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antineoplasia drugs2 xls downstate

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					     Class                Drug name                            Mechanism                         Target cancer                Adverse affects                                Misc.
                                                                                                   Widely used
                                                                                                                         Bladder related problems
                       Cyclophosphamide              Cross-links DNA, "breaking" DNA            (lymphomas, BCs,                                                        Activated in liver
Alkylating agents                                                                                                      (hemorrhagic cystitis, cancer)
                                                                                                   and others)
                            Mephalin                             See above                      Multiple myeloma                     --                                         --
                                                                                                Germ-line cancers
                                                                                                                        Nephrotoxicity, ototoxicity,
   Platinum                                        Similar to aklyating agents, but form             (ovarian,                                                Other drugs in class are carboplatin,
                            Cisplatin                                                                               neurotoxicity, metallic taste, emesis,
  compounds                                                 platinum cross-links                 testicular), lung,                                                        oxalipatin
                                                                                                                             myelosuppression
                                                                                                       colon


                                                    Inhibits THF, thus preventing the
                                                                                                ALL, Burkitt's and      Mucositis, myelosuppression,         Give leucovorin to bypass THF step if
                         Methotrexate            production of thymine and purines. S-
                                                                                                      others            nephrotoxicity, neurotoxicity                treatment is too toxic
                                                            phase dependent


