nektar Therapeutics   -
processing technology                                              White, crystalline
                                                                   powder. Soluble in
                                                                   alcohol, sparingly
                                                                   soluble in water. Melts
                                                                   at about 156 oC. n-
                                                                   Octanol/Water
                                                                   Partition Coefficient is
                                                                   1.7 x 10 -3 at pH 7.
                                                                   pKa=9.14. : albuterol


SkyeHaler and          Once daily                 SkyeHaler DPI·   ·: indacaterol         -                       -
SkyeProtect.           administration. Phase SkyeProtect™
                       III trial studies 75, 150,
                       300 & 600 µg o.d via
                       SDDPI trials

-                      -                       -                   -                      Novartis AG             -
-                      -                       -                   -                      -                       -
-                      -   -            -                     -                     -




Indacaterol in Fixed   -   TwistHaler   ·: indacaterol·USP 29 Schering-Plough Corp. -
Combination With                        (Mometasone Furoate)
Mometasone Furoate                      White to off-white
Delivered Via a MDDPI                   powder. Melts at about
(Twisthaler). (Source:                  220, with
clinicaltrials/gov,                     decomposition.
NCT00556673)                            Soluble in acetone and
                                        in methylene chloride.:
                                        mometasone furoate
Propellant HFA-134a   50 nad 100 mcg per       -                      ·(EP5.0) A white or      Teva Pharmaceutical   -
(Norflurane) and      actuation inhalers.                             almost white,            Industries Ltd.
ethanol.              Daily doses of 100 to                           crystalline powder,
                      800 mcg in divided                              practically insoluble in
                      doses.                                          water, freely soluble in
                                                                      acetone, sparingly
                                                                      soluble in alcohol.
                                                                      It melts at about 210
                                                                      °C, with
                                                                      decomposition.:
                                                                      beclomethasone
                                                                      dipropionate


Propellant HFA-134a   Qvar 50 and 100          3M MDI Metering        ·(EP5.0) A white or      3M Health Care        Year of EU Approval:
(Norflurane) and      deliver 50 mcg and       Valves· HFA-MDI        almost white,                                  2003-09-24
ethanol.              100 mcg from the         Ethanol Formulations   crystalline powder,
                      actuator respectively.                          practically insoluble in
                      Dosed twice daily.                              water, freely soluble in
                                                                      acetone, sparingly
                                                                      soluble in alcohol.
                                                                      It melts at about 210
                                                                      °C, with
                                                                      decomposition.:
                                                                      beclomethasone
                                                                      dipropionate
Propellant HFA-134a    50 mcg and 100 mcg Easi-Breathe· HFA-         ·(EP5.0) A white or      Teva Pharmaceutical   Year of EU Approval:
(Norflurane) and       per actuation inhalers. MDI Ethanol           almost white,            Industries Ltd.       2004-06-24
ethanol anhydrous in   Dosed at 100-800 mcg Formulations             crystalline powder,
Easi-breathe device    per day in two divided                        practically insoluble in
                       doses.                                        water, freely soluble in
                                                                     acetone, sparingly
                                                                     soluble in alcohol.
                                                                     It melts at about 210
                                                                     °C, with
                                                                     decomposition.:
                                                                     beclomethasone
                                                                     dipropionate


Each unit contains a   Qvar 40 and 80 deliver 3M MDI Metering        ·(EP5.0) A white or      3M Health Care        Year of US Approval:
solution of drug in    40 mcg and 80 mcg      Valves· HFA-MDI        almost white,                                  2000-09-15
ethanol and HFA-134a   from the actuator      Ethanol Formulations   crystalline powder,                            Earliest US Market
non-CFC propellant.    respectively. Each                            practically insoluble in                       Exclusivity: 2009-01-
                       dose is approx. 50                            water, freely soluble in                       01
                       mcL.                                          acetone, sparingly                             Earliest Patent
                       Dosed twice daily.                            soluble in alcohol.                            Exclusivity: 2009-11-
                                                                     It melts at about 210                          28
                                                                     °C, with
                                                                     decomposition.:
                                                                     beclomethasone
                                                                     dipropionate
-                      In Phase 1 trial,      -   -   -                      -
                       patients will be
                       randomized to receive
                       placebo or R1671, at a
                       starting dose of
                       0.0015mg, by
                       intravenous infusion;
                       this dose will be
                       escalated in
                       subsequent groups of
                       patients after a
                       satisfactory
                       assessment of the
                       data from the previous
                       dose. The anticipated
                       time on study
                       treatment is

Small molecules to be Phase 1 trial: Inhaled, -   -   Rigel Pharmaceuticals, -
delivered in          two doses 4 hours               Inc.
undisclosed DPI       apart
device
-   -                    -                     ·: valategrast          -                 -
                                               hydrochloride




-   -                    -                     -                       -                 -




-                                     30
    administered as single Acu-Breathe™ Dose   ·USP 29 (Albuterol       Respirics Inc.   -
    dose dry powder in a Disposable DPI        Sulfate) White or
    novel inhaler                              practically white
                                               powder. Freely soluble
                                               in water; slightly
                                               soluble in alcohol, in
                                               chloroform, and in
                                               ether. pKa=9.14.
                                               Solubility: 24.5% w/v at
                                               pH 7.: albuterol sulfate
Inactive ingredients:   Light yellow dry syrup. -   ·Tranilast occurs as     -   Year of Japan
Sucrose, D-Mannitol,    The usual dosage in         light yellow crystals or     Approval: 1987-10-01
Microcrystalline        children is 0.1 g/kg (5     a crystalline powder. It
cellulose, Carmellose   mg/kg of tranilast)         is odorless and
sodium, Hydroxypropyl   daily in three divided      tasteless. It is freely
cellulose               doses in suspensions        soluble in N,N-
                                                    dimethylformamide,
                                                    soluble in 1,4-dioxane,
                                                    slightly soluble in
                                                    ethanol (99.5), very
                                                    slightly soluble in
                                                    diethyl ether, and
                                                    practically insoluble in
                                                    water.: tranilast
Inactive ingredients:   0.5 and 1 g light yellow -   ·Tranilast occurs as     -               Year of Japan
Lactose, D-Mannitol,    fine granule. The usual      light yellow crystals or                 Approval: 1982-08-01
Hydroxypropyl           adult dosage is one          a crystalline powder. It
cellulose, Talc         gram (100 mg of              is odorless and
                        tranilast) three times       tasteless. It is freely
                        daily. The usual             soluble in N,N-
                        dosage in children is        dimethylformamide,
                        0.05 g/kg (5 mg /kg of       soluble in 1,4-dioxane,
                        tranilast) daily in three    slightly soluble in
                        divided doses.               ethanol (99.5), very
                                                     slightly soluble in
                                                     diethyl ether, and
                                                     practically insoluble in
                                                     water.: tranilast




-                       -                        -   -                        MedPharm Ltd.   -
-                          -                       -   -                       -                       -




Inhalation solution for    2.25% inhalation        -   ·USP 29                   Nephron               -
use in aerosol             solution. If                (Racepinephrine)          Pharmaceuticals Corp.
bronchodilator therapy     administered via            White to nearly white,
employing hand-bulb        hand-bulb nebulizer,        crystalline, odorless
nebulizer or oxygen        racepinephrine              powder, gradually
aerosolization. Inactive   inhalation solution         darkening on exposure
ingredients: Benzoic       does not require            to light and air. With
Acid, Chlorobutanol,       dilution; however, if       acids, it forms salts
Potassium                  administered via jet        that are readily soluble
Metabisulfite,             nebulizer, it should be     in water, and the base
Propylene Glycol,          diluted to a                may be recovered by
Sodium Chloride,           volume of 3 to 5 mL         the addition of
Sodium Metabisulfite,      with sterile 0.9%           ammonium hydroxide.
Water for Injection        sodium chloride             Very slightly soluble in
                           solution. For use in        water and in alcohol;
                           hand-bulb nebulizer: 1      insoluble in ether, in
                           to 3 inhalations not        chloroform, and in
                           more                        fixed and volatile oils.:
                           often than every 3          racepinephrine
                           hours. For use in a jet
                           nebulizer:
                           Administered for
                           fifteen minutes every
                           three to four hours.
-   Reslizumab 1 mg/kg, 2 -                 ·: reslizumab   -                     -
    mg/kg, 3 mg/kg were
    studied in the Phase 2-
    3 trials. IV
    administration once
    monthly.Phase 2-3
    trials




-   -                     Airmax/Spriomax   ·: etiprednol   Teva Pharmaceutical   -
                                            dicloacetate    Industries Ltd.


