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PFIZER INC.

These results are supplied for informational purposes only.

Prescribing decisions should be made based on the approved package insert.

For publications based on this study, see associated bibliography.





PROPRIETARY DRUG NAME/INN: Zithromax®/Azithromycin



THERAPEUTIC AREA AND FDA APPROVED INDICATIONS: See USPI



PROTOCOL NO.: A0661102



PROTOCOL TITLE: A Multicenter, Randomized, Double-Blind, Double-Dummy

Comparative Trial of Azithromycin SR Versus Levofloxacin for the Treatment of Acute

Exacerbation of Chronic Bronchitis (AECB)



Study Center(s): Study included 84 centers in Brazil (5), Canada (8), Costa Rica (1), Germany

(8), India (6), Lithuania (3), Mexico (1), Netherlands (2), Russian Federation (7), Spain (5),

United Kingdom (4), Venezuela (2), and the United States (32). Sixty-three of these centers

enrolled subjects (including screening failures).



Study Initiation and Completion Dates: 10 January 2003 to 31 March 2004



Phase of Development: Phase 3

01000005338675 \ 1.5 \ Approved \ 25-Oct-2005 09:41









Study Objective(s):

Primary objective: To confirm the hypothesis that a single, 2.0 g dose of azithromycin SR is

clinically non-inferior to 7 days of levofloxacin 500 mg/day (two 250 mg capsules once daily),

when used to treat adults with AECB



Secondary objectives: To assess safety and the bacteriologic efficacy of both treatment regimens



METHODS



Study Design:



This was a randomized, double-blind, double-dummy, active-controlled, multicenter,

international study in which subjects with AECB were assigned to receive oral therapy with

azithromycin SR (a single 2.0 g dose) or levofloxacin (500 mg once daily for 7 days). Enrolled

subjects were stratified into 2 groups based on systemic steroid use at the time of randomization.

Clinical and bacteriologic responses were assessed at the Test of Cure (TOC) visit (14-21 days

post first dose) and Long Term Follow Up (LTFU) visit (28-35 days post first dose). All

subjects who received at least 1 dose of study medication were assessed for safety. All Baseline

pathogens were tested for susceptibility to azithromycin and levofloxacin according to NCCLS

procedures.

CLINICAL STUDY SYNOPSIS



Number of Patients (planned and analyzed):



A total of 530 subjects (265 per treatment arm) were planned for enrollment; 551 subjects were

randomized in the study, and 542 subjects received treatment (268 azithromycin SR, 274

levofloxacin).



Diagnosis and Main Criteria for Inclusion:



Eligible subjects were men or women ≥50 years of age, with a current or past history of smoking

of at least 20 pack-years, a diagnosis of chronic bronchitis (defined as chronic cough and sputum

production on most days for 3 consecutive months for >2 consecutive years), and clinical

evidence of AECB, as demonstrated by the production of purulent sputum (defined by the

presence of >25 polymorphonuclear leukocytes per low power field) and all of the following

signs and symptoms: increased sputum production, increased dyspnea, and increased sputum

purulence. Pack years were calculated by multiplying the average number of cigarette packs

smoked per day times the number of years smoked (eg, 2 packs per day times 15 years equals

30 pack years).



Study Treatment:



Azithromycin SR and matching placebo were supplied as white/off-white powder for oral

suspension in a 100-mL bottle. Azithromycin SR was administered orally as a single 2.0 g dose

01000005338675 \ 1.5 \ Approved \ 25-Oct-2005 09:41









slurry, to be taken at least 1 hour before or 2 hours after a meal. Levofloxacin 250 mg and

matching placebo were supplied as black/blue (gray in Eastern Europe), opaque, hard gelatin

Size #0 capsules in a 60 mL bottle. Each bottle contained 14 capsules.