                                                    Inhibits multiple targets of folate
                                                                                                Mesothelioma, lung
                          Pemetrexed               metabolism. As with MTX, S-phase                                       Probably same as above?               Give folate & B12 if overly toxic
                                                                                                     cancer
                                                              dependent
                                                                                                 Colorectal cancer,
                       5'fluorouracil / 5-        Inhibitis thymidine synthesis and DNA
                                                                                                   as well as BC,     Diarrhea and hand-foot syndrome             Leucovorin = synergistic
                             fdUMP                                 repair
                                                                                                gastric, esophageal
                          Capecitabine                    Oral pro-drug of fdUMP                                                                             Same as above
                                                                                                                         Nausea, diarrhea, stomatitis,
Antimetabolites                                     Incorporated into DNA as cytosine
                           Cytarabine                                                             AML, ALL, NHL          chemical conjunctivitis, and                           --
                                                   analogue, causing chain termination
                                                                                                                              cerebellar ataxia
                      Purine analogues (6-
                                                Inhibit purine synthesis, incorporated into                              Myelosuppression, mucositis,
                       meraptopurine, 6-                                                         Acute leukemias                                                       Require activation
                                                  DNA/RNA, causing chain termination                                  hepatotoxicity, immunosuppression
                          thioguanine)
                                                   Purine antagonist. Phosphorylated into
                                                   active form, where it inhibits DNA pol,                                Myelosuppression,
                                                                                                                                                              Give antibiotics due to compromised
                          Fludarabine                    prim, lig, and others. Only            Indolent NHL, CLL immunosuppression of T cells, watch
                                                                                                                                                                        immune system
                                                  antimetabolite that is apoptotic and                              out for opportunistic infections
                                                       cytotoxic outside of S phase
                                                  Incorporated into DNA, inducing strand
                           Cladribine                                                           Hairy cell leukemia                   --                                        --
                                                       breaks and NAD/ATP depletion
                                                 Urea analogue. Inhibits DNA synthesis via
                                                                                                 CML, P vera, ET,
                          Hydroxyurea              ribonucleotide reductase. Works in S                                               --                                        --
                                                                                                       RT
                                                                    phase.
                       Vinca alkaloids (eg         Prevents polymerization of tubulin and          NHL, Kaposi's
                     vincitrine, vinblastine,   formation of mitotic spindles, arresting cell   sarcoma, BC, lung               Neurotoxicity                                   --
                           vinorelbine)                         in metaphase                     cancer, Hodgkins
Mitotic inhibitors
                                                     Stabilizes mitotic spindles, prevent        BC, lung cancer,         Hypersensitivity reaction to
                     Taxane (eg paclitaxel,
                                                    Depolymerization. Exerts effects in M       prostate, bladder,     solubilizing agent (cremophore),                         --
                          docetaxel)
                                                                    phase.                            ovarian          myelosuppression, neurotoxicity
                     Anthracycline (a bunch        Forms tripartite complex with topo II,
                     of drugs with "rubi" in     preventing re-ligation and leaving broken      AML, BC (curative)              Cardiotoxicity                                  --
                          their name)                               strands
                          Camptothecins                                                           Colon, lung,
                                                              Inhibits Topo I                                            Diarrhea, myelosuppression
 Topoisomerase       (irinotecan, topotecan)                                                     ovarian, gastric
  related drugs
                                                                                           Germ-line cancers,
                      Epipodophyllotoxins
                                                Stabilizes Topo II binding, preventing DNA Hodgkins and NHL,
                          (etoposide,                                                                                      acute myeloid carcinoma                              --
                                                        release. Causes G2 arrest.           small AND non-
                          tenoposide)
                                                                                            small lung cancer
                                                  Has two binding sites. The first binds to
                                                 iron, while the second binds to DNA. The
                                                                                            Testicular cancer, Pulmonary toxicity (occurs commonly
                           Bleomycin                close proximity of the metal to DNA
                                                                                            Hodgkins Diseaes                smokers)
 Miscellaneous                                    induces oxidative stress and free radical
     drugs                                                        formation
                                                   Hydrolyzes asparagine to aspartic acid
                                                                                            Pediatric and adult
                          Asparginase           and ammonia (tumor cells lack asparagine                                         --                                             --
                                                                                                    ALL
                                                                synthetase)
                                         Surge in LH and FSH, followed by
                                                                               Prostate cancer, as
                                       inhibition of gonadotropin (feedback).
               GnRH antagonists                                                 well as metastatic                Well, castration…               Used in neoadjuvant therapy
                                       Reduces production of testosterone in
                                                                                  breast cancer
                                     testes (medical castration for 3-4 weeks)
                                     Inhibit binding and nuclear translocation
             AR blockers (flutamide, of AR's. Added benefit increased levels of
                                                                                                         Vasomotor flushing, gynecomastia,      Additional toxicities observed in
                   nilutamide,           testosterone due to interruption of               PA
                                                                                                         mastodynia, possible loss of libido       flutamide and nilutamide
                 bicalumatide)         negative feedback, attenuating loss of
                                                       libido
                                                                                                           Hot flashes, increased chances of
                                       Selective estrogen receptor modulator.                                                                    Prevents osteoperosis in post-
                                                                                                                 endometrial cancer,
                   Tamoxifen          Block estrogen stimulation of BC (similar            BC                                                    menopausal women, decreases
                                                                                                         thromboembolic phenomena, retinal
                                                   to AR blockers).                                                                             cholesterol (and potentially CVD)
                                                                                                                   tox and cataracts
Hormonal
                                      Inhibits final step of estrogen synthesis.
 therapy
                                      Can only be used to inhibit production in
                                      post-menopausal women who rely ONLY                                Osteoporosis as well as arthralgias
              Aromatase inhibitors                                                         BC                                                    No risk of endometrial cancer
                                         only adipose aromatase (will cause                                       and myalgias
                                       increase in pre-meno due to feedback
                                                         loop)

                                                                              Advanced breast
             Medroxyprogesterone     Widespread hormonal suppression as well
                                                                             cancer, metastatic Appetite stimulation and weight gain              Used for anorexia-caachexia
                and megstrol                  as direct tumor killing
                                                                             endometrial cancer