-   -                     -                 -               Respivert, Inc        -
Oral inhalation solution   The recommended        -             ·White to off-white      GlaxoSmithKline Plc   Year of EU Approval:
via a nebuliser.           dose is 0.4 to 2ml                   crystalline substance,                         2003-04-15
1ml or 2ml plastic         solution (100-500                    freely soluble in water
ampoules containing        micrograms) up to four               and lower alcohols. It
0.25mg/ml of               times daily.                         is a quaternary
Ipratropium Bromide                                             ammonium compound
Ph.Eur. Sodium                                                  and thus exists in an
Chloride, Diluted                                               ionized state in
Phosphoric Acid,                                                aqueous solutions. It is
Purified Water                                                  relatively insoluble in
                                                                non-polar media.. The
                                                                pH of a 1% solution in
                                                                water is 5.0 to 7.5. :
                                                                ipratropium bromide
                                                                hydrate




AeroEclipse Nebulizer 10 mg, 50 mg, 100           AeroEclipse   -                      Trudell Medical         -
                      mg, or 200 mg                                                    International
                      nebulizer charge
-   100 mg tablets. Three -   ·Tranilast occurs as     -   -
    times daily.              light yellow crystals or
                              a crystalline powder. It
                              is odorless and
                              tasteless. It is freely
                              soluble in N,N-
                              dimethylformamide,
                              soluble in 1,4-dioxane,
                              slightly soluble in
                              ethanol (99.5), very
                              slightly soluble in
                              diethyl ether, and
                              practically insoluble in
                              water.: tranilast




-   10% granules          -   ·: repirinast            -   -




-   150 mg tablets.       -   ·: repirinast            -   -
-                  -   -   ·: S-5751            -                      -


-                  -   -   -                    -                      -

-                  -   -   -                    -                      -

-                  -   -   -                    -                      -

-                  -   -   -                    -                      -

inhaled IFN-beta   -   -   ·: interferon beta   Dr. Rentschler Holding -
                                                GmbH & Co. KG




inhaled IFN-beta   -   -   ·: interferon beta   Dr. Rentschler Holding -
                                                GmbH & Co. KG




-                  -   -   -                    -                      -
-                  -   -   -                    -                      -

-                  -   -   -                    -                      -
-                  -   -   -                    -                      -
-                        -            -          -                    -                   -




An IFN&#946;             -            -          ·: interferon beta   Synairgen           -
formulation suitable for
inhalation through an
appropriate aerosol
delivery system




Barrier function protein -            -          -                    -                   -




-                        -            -          -                    -                   -




-                        -            -          -                    -                   -


Undisclosed device.      Once a day   SunHaler   -                    Sun Pharma          -
Possibly SunHaler.                                                    Advanced Research
                                                                      Company Ltd
Delivers 100 mcg drug Dosed 1-2 puffs up to   Easi-Breathe   ·USP 29 (Albuterol)      Teva Pharmaceutical   Year of EU Approval:
in alcohol. HFA used 4 times daily                           White, crystalline       Industries Ltd.       2000
as propellant. 200                                           powder. Soluble in
doses per unit.                                              alcohol, sparingly
List of Excipients:                                          soluble in water. Melts
Ethanol, anhydrous                                           at about 156 oC. n-
Norflurane (Propellant                                       Octanol/Water
HFA-134a)                                                    Partition Coefficient is
Salamol Easi-Breathe                                         1.7 x 10 -3 at pH 7.
CFC-Free Inhaler                                             pKa=9.14. : albuterol
contains a new
propellant (HFA-
134a)
and does not contain
any chlorofluorocarbon
(CFC) propellants.


EasiBreathe with      100 microgram dose      Easi-Breathe   ·USP 29 (Albuterol)      Teva Pharmaceutical   -
CFC's                                                        White, crystalline       Industries Ltd.
                                                             powder. Soluble in
                                                             alcohol, sparingly
                                                             soluble in water. Melts
                                                             at about 156 oC. n-
                                                             Octanol/Water
                                                             Partition Coefficient is
                                                             1.7 x 10 -3 at pH 7.
                                                             pKa=9.14. : albuterol
3M MDI Metering       Metered dose inhaler   3M MDI Metering   ·USP 29 (Albuterol)      3M Health Care         -
Valves technology.                           Valves            White, crystalline
HFA 134-A formulation                                          powder. Soluble in
in an improved                                                 alcohol, sparingly
Autohaler device for                                           soluble in water. Melts
easy use.                                                      at about 156 oC. n-
                                                               Octanol/Water
                                                               Partition Coefficient is
                                                               1.7 x 10 -3 at pH 7.
                                                               pKa=9.14. : albuterol


-                       -                    CycloHaler        ·USP 29 (Albuterol)      Teva Pharmaceutical    -
                                                               White, crystalline       Industries Ltd.
                                                               powder. Soluble in
                                                               alcohol, sparingly
                                                               soluble in water. Melts
                                                               at about 156 oC. n-
                                                               Octanol/Water
                                                               Partition Coefficient is
                                                               1.7 x 10 -3 at pH 7.
                                                               pKa=9.14. : albuterol


Phares lipid based      -                    SupraVail MLM     ·USP 29 (Albuterol)      Phares Drug Delivery   -
HFA formulation that is                                        White, crystalline       AG
stable for 2 years.                                            powder. Soluble in
                                                               alcohol, sparingly
                                                               soluble in water. Melts
                                                               at about 156 oC. n-
                                                               Octanol/Water
                                                               Partition Coefficient is
                                                               1.7 x 10 -3 at pH 7.
                                                               pKa=9.14. : albuterol
-                    The usual dose for an -             ·USP 29 (Albuterol)      Galen Limited       -
                     adult is 2.5 or 5 mg up             White, crystalline
                     to 4 times a day.                   powder. Soluble in
                                                         alcohol, sparingly
                                                         soluble in water. Melts
                                                         at about 156 oC. n-
                                                         Octanol/Water
                                                         Partition Coefficient is
                                                         1.7 x 10 -3 at pH 7.
                                                         pKa=9.14. : albuterol


TAIFUN® DPI          200 doses per unit.   TAIFUN® DPI   ·USP 29 (Albuterol)      Akela Pharma Inc.   -
technology. 50 and   Dose up to 4 times                  White, crystalline
100 mcg salbutamol   daily.                              powder. Soluble in
and lactose.                                             alcohol, sparingly
                                                         soluble in water. Melts
                                                         at about 156 oC. n-
                                                         Octanol/Water
                                                         Partition Coefficient is
                                                         1.7 x 10 -3 at pH 7.
                                                         pKa=9.14. : albuterol
-   Once-daily dosing   -   ·: senicapoc           -                -




-   -                   -   ·Ciclesonide is a white Sepracor Inc.   -
                            to yellow-white
                            powder, practically
                            insoluble in water and
                            freely
                            soluble in ethanol and
                            acetone: ciclesonide
25 micrograms of         25/50, 25/125 and        -   ·A white to off-white   GlaxoSmithKline Plc   Year of EU Approval:
salmeterol (as           25/250 mcg/actuation.        powder. It is freely                          2000-06-16
salmeterol xinafoate)    Dosed as two                 soluble in methanol;
and 50, 125 or 250       inhalations twice daily.     slightly soluble in
micrograms of                                         ethanol, chloroform,
fluticasone propionate                                and isopropanol; and
(delivered from the                                   sparingly soluble in
valve). This is                                       water.
equivalent to 21
micrograms of                                         : salmeterol
salmeterol and 44                                     xinafoate·(EP5.0)
micrograms, 110                                       White or almost white
micrograms and 220                                    powder. Practically
micrograms of                                         insoluble in water,
fluticasone propionate                                sparingly soluble in
delivered from the                                    methylene chloride,
actuator (delivered                                   slightly soluble in
dose). Excipients:                                    alcohol.: fluticasone
Norflurane (HFA                                       propionate
134a).
Disks comprising four   One blister (50          Diskhaler   ·A white to off-white    GlaxoSmithKline Plc   Year of EU Approval:
regularly spaced        micrograms) twice                    powder. It is freely                           1996-10-14
double-foil blisters    daily, increasing to two             soluble in methanol;
each delivering a       blisters (2 x 50                     slightly soluble in
mixture of 50           micrograms) twice                    ethanol, chloroform,
micrograms salmeterol   daily if required.                   and isopropanol; and
(as xinafoate) and                                           sparingly soluble in
lactose used in a                                            water.
Diskhaler device.
                                                             : salmeterol xinafoate
DISKUS device             Teal green unit         Diskus/AccuHaler   ·A white to off-white    GlaxoSmithKline Plc   Year of US Approval:
technology.Specially      containing 60 blisters.                    powder. It is freely                           1997-09-19
designed plastic          Each blister contains                      soluble in methanol;                           Earliest US Market
devices containing a      50 mcg of drug                             slightly soluble in                            Exclusivity: 2008-01-
double foil blister.      blended with lactose to                    ethanol, chloroform,                           01
Each blister contains     a weight of 12.5 mg.                       and isopropanol; and                           Earliest Patent
50 mcg of drug                                                       sparingly soluble in                           Exclusivity: 2008-02-
blended with lactose to    The drug product is                       water.                                         12
a weight of 12.5 mg.      packaged within a teal                                                                    Year of EU Approval:
                          green, plastic-coated,                     : salmeterol xinafoate                         2000-07-13
                          moisture-protective foil
                          pouch. Contents are
                          inhaled twice daily.