The study regimens were administered in a double-blind, double-dummy fashion. Subjects

assigned to receive azithromycin SR received their single dose of active azithromycin SR and

2 capsules of levofloxacin placebo on Day 1, and then continued with QD dosing of levofloxacin

placebo for the next 6 days. Subjects assigned to receive levofloxacin received azithromycin SR

placebo and 2 capsules of active levofloxacin on Day 1, and then continued with QD dosing of

active levofloxacin for the next 6 days. The first dose of each study medication was given in an

observed setting such that subjects took the single dose of azithromycin SR/placebo slurry then,

30 minutes later, 2 capsules of levofloxacin/placebo.



Efficacy Evaluations:



The primary efficacy parameter was the sponsor assessment of Clinical Response (clinical cure

rate) in the Clinical Per Protocol population at the TOC visit. The secondary efficacy parameter

was bacteriologic response (eradication rate) at the TOC visit. Additional secondary efficacy

parameters included: Investigator assessment of clinical response at the TOC visit, sponsor

assessment of clinical response by Baseline pathogen at the TOC visit, and clinical and

bacteriologic responses at LTFU. Susceptibilities of Baseline pathogens were also summarized.









Protocol A0661102 / Page 2 of 12

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CLINICAL STUDY SYNOPSIS



Safety Evaluations:



Adverse events (AEs) were assessed for all treated subjects. Clinical laboratory tests

(hematology and blood chemistry) and vital signs were collected at Baseline and the End of

Treatment (EOT) visit. Physical examinations were done at Baseline and as deemed necessary

by the investigator at subsequent visits.



Statistical Methods:

Efficacy: The primary efficacy analysis compared clinical cure rates (based on sponsor-assessed

clinical response) of the azithromycin SR and levofloxacin regimens at the TOC visit

(Day 14-21) in the Clinical Per Protocol population. A 95% confidence interval (CI) for the

difference in cure rates was constructed based on normal approximation to the binomial

distribution with stratification for systemic steroid use. There was no adjustment for centers.

Azithromycin SR was considered non-inferior to levofloxacin if the lower limit of the 95% CI

for the difference in cure rates (azithromycin SR minus levofloxacin) was greater than -10%.



The CI for the difference in overall bacteriologic eradication rates was constructed using the

normal approximation to the binomial distribution and accounted for steroid use stratification.

Success for bacteriologic endpoints was based on combining the categories of eradication and

presumed eradication. For all other secondary efficacy endpoints, frequency tables for each

response were provided.

01000005338675 \ 1.5 \ Approved \ 25-Oct-2005 09:41









Clinical Per Protocol Subjects were All Treated Subjects who had a diagnosis of chronic

bronchitis and clinical evidence of AECB, a negative chest radiograph for pneumonia, and who

received: at least 6 days of dosing of study medication (including both active and placebo doses),

no concomitant systemic antibiotic with activity against key AECB pathogens, and an

assessment in the appropriate visit window. Bacteriologic Per Protocol Subjects were Clinical

Per Protocol Subjects with a Baseline bacterial pathogen identified by culture.









Protocol A0661102 / Page 3 of 12

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CLINICAL STUDY SYNOPSIS



RESULTS







Table S1 Subject Disposition and Demography:

Evaluation Group, N (%) of Subjectsa Azithromycin SR Levofloxacin

Screened 621

All Randomized 551

All Treated 268 274

Completed Study 249 (92.9) 251 (91.6)

Discontinued from Study 19 (7.1) 23 (8.4)

Evaluated for Primary Efficacyb 220 (82.1) 218 (79.6)

Analyzed for Safety:

Adverse Events 268 (100.0) 274 (100.0)

Laboratory Datac 258 (96.3) 260 (94.9)

a

Percentages are based on the All Treated Subjects.

b

Clinical Per Protocol Population at the TOC visit.

c

Number of treated subjects with at least one laboratory observation during the study.





Treatment groups were generally similar with respect to Baseline characteristics. An overview

of subject disposition and demography is shown in Table S1. Approximately 69% of all treated

subjects were men. The majority of subjects were white (60%), with a mean age of 62 years for

01000005338675 \ 1.5 \ Approved \ 25-Oct-2005 09:41









both treatment groups. Systemic steroid use was similar (10%) in each group. In addition,

duration (in years) of the subjects’ underlying disease (chronic bronchitis), mean duration of

current exacerbation, and Baseline signs and symptoms were similar between treatment groups.