Pressurised inhalation White to off white       -                    ·A white to off-white    GlaxoSmithKline Plc   Year of EU Approval:
suspension.             suspension sealed in                         powder. It is freely                           2005-10-28
Norflurane (HFA         an aluminium canister                        soluble in methanol;
134a), a                in a green actuator.                         slightly soluble in
hydrofluoroalkane (non- One metered dose (ex-                        ethanol, chloroform,
chlorofluorocarbon)     valve) contains 25                           and isopropanol; and
propellant              micrograms salmeterol                        sparingly soluble in
                        (as xinafoate). This is                      water.
                        equivalent to a
                        delivered dose (ex-                          : salmeterol xinafoate
                        actuator) of 21
                        micrograms salmeterol
                        (as xinafoate). Two
                        actuations of 25
                        micrograms salmeterol
                        twice daily.
A pressurized,              Inhalation Aerosol is   -   ·A white to off-white    GlaxoSmithKline Plc   Year of US Approval:
metered-dose aerosol        supplied in 13-g            powder. It is freely                           1994-02-04
unit for oral inhalation.   canisters containing        soluble in methanol;                           Earliest US Market
It contains a               120 metered                 slightly soluble in                            Exclusivity: 2008-01-
microcrystalline            actuations in boxes of      ethanol, chloroform,                           01
suspension of               1. Each actuation           and isopropanol; and                           Earliest Patent
salmeterol xinafoate in     delivers 25 mcg of          sparingly soluble in                           Exclusivity: 2008-02-
a mixture of 2              salmeterol base (as         water.                                         12
chlorofluorocarbon          salmeterol xinafoate)
propellants                 from the valve and 21       : salmeterol xinafoate
(trichlorofluoromethan      mcg of salmeterol
e and                       base (as salmeterol
dichlorodifluoromethan      xinafoate) from the
e) with soya lecithin.      actuator. Each canister
36.25 mcg of                is supplied with a
salmeterol xinafoate is     green plastic actuator.
equivalent to 25 mcg        Twice daily
of salmeterol base.         administration.
Each actuation
delivers 25 mcg of
salmeterol base (as
salmeterol xinafoate)
from the valve and 21
mcg of salmeterol
base (as salmeterol
xinafoate) from the
actuator. Each 6.5-g
canister provides 60
inhalations and each
13-g canister provides
120 inhalations
SIMPONI does not            SIMPONI must be         Smartject   ·: golimumab   -   Year of US Approval:
contain preservatives.      refrigerated at 2ºC to                                 2009-04-24
The solution is clear to    8ºC (36ºF to 46ºF) and
slightly opalescent,        protected from light..
colorless to light yellow   Each single dose
with a pH of                SmartJect autoinjector
approximately 5.5.          contains a prefilled
SIMPONI is provided         glass syringe (27
in one strength: 50 mg      gauge ½ inch)
of the golimumab            providing 50 mg of
antibody in 0.5 mL of       SIMPONI per 0.5 mL
solution. Each 0.5 mL       of solution. Each
of SIMPONI contains         single dose prefilled
50 mg of the                glass syringe (27
golimumab antibody,         gauge ½ inch)
0.44 mg of L-histidine      contains 50 mg of
and L-histidine             SIMPONI per 0.5 mL
monohydrochloride           of solution. The
monohydrate, 20.5 mg        SIMPONI dose
of sorbitol, 0.08 mg of     regimen is 50 mg
polysorbate 80, and         administered by
Water for Injection.        subcutaneous (SC)
                            injection once a
                            month. For patients
                            with rheumatoid
                            arthrtis (RA), SIMPONI
                            should be given in
                            combination with
                            methotrexate and for
                            patients with psoriatic
                            arthrtis (PsA) or
                            ankylosing spondylitis
                            (AS), SIMPONI
                            may be given with or
Inactive ingredients:    4 mg (oval) and 5 mg -     ·Montelukast sodium is Merck and Co Inc.   Year of US Approval:
mannitol,                (round), pink, biconvex-   a hygroscopic,                             1998-02-20
microcrystalline         shaped chewable            optically active, white                    Earliest US Market
cellulose,               tablets.                   to off-white powder.                       Exclusivity: 2008-08-
hydroxypropyl            The dosage for             Montelukast sodium is                      27
cellulose, red ferric    pediatric patients 6 to    freely soluble in                          Earliest Patent
oxide, croscarmellose    14 years of age is one     ethanol, methanol, and                     Exclusivity: 2012-02-
sodium, cherry flavor,   5-mg chewable tablet       water and practically                      03
aspartame and            daily.                     insoluble in                               Year of EU Approval:
magnesium stearate.      The dosage for             acetonitrile. :                            1998-01-15
                         pediatric patients 2 to    montelukast sodium                         Year of Japan
                         5 years of age is one 4-                                              Approval: 2001-08-01
                         mg chewable tablet
                         daily

                         In Japan,
                         recommended dosage
                         for pediatric patients
                         aged 6 years or older
                         is 5 mg as
                         montelukast orally
                         administered once
                         daily
                         before sleep.
Inactive ingredients:   SINGULAIR Oral         -   ·Montelukast sodium is -   Year of US Approval:
mannitol,               Granules are supplied      a hygroscopic,             2002-07-26
hydroxypropyl           as 4 mg white              optically active, white    Earliest US Market
cellulose, and          granules with 500 mg       to off-white powder.       Exclusivity: 2008-08-
magnesium stearate      net weight. Once daily     Montelukast sodium is      27
                        administration             freely soluble in          Year of EU Approval:
                                                   ethanol, methanol, and     2003-02-14
                                                   water and practically
                                                   insoluble in
                                                   acetonitrile. :
                                                   montelukast sodium
Inactive ingredients:      beige, rounded square- -   ·Montelukast sodium is -                   Year of US Approval:
microcrystalline           shaped, film-coated 10-    a hygroscopic,                             1998-02-20
cellulose, lactose         mg Singulair tablet        optically active, white                    Earliest US Market
monohydrate,               contains 10.4 mg           to off-white powder.                       Exclusivity: 2008-08-
croscarmellose             montelukast sodium,        Montelukast sodium is                      27
sodium, hydroxypropyl      which is the molar         freely soluble in                          Earliest Patent
cellulose, and             equivalent to 10.0 mg      ethanol, methanol, and                     Exclusivity: 2012-02-
magnesium stearate.        of free acid.              water and practically                      03
The film coating           The dosage for             insoluble in                               Year of EU Approval:
consists of:               adolescents and adults     acetonitrile. :                            1998-01-15
hydroxypropyl              15 years of age and        montelukast sodium                         Year of Japan
methylcellulose,           older is one 10 mg                                                    Approval: 2001-08-01
hydroxypropyl              tablet daily.
cellulose, titanium        In clinical studies, a
dioxide, red iron oxide,   single tablet of
yellow iron oxide, and     SINGULAIR 10 mg
carnauba wax.              prevented EIB when
                           taken two hours before
                           exercise [19670].



Sirna is currently        -                       -   -                      Merck and Co Inc.   -
developing siRNAs
formulated to provide a
long duration of activity
after local
administration to the
lungs.
-   25 and 50 mg tablets.   -   ·Odorless, white to   -   -
    Three times daily.          yellowish white
                                crystalline powder:
                                amlexanox
Inactive ingredients:    2.5 microgram          Respimat   ·Tiotropium bromide is Boehringer Ingelheim   Year of EU Approval:
Benzalkonium             tiotropium per puff (2            a white or yellowish                          2007-09-12
chloride; disodium       puffs comprise one                white powder. It is
edetate; water,          medicinal dose) and is            sparingly soluble in
purified; Hydrochloric   equivalent to 3.124               water and soluble in
acid 3.6 % (for pH       microgram tiotropium              methanol. : tiotropium
adjustment)              bromide monohydrate.              bromide monohydrate
                         The recommended
                         dose for adults is 5
                         microgram tiotropium
                         given as two puffs
                         from the Respimat
                         inhaler once daily, at
                         the same time of the
                         day. The
                         recommended dose
                         should not be
                         exceeded.
SPIRIVA HandiHaler        SPIRIVA capsules,     HandiHaler   ·Tiotropium bromide is Boehringer Ingelheim   Year of US Approval:
consists of a capsule     contain 18 mcg                     a white or yellowish                          2004-01-30
dosage form               tiotropium, are light              white powder. It is                           Earliest US Market
containing a dry          green. The                         sparingly soluble in                          Exclusivity: 2009-01-
powder formulation of     recommended dosage                 water and soluble in                          30
SPIRIVA (tiotropium       of SPIRIVA                         methanol. : tiotropium                        Earliest Patent
bromide) intended for     HandiHaler is the                  bromide monohydrate                           Exclusivity: 2014-03-
oral inhalation only      inhalation of the                                                                11
with the HandiHaler       contents of one
inhalation device. Each   SPIRIVA capsule,
light green, hard         once-daily
gelatin capsule
contains 18 mcg
tiotropium (equivalent
to 22.5 mcg tiotropium
bromide monohydrate)
blended with lactose
monohydrate as the
carrier.
-   10 and 20 mcg tablets. -   ·(EP5.0) A white or       -   -
    20-40 mcg twice daily.     almost white,
                               crystalline powder,
                               soluble in water and in
                               alcohol, slightly soluble
                               in acetone. It melts at
                               about 173 °C, with
                               decompositio:
                               clenbuterol
                               hydrochloride
Each 10.2 g Symbicort     Administered twice      -   ·Budesonide is a white AstraZeneca Plc   Year of US Approval:
80/4.5 or 160/4.5         daily. The inhaler          to off-white, odorless                   2006-07-21
cannister is formulated   should be primed            powder that is                           Earliest US Market
with HFA 227              before using for the        practically insoluble in                 Exclusivity: 2009-07-
propelled pressurized     first time by releasing     water and in heptane,                    21
metered dose inhaler      two test sprays. In         sparingly soluble in
containing 120            cases where the             ethanol, and freely
actuations. After         inhaler has not been        soluble in chloroform.
priming, each             used in seven days or       Its partition coefficient
actaution delivers        when it has been            between octanol and
91/5.1 micrograms or      dropped, prime the          water at pH 5 is 1.6 x
181/5.1 micrograms        inhaler again by            10.3 : budesonide·It
from the valve and        shaking well for 5          occurs as a white or
either 80/4.5 or          seconds and releasing       pale yellowish white
160/4.5 micrograms        2 test sprays into the      crystalline powder. It is
from the actuator. The    air.                        freely soluble in acetic
formulation contains                                  acid (100), soluble in
micronized drugs,                                     methanol, very slightly
povidone K-25, and                                    soluble in water or
polyethylene glycol                                   ethanol (95), and
1000                                                  practically insoluble in
                                                      diethyl ether. Its
                                                      methanol solution (1
                                                      &#8594; 100) shows
                                                      no optical rotation.:
                                                      formoterol fumarate
                                                      dihydrate
Turbuhaler DPI device 100/6 Turbohaler:      Turbuhaler   ·Budesonide is a white AstraZeneca Plc   Year of EU Approval:
with lactose          Each delivered dose                 to off-white, odorless                   2001-05-15
formulation           contains: budesonide                powder that is
                      80 mcg/inhalation and               practically insoluble in
                      formoterol fumarate                 water and in heptane,
                      dihydrate 4.5                       sparingly soluble in
                      mcg/inhalation. 200/6               ethanol, and freely
                      Turbohaler: Each                    soluble in chloroform.
                      delivered dose                      Its partition coefficient
                      contains: budesonide                between octanol and
                      160 mcg/inhalation                  water at pH 5 is 1.6 x
                      and formoterol                      10.3 :
                      fumarate dihydrate 4.5              budesonide·White to
                      mcg/inhalation. 400/12              yellow crystal slightly
                      Turbohaler: Each                    soluble in water.:
                      delivered dose                      formoterol
                      contains: budesonide
                      320 mcg/inhalation
                      and formoterol
                      fumarate dihydrate 9
                      mcg/inhalation.
                      Asthma
                      Adults(18 years and
                      older):
                      80/4.5 and 160/4.5
                      mcg/inhalation:Usual
                                2
                      dose is 1– inhalations
                      twice daily. Maximum
                      dose is 4 inhalations
                      twice daily.
                      320/9
                      mcg/inhalation:Usual
                      dose is 1 inhalation
                      twice daily. Maximum
-   -   -   -   Synairgen            -




-   -   -   -   -                    -




-   -   -   -   Targepeutics, Inc.   -




-   -   -   -   Targepeutics, Inc.   -
-                -                        -           -                      Targepeutics, Inc.     -




-                In a Phase II study, the -           ·: bimosiamose         Revotar                -
                 dosage was 70 mg of                                         Biopharmaceuticals
                 Bimosiamose twice a                                         AG
                 day. [27616]
-                -                        -           -                      -                      -

-                -                        -           -                      -                      -

Captisol based   -                        CAPTISOL®   -                      CyDex                  -
formulation                                                                  Pharmaceuticals, Inc




-                -                        -           -                      -                      -

-                -                        -           -                      -                      -




-                600 micrograms dosed -               ·: nitric oxide-donating Nicox SA             -
                 in Phase II [1307]                   derivative of
                                                      budesonide
Undisclosed nebulizer 250 micrgrams and       -   -   Topigen                -
                      500 micrograms once             Pharmaceuticals Inc.
                      a day over a 14-day
                      period being studied in
                      Phase II [17654]




-                      -                      -   -   -                      -
TUSSI-12D is an           5 mL (one               -   ·: carbetapentane     -   -
antitussive/antihistami   teaspoonful) of the         tannate·: pyrilamine
ne/nasal decongestant     blue-colored, grape-        tannate·:
combination available     flavored suspension         phenylephrine tannate
for oral administration   containing
as a Suspension.          Carbetapentane
Other ingredients:        Tannate 30 mg,
benzoic acid, FD&C        Pyrilamine Tannate 30
Blue No. 1, FD&C Red      mg, Phenylephrine
No. 3, FD&C Red No.       Tannate 5 mg. 5 to 10
40, FD&C Yellow No. 5     mL (1 to 2
(see Precautions),        teaspoonfuls) for
flavors (natural and      children over six years
artificial), glycerin,    of age and 2.5 to 5 mL
kaolin, magnesium         (1/2 to 1 teaspoonful)
aluminum silicate,        for children two to six
methylparaben, pectin,    years of age. The
purified water,           recommended dose
saccharin sodium,         should be
sucrose.                  administered every 12
                          hours.
TUSSI-12D is an           Pink-colored, capsule- -             ·: carbetapentane     -                    -
antitussive/antihistami   shaped tablet                        tannate·: pyrilamine
ne/nasal decongestant     containing                           tannate·:
combination available     Carbetapentane                       phenylephrine tannate
for oral administration   Tannate 60 mg,
as Tablets. Other         Pyrilamine Tannate 40
ingredients: corn         mg, Phenylephrine
starch, dibasic calcium   Tannate 10 mg. 1 or 2
phosphate, FD&C Blue      tablets for adults and
No. 1, FD&C Red No.       children 12 years of
40, magnesium             age and older and 1/2
stearate,                 or 1 tablet for children
methylcellulose,          6 to 11 years. The
polygalacturonic          recomended dose
acid,                     should be
povidone, silicon         administered every 12
dioxide, talc.            hours.




Taifun DPI                -                      TAIFUN® DPI   ·Budesonide is a white Akela Pharma Inc.   -
                                                               to off-white, odorless
                                                               powder that is
                                                               practically insoluble in
                                                               water and in heptane,
                                                               sparingly soluble in
                                                               ethanol, and freely
                                                               soluble in chloroform.
                                                               Its partition coefficient
                                                               between octanol and
                                                               water at pH 5 is 1.6 x
                                                               10.3 : budesonide
Taifun DPI              -   TAIFUN® DPI   ·White to yellow crystal Akela Pharma Inc.   -
                                          slightly soluble in
                                          water.: formoterol



Miat-Haler, multidose   -   Miat-Haler    ·(EP5.0) A white or      Miat Spa            -
DPI.                                      almost white,
                                          crystalline powder,
                                          practically insoluble in
                                          water, freely soluble in
                                          acetone, sparingly
                                          soluble in alcohol.
                                          It melts at about 210
                                          °C, with
                                          decomposition.:
                                          beclomethasone
                                          dipropionate