Treatment groups were similar with respect to the number and type of pathogens isolated at

Baseline, with M. catarrhalis and S. pneumoniae being the most common isolates. The number

of discontinuations was similar between the azithromycin SR treatment group (7.1%) and the

levofloxacin treatment group (8.4%). Reasons for discontinuation are listed in Table S2.









Protocol A0661102 / Page 4 of 12

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CLINICAL STUDY SYNOPSIS



Table S2 Discontinuations From Study (All Treated Subjects)

Number (%) of Subjects Azithromycin SR Levofloxacin

N = 268 N = 274

Subject Died 0 (0.0) 2 (0.7)

Discontinuations

Related to Study Druga 7 (2.6) 7 (2.6)

Adverse Eventb 1 (0.4) 2 (0.7)

Lack of efficacy 6 (2.2) 5 (1.8)

Not Related to Study Druga 12 (4.5) 14 (5.1)

Adverse Eventb 2 (0.7) 7 (2.6)

Other 2 (0.7) 1 (0.4)

Subject Defaultedc 8 (3.0) 6 (2.2)

Total 19 (7.1) 23 (8.4)

a

Relationship to Study Drug is derived as Related if reason for discontinuation is Insufficient Clinical

Response (Lack of Efficacy), or due to a treatment-related adverse event; otherwise, Relationship is

derived as Not Related.

b

Includes only subjects who discontinued due to an adverse event (AE) according to their completed

subject summary CRF.

c

Includes subjects who discontinued due to the following reasons: Lost to Follow-Up or Subject No

Longer Willing to Participate in Study.





Baseline susceptibility: The majority of isolates were susceptible to both azithromycin and

levofloxacin, as shown below in Table S3.

01000005338675 \ 1.5 \ Approved \ 25-Oct-2005 09:41









Table S3 Susceptibility of Specific Baseline Pathogens, Number of Pathogens

(All Randomized Subjects Without Regard to Treatment Group)

Susceptibilitya to Azithromycin Susceptibilitya to Levofloxacin

Baseline Pathogens Total S I R Not Total S I R Not

Testedb Testedb

H. influenzae 46 46 0 0 0 46 46 0 0 0

M. catarrhalis 57 0 0 0 57 57 0 0 0 57

S. aureus 32 20 0 12 0 32 27 4 1 0

S. pneumoniae 56 45 0 11 0 56 55 0 1 0

H. parainfluenzae 28 27 0 0 1 28 28 0 0 0

S = Susceptible, I = Intermediate, R = Resistant; susceptibility based upon current breakpoints per organism

for azithromycin and levofloxacin, Pathogens: Haemophilus influenzae (H. influenzae), Moraxella

catarrhalis (M. catarrhalis), Staphylococcus aureus (S. aureus), Streptococcus pneumoniae

(S. pneumoniae), and Haemophilus parainfluenzae (H. parainfluenzae).

a

Susceptibility results based on MIC and/or disk diffusion testing; disk result used only if MIC result

missing.

b

Not tested includes pathogens for which no NCCLS breakpoint criteria have been established.





Efficacy Results:



Primary Efficacy Results:



Subjects in the Clinical Per Protocol population treated with azithromycin SR had a clinical cure

rate at TOC of 93.6% compared with 92.7% for subjects treated with levofloxacin. The 95% CI

around the difference in cure rates at TOC was -3.4% to 5.5%. The lower limit of this CI was

greater than -10%, indicating that azithromycin SR therapy was non-inferior to levofloxacin



Protocol A0661102 / Page 5 of 12

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CLINICAL STUDY SYNOPSIS



therapy in the treatment of AECB. Of those subjects who were assessed as clinical cure at TOC,

over 98% of the subjects in both treatment groups remained a clinical cure at the LTFU visit. A

summary of clinical response is shown in the Table S4.