Tempo pMDI              -   Tempo         ·(EP5.0) White or        MAP Pharmaceuticals -
                                          almost white powder. Inc.
                                          Practically insoluble in
                                          water, sparingly
                                          soluble in methylene
                                          chloride, slightly
                                          soluble in alcohol.:
                                          fluticasone propionate
Uses Osmodex            300mg plus once daily. Osmodex/TechnoPho ·USP 29                  Osmotica      Year of EU Approval:
Osmotic tablet          Boxes of 15 and 30     enix/ProSLO®      (Theophylline) White, Pharmaceutical   1997
technology. Each        coated extended-                         odorless, crystalline
extended-release        release tablets as                       powder, having a bitter
tablet as SOL           osmotic release                          taste. Is stable in air.
(Osmotic Release        system                                   Slightly soluble in
System)                                                          water, but more
contains:Theophylline                                            soluble in hot water;
(as monoethalomine),                                             freely soluble in
300 mg; anhydrous                                                solutions of alkali
theophylline, 100 mg                                             hydroxides and in
                                                                 ammonia; sparingly
                                                                 soluble in
                                                                 alcohol, in chloroform,
                                                                 and in ether.:
                                                                 theophylline
Mystic EHD nebulizer   -   Mystic™   ·USP 29 (Terbutaline Ventaira   -
                                     Sulfate) White to gray-
                                     white, crystalline
                                     powder. Is odorless or
                                     has a faint odor of
                                     acetic acid. Soluble in
                                     water and in 0.1 N
                                     hydrochloric acid;
                                     slightly soluble in
                                     methanol; insoluble in
                                     chloroform.: terbutaline
                                     sulfate
(Japan label) Inactive      100, 200, 300 mg, and -    ·USP 29                  Elan Corporation Plc.   Year of US Approval:
ingredient: (100 mg):       450 mg extended            (Theophylline) White,                            1980-01-31
Sucrose, corn starch,       release tablets. The       odorless, crystalline                            Year of Japan
lactose, magnesium          usual adult dosage is      powder, having a bitter                          Approval: 1984-04-01
stearate, acacia,           200 mg of theophylline     taste. Is stable in air.
cellulose acetate           (2 tablets) twice daily.   Slightly soluble in
phthalate,                  The usual children         water, but more
talc, sodium lauryl         dosage is 100 - 200        soluble in hot water;
sulfate, gryceryl           mg (1-2 tablets) twice     freely soluble in
stearate,                   daily. 400 mg of           solutions of alkali
white beeswax,              theophylline (2 tablets)   hydroxides and in
cetanol, myristyl           may be orally              ammonia; sparingly
alcohol, diethyl            administered to adult      soluble in
phthalate (200 mg):         patients with bronchial    alcohol, in chloroform,
Sucrose, corn starch,       asthma once daily at       and in ether.:
lactose, magnesium          bedtime.                   theophylline
stearate, cellulose
acetate phthalate,
hydroxypropylmethylce
llulose, gryceryl
stearate, white
beeswax, cetanol,
myristyl alcohol, diethyl
phthalate
Microencapsulated        50 mg, 75 mg, 125       -   ·USP 29                  Elan Corporation Plc.   Year of US Approval:
beads consisting of      mg, or 200 mg               (Theophylline) White,                            1985-09-10
ethylcellulose,          capsules. The entire        odorless, crystalline
hydroxypropylcellulose   contents of a Theo-Dur      powder, having a bitter
, povidone, and          Sprinkle capsule are        taste. Is stable in air.
sucrose                  intended to be              Slightly soluble in
                         sprinkled on a small        water, but more
                         amount of soft food         soluble in hot water;
                         immediately prior to        freely soluble in
                         ingestion, or it may be     solutions of alkali
                         swallowed whole.            hydroxides and in
                         Administered 2-3 times      ammonia; sparingly
                         daily.                      soluble in
                                                     alcohol, in chloroform,
                                                     and in ether.:
                                                     theophylline
Generic for TheoDur   300 mg, 400 mg, 450   -   ·USP 29                  Sun Pharmaceutical   Year of US Approval:
                      mg, 600 mg tablets        (Theophylline) White, Industries              2004-04-30
                                                odorless, crystalline
                                                powder, having a bitter
                                                taste. Is stable in air.
                                                Slightly soluble in
                                                water, but more
                                                soluble in hot water;
                                                freely soluble in
                                                solutions of alkali
                                                hydroxides and in
                                                ammonia; sparingly
                                                soluble in
                                                alcohol, in chloroform,
                                                and in ether.:
                                                theophylline

Generic for Theodur   200 and 300 mg        -   ·USP 29                  URL Pharma, Inc.     -
                      sustained release         (Theophylline) White,
                      tablets.                  odorless, crystalline
                                                powder, having a bitter
                                                taste. Is stable in air.
                                                Slightly soluble in
                                                water, but more
                                                soluble in hot water;
                                                freely soluble in
                                                solutions of alkali
                                                hydroxides and in
                                                ammonia; sparingly
                                                soluble in
                                                alcohol, in chloroform,
                                                and in ether.:
                                                theophylline
Sustained release   200 mg and 300 mg   -   ·USP 29                  United         -
capsules            sustained release       (Theophylline) White, Pharmaceuticals
                    capsules                odorless, crystalline
                                            powder, having a bitter
                                            taste. Is stable in air.
                                            Slightly soluble in
                                            water, but more
                                            soluble in hot water;
                                            freely soluble in
                                            solutions of alkali
                                            hydroxides and in
                                            ammonia; sparingly
                                            soluble in
                                            alcohol, in chloroform,
                                            and in ether.:
                                            theophylline
Inactive ingredients:     Each 1 g of white,     -   ·USP 29                  Eisai Co. Ltd   Year of Japan
light anhydrous silicic   sustained-release          (Theophylline) White,                    Approval: 1987-10-01
acid, hydrogenated oil,   granules contains 500      odorless, crystalline
talc, povidone K30 and    mg of theophylline.        powder, having a bitter
hydrated silicon          The usual adult            taste. Is stable in air.
dioxide                   dosage for oral use is     Slightly soluble in
                          0.4 g of theophylline      water, but more
                          twice daily                soluble in hot water;
                                                     freely soluble in
                                                     solutions of alkali
                                                     hydroxides and in
                                                     ammonia; sparingly
                                                     soluble in
                                                     alcohol, in chloroform,
                                                     and in ether.:
                                                     theophylline
Inactive ingredients:     50, 100 and 200 mg      -   ·USP 29                  Eisai Co. Ltd   Year of Japan
ethylcellulose,           white, speckled             (Theophylline) White,                    Approval: 1987-10-01
croscarmellose            sustained-release           odorless, crystalline
sodium, light             tablets. The usual          powder, having a bitter
anhydrous silicic acid,   adult dosage for oral       taste. Is stable in air.
microcrystalline          use is 200 mg of            Slightly soluble in
cellulose,                theophylline                water, but more
hydrogenated oil,         twice daily.                soluble in hot water;
calcium stearate, talc,                               freely soluble in
corn starch, lactose,                                 solutions of alkali
hydroxypropylcellulose                                hydroxides and in
and hydrated silicon                                  ammonia; sparingly
dioxide.                                              soluble in
                                                      alcohol, in chloroform,
                                                      and in ether.:
                                                      theophylline
-                   -   Minextab           ·USP 29                  Galenix             -
                                           (Theophylline) White,
                                           odorless, crystalline
                                           powder, having a bitter
                                           taste. Is stable in air.
                                           Slightly soluble in
                                           water, but more
                                           soluble in hot water;
                                           freely soluble in
                                           solutions of alkali
                                           hydroxides and in
                                           ammonia; sparingly
                                           soluble in
                                           alcohol, in chloroform,
                                           and in ether.:
                                           theophylline

12 hour sustained   -   SCOLR Amino Acid   ·USP 29                  SCOLR Pharma Inc.   -
release tablets         CDT                (Theophylline) White,
                                           odorless, crystalline
                                           powder, having a bitter
                                           taste. Is stable in air.
                                           Slightly soluble in
                                           water, but more
                                           soluble in hot water;
                                           freely soluble in
                                           solutions of alkali
                                           hydroxides and in
                                           ammonia; sparingly
                                           soluble in
                                           alcohol, in chloroform,
                                           and in ether.:
                                           theophylline
-   100 mg, 125 mg, 200    -   ·USP 29                  Forest Laboratories   Year of US Approval:
    mg, 300 mg capsules        (Theophylline) White, Inc                      1994-02-14
    administered twice a       odorless, crystalline
    day.                       powder, having a bitter
                               taste. Is stable in air.
                               Slightly soluble in
                               water, but more
                               soluble in hot water;
                               freely soluble in
                               solutions of alkali
                               hydroxides and in
                               ammonia; sparingly
                               soluble in
                               alcohol, in chloroform,
                               and in ether.:
                               theophylline

-   100 mg, 200 mg, 300 -      ·USP 29                  Forest Laboratories   Year of US Approval:
    mg and 450 mg tablets      (Theophylline) White, Inc                      1985-02-21
                               odorless, crystalline
                               powder, having a bitter
                               taste. Is stable in air.
                               Slightly soluble in
                               water, but more
                               soluble in hot water;
                               freely soluble in
                               solutions of alkali
                               hydroxides and in
                               ammonia; sparingly
                               soluble in
                               alcohol, in chloroform,
                               and in ether.:
                               theophylline
Pressurized inhalation   The initial dose is 4 mg -   ·Nedocromil sodium, a Sanofi-Aventis   Year of EU Approval:
suspension. HFA          (2 actuations) four          yellow powder, is                      2005-10-11
based MDI containing     times daily. Once            soluble in water:
1,1,1,2,3,3,3 -          control of symptoms          nedocromil sodium
heptafluoropropane       has been achieved it
(HFA-227), povidone      may be possible to
K30, polyethylene        reduce the dose to a
glycol (PEG) 600,        maintenance dose of
levomenthol              4mg (2 actuations)
                         twice daily. The
                         aluminium can is fitted
                         with a metering valve
                         which delivers
                         actuations each
                         containing 2 mg of
                         nedocromil sodium.
                         Each canister contains
                         112 actuations. Tilade
                         CFC-Free Inhaler: The
                         cartoned pack consists
                         of an aerosol canister
                         and two plastic
                         adaptors with dustcaps
Tilade Inhaler is a       16.2 gram container      -   ·Nedocromil sodium, a Sanofi-Aventis   Year of US Approval:
pressurized metered-      with at least 104            yellow powder, is                      1992-12-30
dose aerosol              inhalations. Dosed 2         soluble in water:                      Earliest US Market
suspension for            inhalations four times       nedocromil sodium                      Exclusivity: 2006-01-
inhalation containing     a day                                                               01
micronized nedocromil                                                                         Earliest Patent
sodium and sorbitan                                                                           Exclusivity: 2005-07-
trioleate, as well as                                                                         26
dichlorotetrafluoroetha
ne and
dichlorodifluoromethan
e as propellants. Each
Tilade canister
contains 210 mg
nedocromil sodium.
Each actuation meters
2.00 mg nedocromil
sodium from the valve
and delivers 1.75 mg
nedocromil sodium
from the mouthpiece.
Each 16.2 g canister
provides at least 104
metered actuations.
Mystic EHD nebulizer   -   Mystic™   ·USP 29                  Ventaira             -
                                     (Triamcinolone
                                     Acetonide) White to
                                     cream-colored,
                                     crystalline powder,
                                     having not more than a
                                     slight odor. Practically
                                     insoluble in water;
                                     sparingly soluble in
                                     dehydrated alcohol, in
                                     chloroform, and in
                                     methanol.:
                                     triamcinolone
                                     acetonide


-                      -   -         ·Tulobuterol occurs as Nipro Patch Co. Ltd.   -
                                     white crystals or
                                     crystalline powder. It is
                                     odorless. It is very
                                     soluble in methanol,
                                     freely soluble in
                                     ethanol (95), acetic
                                     acid (100), diethylether
                                     or isopropylether,
                                     sparingly soluble in
                                     hexane and practically
                                     insoluble in water. It
                                     has no optical rotation:
                                     tulobuterol
LTS Drug In          -       LTS Drug In   ·Tulobuterol occurs as LTS Lohmann          -
Adhesives technology         Adhesives     white crystals or
                                           crystalline powder. It is
                                           odorless. It is very
                                           soluble in methanol,
                                           freely soluble in
                                           ethanol (95), acetic
                                           acid (100), diethylether
                                           or isopropylether,
                                           sparingly soluble in
                                           hexane and practically
                                           insoluble in water. It
                                           has no optical rotation:
                                           tulobuterol



Captisol solubilizer     -   CAPTISOL®     -                    CyDex                  -
with undisclosed                                                Pharmaceuticals, Inc
corticosteroid

Mystic inhaler and       -   Mystic™       -                    Ventaira               -
formulation of long
acting broncho-dilator
and steroid
Mystic                   -   Mystic™       -                    Ventaira               -


Mystic                   -   Mystic™       -                    Ventaira               -
Inactive Ingredients:     400 (round) and 600      -              ·USP 29                  Otsuka                Year of US Approval:
cetostearyl alcohol,      mg (rectangular,                        (Theophylline) White, Pharmaceutical Co.,      1982-09-01
hydroxyethyl cellulose,   concave) white,                         odorless, crystalline    Ltd.
magnesium stearate,       opaque plastic                          powder, having a bitter
povidone and talc.        controlled release                      taste. Is stable in air.
                          tablets. Once daily                     Slightly soluble in
                          administration.                         water, but more
                                                                  soluble in hot water;
                                                                  freely soluble in
                                                                  solutions of alkali
                                                                  hydroxides and in
                                                                  ammonia; sparingly
                                                                  soluble in
                                                                  alcohol, in chloroform,
                                                                  and in ether.:
                                                                  theophylline




NanoCrystal               In Phase III, patients   NanoCrystal®   ·Budesonide is a white Elan Corporation Plc.   -
formulation for           are randomized to                       to off-white, odorless
nebulization              either 0.25mg UDB,                      powder that is
                          0.135mg UDB or                          practically insoluble in
                          placebo given twice a                   water and in heptane,
                          day over a 12-week                      sparingly soluble in
                          treatment period.                       ethanol, and freely
                          [30743]                                 soluble in chloroform.
                                                                  Its partition coefficient
                                                                  between octanol and
                                                                  water at pH 5 is 1.6 x
                                                                  10.3 : budesonide


-                         -                        -              -                      -                       -
Generic combination -     GyroHaler   ·This entery is used as Vectura Group Plc   -
formulation delivered                 a place holder in the
with Gyrohaler device.                database for NCE or
                                      undisclosed small
                                      molecules. It is
                                      required to be used in
                                      some cases (e.g.
                                      combination products)
                                      in order for charts and
                                      statistics to function
                                      properly.: undisclosed
                                      small molecule·This
                                      entery is used as a
                                      place holder in the
                                      database for NCE or
                                      undisclosed small
                                      molecules. It is
                                      required to be used in
                                      some cases (e.g.
                                      combination products)
                                      in order for charts and
                                      statistics to function
                                      properly.: undisclosed
                                      small molecule




VR632 is being        -   GyroHaler   -                      Vectura Group Plc    -
developed as a
generic combination
product using the
GyroHaler® DPI
Believed to be       -    GyroHaler   -                      Vectura Group Plc    -
GyroHaler device due
to local delivery
-   -   -   -   -                   -


-   -   -   -   -                   -




-   -   -   -   PowerVerde Systems, -
                Inc.
Collaboration to to     -   -   -   Vectura Group Plc   -
develop a dry powder
inhaler as a
Boehringer Ingelheim
branded device, to
deliver a range of
proprietary respiratory
products of Boehringer
Ingelheim, mainly for
the treatment of
asthma and chronic
obstructive pulmonary
disease.
Ventide Inhaler is a      Adults: 2 inhalations 3 -   ·USP 29 (Albuterol)      GlaxoSmithKline Plc   Year of EU Approval:
pressurised metered-      or 4 times daily.           White, crystalline                             1995
dose inhaler delivering   Children: 1-2               powder. Soluble in
100 micrograms            inhalations 2, 3 or 4       alcohol, sparingly
Salbutamol BP and 50      times daily.                soluble in water. Melts
micrograms                                            at about 156 oC. n-
Beclomethasone                                        Octanol/Water
Dipropionate BP per                                   Partition Coefficient is
actuation.                                            1.7 x 10 -3 at pH 7.
                                                      pKa=9.14. :
                                                      albuterol·(EP5.0) A
                                                      white or almost white,
                                                      crystalline powder,
                                                      practically insoluble in
                                                      water, freely soluble in
                                                      acetone, sparingly
                                                      soluble in alcohol.
                                                      It melts at about 210
                                                      °C, with
                                                      decomposition.:
                                                      beclomethasone
                                                      dipropionate
200 micrograms          One ventide rotacap   RotoHaler   ·USP 29 (Albuterol       GlaxoSmithKline Plc   Year of EU Approval:
microfine Salbutamol    containing 400                    Sulfate) White or                              1999
(as sulphate) and 100   micrograms                        practically white
micrograms microfine    salbutamol (as                    powder. Freely soluble
Beclomethasone          sulphate) and 200                 in water; slightly
Dipropionate per        micrograms                        soluble in alcohol, in
capsule or 400          beclomethasone                    chloroform, and in
micrograms microfine    dipropionate three or             ether. pKa=9.14.
Salbutamol (as          four times a day. The             Solubility: 24.5% w/v at
sulphate) and 200       maximum dose is one               pH 7.: albuterol
micrograms microfine    ventide rotacap four              sulfate·(EP5.0) A white
Beclomethasone          times a day.                      or almost white,
Dipropionate per                                          crystalline powder,
capsule. For use with                                     practically insoluble in
Rotohaler device                                          water, freely soluble in
                                                          acetone, sparingly
                                                          soluble in alcohol.
                                                          It melts at about 210
                                                          °C, with
                                                          decomposition.:
                                                          beclomethasone
                                                          dipropionate
Novolizer technology.   -   Novolizer®   ·USP 29 (Albuterol)      Almirall   Year of EU Approval:
100 mcg salbutamol                       White, crystalline                  1999
(120 mcg as sulfate)                     powder. Soluble in
and lactose                              alcohol, sparingly
monohydrate                              soluble in water. Melts
                                         at about 156 oC. n-
                                         Octanol/Water
                                         Partition Coefficient is
                                         1.7 x 10 -3 at pH 7.
                                         pKa=9.14. : albuterol
Ventodisks contain    Carton containing 14 Diskhaler   ·USP 29 (Albuterol       GlaxoSmithKline Plc   Year of EU Approval:
200mcg or 400 mcg     disks plus a diskhaler.          Sulfate) White or                              1998-12-03
salbutamol sulphate   200 micrograms or                practically white
with lactose BP For   400 micrograms may               powder. Freely soluble
use with Diskhaler    be administered as a             in water; slightly
device.               single dose.                     soluble in alcohol, in
                      The maximum dose is              chloroform, and in
                      400 micrograms four              ether. pKa=9.14.
                      times daily.                     Solubility: 24.5% w/v at
                                                       pH 7.: albuterol sulfate
Ventolin Accuhaler is a    Ventolin Accuhaler is a Diskus/AccuHaler   ·USP 29 (Albuterol       GlaxoSmithKline Plc   Year of EU Approval:
plastic inhaler device     plastic inhaler device                     Sulfate) White or                              1995-12-01
containing a foil strip    containing a foil strip                    practically white
with 60 regularly          with 60 regularly                          powder. Freely soluble
spaced blisters each       spaced blisters each                       in water; slightly
containing a mixture of    containing a mixture of                    soluble in alcohol, in
200 micrograms of          200 micrograms of                          chloroform, and in
microfine salbutamol       microfine salbutamol                       ether. pKa=9.14.
(as sulphate) and          (as sulphate) and                          Solubility: 24.5% w/v at
larger particle lactose.   larger particle lactose.                   pH 7.: albuterol sulfate
                           200 micrograms as a
                           single dose. Dose four
                           times daily.
Each actuation           Each canister provides -   ·USP 29 (Albuterol)      GlaxoSmithKline Plc   Year of US Approval:
contains 90 mcg          200 inhalations.           White, crystalline                             1981-05-01
microcrystalline         Dosed as two               powder. Soluble in
albuterol, oleic acid,   inhalations four times     alcohol, sparingly
and CFC propellants.     daily                      soluble in water. Melts
                                                    at about 156 oC. n-
                                                    Octanol/Water
                                                    Partition Coefficient is
                                                    1.7 x 10 -3 at pH 7.
                                                    pKa=9.14. : albuterol
CFC MDI, generic for      100 mcg per actuation, -   ·USP 29 (Albuterol)      Amphastar              Year of US Approval:
Ventolin CFC              90 mcg delivered.          White, crystalline       Pharmaceuticals Inc.   1996-08-14
                          Canister containing        powder. Soluble in
                          200 doses                  alcohol, sparingly
                                                     soluble in water. Melts
                                                     at about 156 oC. n-
                                                     Octanol/Water
                                                     Partition Coefficient is
                                                     1.7 x 10 -3 at pH 7.
                                                     pKa=9.14. : albuterol