Table S4 Summary of Clinical Response (Clinical Per Protocol Subjects)

Number (%) of Subjects

Azithromycin SR Levofloxacin 95% CIa

Subjects at TOC 220 218

Cure 206 (93.6) 202 (92.7) -3.4, 5.5

Failure 14 (6.4) 16 (7.3)

Subjects at LTFU 197 193

Cure 194 (98.5) 190 (98.4)

Relapse 3 (1.5) 3 (1.6)

Clinical response is sponsor assessed.

TOC=Test of Cure; LTFU=Long Term Follow-Up.

a

95% confidence interval for the treatment difference in cure rates; note that a lower limit > -10%

indicates non-inferiority.



In general, there were no remarkable differences between treatment groups in clinical cure rates

by gender, age, race, or steroid-use in the Clinical Per Protocol population.



Secondary Efficacy Results:

01000005338675 \ 1.5 \ Approved \ 25-Oct-2005 09:41









Cure rates based upon the investigators’ assessment of clinical response for subjects in the

Clinical Per Protocol population at the TOC visit (shown in Table S5) were very similar to those

based upon the sponsor assessment of clinical response (shown in Table S6).









Protocol A0661102 / Page 6 of 12

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CLINICAL STUDY SYNOPSIS



Table S5 Investigator Assessment of Clinical Response at TOC (Clinical Per Protocol

Subjects)

Investigator Assessment of Response, Azithromycin SR Levofloxacin

n (%) N = 220 N = 218

Cure 207 (94.1) 201 (92.2)

Failure 11 (5.0) 14 (6.4)

Signs/Symptoms persisted/worsened 9 (4.1) 11 (5.0)

New signs/symptoms 0 ─ 2 (0.9)



Developed pneumonia 2 (0.9) 1 (0.5)



Not Done 0 ─ 0 ─

Missing 2 (0.9) 3 (1.4)

TOC = Test of Cure.







Table S6 Sponsor Assessment of Clinical Response (Clinical Per Protocol Subjects),

Number (%) of Subjects

Azithromycin SR Levofloxacin Difference 95% CIa

Subjects at EOT 215 215

Cure 209 (97.2) 207 (96.3) — —

Failure 6 (2.8) 8 (3.7)

Subjects at TOC 220 218

01000005338675 \ 1.5 \ Approved \ 25-Oct-2005 09:41









Cure 206 (93.6) 202 (92.7) 1.0 -3.4, 5.5

Failure 14 (6.4) 16 (7.3)

Subjects at LTFUb 197 193

Cure 194 (98.5) 190 (98.4) — —

Relapse 3 (1.5) 3 (1.6)

a

95% confidence interval for the difference in cure rates between treatment groups; a lower limit of > -10%

indicates non-inferiority.

b

LTFU includes subjects who are cured at TOC and have LTFU assessments.

EOT=End of Treatment; TOC=Test of Cure; LTFU=Long Term Follow-Up.





Clinical cure rates for all treated subjects are shown below in Table S8.









Protocol A0661102 / Page 7 of 12

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CLINICAL STUDY SYNOPSIS



Table S7 Clinical Cure Rates at TOC by Baseline Characteristics: All Treated Subjects

Number Cured / Number of Subjects (%)

Characteristics Azithromycin SR Levofloxacin Total

N = 268 N = 274 N = 542

Gender

Male 162 / 177 (91.5) 174 / 196 (88.8) 336 / 373 (90.1)

Female 82 / 91 (90.1) 68 / 78 (87.2) 150 / 169 (88.8)

Age (years)

90%) in azithromycin SR-treated subjects who had documented

infection with S. pneumoniae, H. influenzae, or M. catarrhalis at Baseline. Treatment-related

adverse events occurred more frequently in azithromycin SR-treated subjects (24%) as compared

with levofloxacin-treated subjects (15%). Most events were mild or moderate digestive system

events. Single-dose treatment with azithromycin SR is safe and effective in the treatment of

AECB in adults.

01000005338675 \ 1.5 \ Approved \ 25-Oct-2005 09:41









Based on a report completed on: 23 July 2004









Protocol A0661102 / Page 12 of 12

PhrmaWebSynopsis-Final- 10/25/05



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