Aqueous, colorless to     0.5% is supplied in    -   ·USP 29 (Albuterol       GlaxoSmithKline Plc    Year of US Approval:
light yellow solution,    amber glass bottles of     Sulfate) White or                               1987-01-16
pH 3.5, providing         20 mL. 2.5 mg of           practically white                               Year of EU Approval:
5mg/ml of albuterol       albuterol administered     powder. Freely soluble                          2000-07-06
sulphate. Inactive        three to four times        in water; slightly
ingredients:              daily.                     soluble in alcohol, in
benzyalkonium                                        chloroform, and in
chloride preservative,                               ether. pKa=9.14.
sulfuric acid to adjust                              Solubility: 24.5% w/v at
to pH 3.5., purified                                 pH 7.: albuterol sulfate
water
Dosed every 4-6 hours
via or continuously
nebulizer
Plastic ampoule          2.5mg to 5mg            -         ·USP 29 (Albuterol       GlaxoSmithKline Plc   Year of US Approval:
containing 2.5 ml of a   salbutamol should be              Sulfate) White or                              1992-04-23
sterile 0.1% or 0.2%     administered up to four           practically white                              Year of EU Approval:
w/v solution of          times a day.                      powder. Freely soluble                         2002-07-10
salbutamol (as                                             in water; slightly
Salbutamol Sulphate                                        soluble in alcohol, in
BP) in normal saline                                       chloroform, and in
and sulfuric acid to                                       ether. pKa=9.14.
adjust pH.                                                 Solubility: 24.5% w/v at
Dosed up to 4 times                                        pH 7.: albuterol sulfate
daily via nebulizer


200mcg microfine        Dosed up to four times RotoHaler   ·USP 29 (Albuterol       GlaxoSmithKline Plc   Year of US Approval:
salbutamol (as          daily.                             Sulfate) White or                              1988-05-04
sulphate) in each light                                    practically white
blue capsule, marked                                       powder. Freely soluble
Ventolin 200 or 400                                        in water; slightly
mcg microfine                                              soluble in alcohol, in
salbutamol (as                                             chloroform, and in
sulphate) in each light                                    ether. pKa=9.14.
blue capsule, marked                                       Solubility: 24.5% w/v at
Ventolin 200. Inactive                                     pH 7.: albuterol sulfate
ingredients: lactose
Delivered using
Rotohaler device.
Sodium citrate, Citric   150 mL or 2000 mL           -   ·USP 29 (Albuterol       GlaxoSmithKline Plc   Year of US Approval:
acid monohydrate,        amber glass bottle.             Sulfate) White or                              1987-06-10
Hydroxypropyl                                            practically white                              Year of EU Approval:
methylcellulose,         Adults                          powder. Freely soluble                         2005-10-14
Sodium benzoate,         The minimum starting            in water; slightly
Saccharin sodium,        dose is 2mg three               soluble in alcohol, in
Sodium chloride,         times a day given as            chloroform, and in
Orange flavour IFF       5ml syrup. The usual            ether. pKa=9.14.
17.42.8187, Purified     effective dose is 4mg           Solubility: 24.5% w/v at
water                    (10ml syrup) three or           pH 7.: albuterol sulfate
                         four times a day, which
                         may be increased to a
                         maximum of 8mg
                         (20ml syrup) three or
                         four times a day if
                         adequate
                         bronchodilatation is not
                         obtained.

                         Elderly
                         In elderly patients or in
                         those known to be
                         unusually sensitive to
                         beta-adrenergic
                         stimulant drugs, it is
                         advisable to initiate
                         treatment with the
                         minimum starting
                         dose.

                         Children
                         2 - 6 years: the
                         minimum starting dose
                         is 1mg as 2.5ml of
Each actuation          Dosed as two           -   ·USP 29 (Albuterol       GlaxoSmithKline Plc   Year of US Approval:
contains 120 mcg        inhalations repeated       Sulfate) White or                              2001-04-19
microcrystalline        every4-6 hrs.              practically white                              Earliest US Market
albuterol sulfate (90                              powder. Freely soluble                         Exclusivity: 2017-01-
mcg base) and HFA-                                 in water; slightly                             01
134a non CFC                                       soluble in alcohol, in                         Earliest Patent
propellant. Device is                              chloroform, and in                             Exclusivity: 2015-04-
available with dose                                ether. pKa=9.14.                               14
counter.                                           Solubility: 24.5% w/v at                       Year of EU Approval:
                                                   pH 7.: albuterol sulfate                       2007-08-14
It is an aqueous         0.0275 mg dosed once -       ·Fluticasone furoate is GlaxoSmithKline Plc   Year of US Approval:
suspension of            daily                        a white powder with a                         2007-04-27
micronized fluticasone                                molecular weight of                           Year of EU Approval:
furoate for topical                                   538.6, and the                                2008-01-15
administration to the                                 empirical
nasal mucosa by                                       formula is
means of a metering                                   C27H29F3O6S. It is
(50 microliters),                                     practically insoluble in
atomizing spray pump.                                 water.: fluticasone
After initial priming,                                furoate
each actuation delivers
27.5 mcg of
fluticasone furoate in a
volume of 50
microliters of nasal
spray suspension. It
also contains 0.015%
w/w benzalkonium
chloride, dextrose
anhydrous, edetate
disodium,
microcrystalline
cellulose and
carboxymethylcellulos
e sodium,
polysorbate 80, and
purified water.




Modified Pari e-flow   -                      eFlow   -                      Pari Pharma GmbH       -
-   -   Easi-Breathe   ·USP 29 (Albuterol)      IVAX Corp.   -
                       White, crystalline
                       powder. Soluble in
                       alcohol, sparingly
                       soluble in water. Melts
                       at about 156 oC. n-
                       Octanol/Water
                       Partition Coefficient is
                       1.7 x 10 -3 at pH 7.
                       pKa=9.14. : albuterol


-   -   -              ·USP 29 (Albuterol)      IVAX Corp.   -
                       White, crystalline
                       powder. Soluble in
                       alcohol, sparingly
                       soluble in water. Melts
                       at about 156 oC. n-
                       Octanol/Water
                       Partition Coefficient is
                       1.7 x 10 -3 at pH 7.
                       pKa=9.14. : albuterol
OROS technology.            Controlled Release    OROS Push-Stick   ·USP 29 (Albuterol       ALZA Corporation   Year of US Approval:
Each Volmax®                Tablets. Salbutamol   System            Sulfate) White or                           1992-12-23
Extended-Release            Sulphate BP 4.82mg                      practically white                           Year of EU Approval:
Tablet for oral             equivalent to                           powder. Freely soluble                      1994-08-01
administration contains     Salbutamol 4mg per                      in water; slightly
4 mg or 8 mg of             tablet. Salbutamol                      soluble in alcohol, in
albuterol as 4.8 mg or      Sulphate BP 9.64mg                      chloroform, and in
9.6 mg, respectively,       equivalent to                           ether. pKa=9.14.
of albuterol sulfate in a   Salbutamol 8mg per                      Solubility: 24.5% w/v at
nondeformable               tablet.                                 pH 7.: albuterol sulfate
cellulosic material that
serves as the rate-
controlling membrane.
Each tablet also
contains the inactive
ingredients cellulose
acetate,
croscarmellose
sodium, FD&C Blue
No. 1 (4 mg tablet
only), hydroxypropyl
cellulose (8 mg tablet
only), hydroxypropyl
methylcellulose,
magnesium stearate,
povidone, silica,
sodium chloride, and
titanium dioxide.




-                           -                     Xcelovair         ·White to yellow crystal Pfizer Inc.        -
                                                                    slightly soluble in
                                                                    water.: formoterol
A 150 mg vial contains    75 mg/vial and 150    -   ·A recombinant DNA- -             Year of US Approval:
202.5 mg of               mg/vial lyophilized       derived humanized                 2003-07-20
Omalizumab, 145.5         powder for SC             IgG1k monoclonal                  Year of EU Approval:
mg sucrose, 2.8 mg L-     administration.           antibody that                     2005-10-25
histidine hydrochloride   150 to 375 mg is          selectively binds to              Year of Japan
monohydrate, 1.8 mg       administered SC every     human                             Approval: 2009-01-21
L-histidine, and 0.5 mg   2 or 4 weeks.             immunoglobulin E
polysorbate 20, and is                              (IgE). The antibody
designed to deliver                                 has a molecular weight
150 mg of                                           of approximately 149
Omalizumab in 1.2 mL                                kilodaltons. :
after reconstitution                                omalizumab
with 1.4 mL SWFI,
USP.




-                         -                     -   ·A recombinant DNA- Tanox, Inc.   -
                                                    derived humanized
                                                    IgG1k monoclonal
                                                    antibody that
                                                    selectively binds to
                                                    human
                                                    immunoglobulin E
                                                    (IgE). The antibody
                                                    has a molecular weight
                                                    of approximately 149
                                                    kilodaltons. :
                                                    omalizumab
Levalbuterol tartrate is    Aerosol for adults and -   ·It is a white to light- 3M Health Care   Year of US Approval:
the generic name for        children 4 years of age    yellow solid, freely                      2005-03-11
(R)-albuterol tartrate in   and older is 2             soluble in water and                      Earliest US Market
the United States.          inhalations (90 mcg)       very slightly soluble in                  Exclusivity: 2008-03-
XOPENEX HFA                 repeated every 4 to 6      ethanol. : levalbuterol                   11
Inhalation Aerosol is a     hours; in some             tartrate                                  Earliest Patent
pressurized metered-        patients, 1 inhalation                                               Exclusivity: 2009-11-
dose aerosol inhaler        every 4 hours may be                                                 28
(MDI), which produces       sufficientXOPENEX
an aerosol for oral         HFA (levalbuterol
inhalation. It contains a   tartrate) Inhalation
suspension of               Aerosol is supplied as
micronized levalbuterol     a pressurized
tartrate, propellant        aluminum canister in a
HFA-134a (1,1,1,2-          box (NDC 63402-510-
tetrafluoroethane),         01). The canister is
Dehydrated Alcohol          labeled with a net
USP, and Oleic Acid         weight of 15 g and
NF.                         contains 200 metered
                            actuations (or
                            inhalations). Each
                            canister is supplied
                            with a blue plastic
                            actuator (or
                            mouthpiece), a red
                            mouthpiece cap, and
                                    s
                            patient’ instructions.
Generic Xopenex   -   -   ·Levosalbutamol, the DEY L.P.   -
                          R(-)-enantiomer of
                          salbutamol. It is a
                          white to off-white,
                          crystalline solid, with a
                          melting point of
                          approximately 187° C
                          and solubility of
                          approximately 180
                          mg/mL in water.
                          Levalbuterol is the (R)-
                          enantiomer of the drug
                          substance racemic
                          albuterol.

                          : levalbuterol
                          hydrochloride
Inactive Ingredients:    600 mg white to off      -   ·USP 29 (Zileuton)       -   Market Launch Date
crospovidone,            white, ovaloid, film-        White to off-white           US: 2005-10-01Year
hydroxypropyl            coated tablets. (300         powder.                      of US Approval: 1996-
cellulose,               mg dosage strength           It is a racemic mixture      12-09
hypromellose,            discontinued). The           (50:50) of R(+) and S(-      Earliest US Market
magnesium stearate,      recommended dosage           ) enantiomers. Zileuton      Exclusivity: 2010-01-
microcrystalline         is one 600-mg tablet         is a practically             01
cellulose,               four times a day for a       odorless, white,             Earliest Patent
pregelatinized starch,   total daily dose of 2400     crystalline powder that      Exclusivity: 2010-12-
propylene glycol,        mg.                          is soluble in methanol       10
sodium starch                                         and ethanol, slightly
glycolate, talc, and                                  soluble in acetonitrile,
titanium dioxide.                                     and practically
                                                      insoluble in water and
                                                      hexane.: zileuton
Each milimeter          25 mg/5mL                 -   ·An                        -   Year of US Approval:
contains, as inactive   concentrate for IV            immunosuppressive,             1997-12-10
ingredients, 3.6 mg     administration.               humanized IgG1                 Year of EU Approval:
sodium phosphate        The recommended               monoclonal antibody            1999-02-26
monobasic               dose for ZENAPAX is           produced by
monohydrate, 11 mg      1.0 mg/kg. Based on           recombinant DNA
sodium phosphate        the clinical trials, the      technology that binds
dibasic heptahydrate,   standard course of            specifically to the
4.6 mg sodium           ZENAPAX therapy is            alpha subunit (p55
chloride, 0.2 mg        five doses. The first         alpha, CD25, or Tac
polysorbate 80 and      dose should be given          subunit) of the human
may contain             no more than 24 hours         high-affinity interleukin-
hydrochloric acid or    before transplantation.       2 (IL-2) receptor.:
sodium hydroxide to     The four remaining            daclizumab
adjust the pH to 6.9.   doses should be given
                        at intervals of 14 days.
                        In the Phase 2 trial of
                        daclizumab in
                        combination with
                        Interferon-&#946; (the
                        CHOICE study) in
                        patients with active
                        relapsing multiple
                        sclerosis, the study
                        patients who received
                        daclizumab 2 mg/kg
                        subcutaneously every
                        two weeks showed a
                        statistically significant
                        72% reduction in the
                        number of new or
                        enlarged gadolinium-
                        enhancing lesions
                        (Gd+) at week 24,
-                       -                         -   -                          -   -
-   -                     -              ·: mequitazine          -                       -


-   -                     -              ·: mequitazine          -                       -


-   Patients enrolled in the CAPTISOL®   ·USP 29 (Zileuton)       CyDex                  -
    Phase I/II trial were                White to off-white       Pharmaceuticals, Inc
    randomized into four                 powder.
    escalating dose                      It is a racemic mixture
    groups (75 mg, 150                   (50:50) of R(+) and S(-
    mg, 300 mg, and 600                  ) enantiomers. Zileuton
    mg), each receiving                  is a practically
    one infusion of either               odorless, white,
    zileuton IV or placebo.              crystalline powder that
    [8208]                               is soluble in methanol
                                         and ethanol, slightly
                                         soluble in acetonitrile,
                                         and practically
                                         insoluble in water and
                                         hexane.: zileuton




-   -                     -              -                       -                       -

-   -                     PADD DPI       ·Mixture of Protein free Britannia              -
                                         synthetic surfactants    Pharmaceuticals
                                         dipalmitoylphosphatidyl
                                         choline(DPPC) and
                                         phosphatidylglycerol
                                         (PG) in the proportion
                                         7:3.: pumactant
ZYFLO CR (zileuton) Adults and children 12 Geomatrix   ·USP 29 (Zileuton)       SkyePharma Plc   Market Launch Date
extended-release          years of age and older:      White to off-white                        US: 2007-09-27Year
tablets                   The recommended              powder.                                   of US Approval: 2007-
for oral administration dose of ZYFLO CR is            It is a racemic mixture                   05-30
are triple-layer          two 600 mg extended-         (50:50) of R(+) and S(-
tablets                   release tablets twice        ) enantiomers. Zileuton
comprised of an           daily, within one hour       is a practically
immediate-release         after morning and            odorless, white,
layer, a middle           evening meals, for a         crystalline powder that
(barrier) layer, and a    total daily dose of 2400     is soluble in methanol
extended-release          mg.                          and ethanol, slightly
layer. ZYFLO CR                                        soluble in acetonitrile,
tablets are oblong, film-                              and practically
coated tablets with one                                insoluble in water and
red layer between two                                  hexane.: zileuton
white layers, debossed
                   C .
on one side with “ T2”
Each tablet contains
600 mg of zileuton and
the following inactive
ingredients:
crospovidone, ferric
oxide, glyceryl
behenate,
hydroxypropyl
cellulose,
hypromellose,
magnesium stearate,
mannitol,
microcrystalline
cellulose, povidone,
pregelatinized starch,
propylene glycol,
sodium starch
-   -   -   -   Discovery Laboratories -
                Inc.




-   -   -   -   -                      -

-   -   -   -   -                      -




-   -   -   -   -                      -




-   -   -   -   -                      -
rEV131 is smaller than     In the Phase II post-  -   -                         -   -
therapeutic anti-          cataract eye
histamine receptor         inflammation trial,
antibodies and its         rEV131, dosed twice a
compact structure          day, will be compared
gives good                 with prednisolone,
bioavailablity by a        dosed four times a day
number of routes           over a two week period
including: injected,       [12378].
inhaled,
intraperitoneal, topical
(ocular and nasal).
The molecule is
thermo-stable and can
be stored in solution
for more than 18
months at room
temperature without
significant loss of
activity.

-                          -                      -   ·: alpha-1 antitrypsin,   -   -
                                                      recombinant human
-   -   -   -   -   -




-   -   -   -   -   -
OrganTransplantation
Antiinflammatory/Immune
MultipleSclerosis
Bronchitis
CerebralPalsy
RheumatoidArthritis
PulmonaryHypertension
RheumatoidArthritis
RheumatoidArthritis
COPD
matory/Immune
Hypertension

				
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