                                      Somatostatin analogue (inhibits a whole
                                       bunch of metabolic processes). Treats
                   Octreotride                                                            --                              --                                   --
                                      symptoms (carcinoid and non-infectious
                                                      diarrhea)
                                       Anti-CD20 expressed on intermediate        Lymphoma and
                                      stage B cells (pre-B cells), so it doesn't  CLL, synergistic
                   Rituximab                                                                                      Infusion reactions                           --
                                       affect stem cell population or existing       with other
                                                  naïve population)                   therapies
                                        Anti-CD52 which presents on normal
                                                                                 CLL and low-grade
                 Alemtuzumab         neutrophils and lymphocytes as well as B-                                            --                     Not used much due to toxicity
                                                                                     lymphoma
                                                and T-cell lymphomas
                                                                                                         Infusion reactions, left ventricular
                  Trastuzumab         HER2/Neu or ErbB-2 antibody. Prevents        BC (metastatic and    ejection fraction deficiency (see
                                                                                                                                                          In CBL case
                   (herceptin)        tyrosine kinase signaling from receptor.     early) that's her2+         CBL case) especially with
                                                                                                                    anthracyclines
                                                                                Squamous cell
                                                                              cancer of head and
             Anti-EGFR (cetuximab    Similar to herceptin. Prevent downstream   neck, advanced              Acneform rash (surrogate for
Monoclonal                                                                                                                                                     --
              and panitumumab)                        signaling                colorectal cancer,         response), dermotological toxicity
antibodies
                                                                                advanced lung
                                                                                     cnacer
                                                                                        Metastatic        Promoted mutation of even more
                                         Binds to angiogenic growth factor,
                   Anti-VEGF                                                         colorectal, lung         prolific forms of cancer,
                                        preventing vascular recruitment and                                                                                    --
             (bevacizumab/avastin)                                                   (non-small cell)      hypertension, proteinuria, heart
                                                    metastasis
                                                                                           and BC                        failure
                                                                                        Relapsed /
                                     Attach radioactive "payload" (e.g. yttrium-
                    Radio-                                                              refractory       Radiaiton-related myelosuppression,
                                     90 or iodine-131) to antibody, specifically                                                                               --
               immunoconjugates                                                       follicular, low-             hypothyroidism
                                          target tumor cells with radiation
                                                                                    grade lymphoma
                                        Anti-CD33, conjugated to cytotoxic
                                      antibiotic. Antibody is endocytosed, and                           Bone marrow suppression, hepatic
                 Gemtuzumab                                                     CD33 positive AML                                                              --
                                     antibiotic is released, destroying DNA and                           toxicity, veno-occlusive disease
                                                     killing the cell
                                                                                      CML,
                                                                                 gastrointestinal
                                     Competively inhibits the BCR-ABL tyrosine                            Neutropenia, thrombocytopenia,
               Imatinib (Gleevac)                                                 stromal tumor                                                                --
                                              kinase at ATP binding site                                  edema in ankles, fluid retention
                                                                                 (KIT+), CMML,
                                                                                       HES
                                                                                         Used in small cell
                                                                                                                                                       Best response in non-smoking, female
                      Erlotinib, gefitinib            HER1/EGFR TK inhibits.              lung cancer and           Rash, diarrhea, pneumonitis
                                                                                                                                                             Asians. 100% bioavailable
                                                                                         pancreatric cancer
Tyrosine kinase
   inhibitors                                                                            Her2/neu+ BC that
                          Lapatanib                 Inhibits TK activity of HER2          don't respond to                        --                                    --
                                                                                             herceptin

                                                                                          Both used to treat
                                                                                         renal cancers. Sora
                     Sorafenib, sunitinib              Multikinase inhibitors            is also indicated for      Both have fairly typically AE's                     --
                                                                                           liver cancer, and
                                                                                             Suni for GIST
                                                                                          Multiple myeloma
                                                Immunomodulatory -- potentially
                         Thalidomide,                                                            and             Sedation, constipation, neuropathy,
                                             decreases production of VEGF and IL-6,                                                                                     --
                         lenalidomide                                                      myelodysplastic               thromboembolism
                                              decreases circulating endothelial cells
                                                                                             syndrome
                                              Down-regulates NF-kB, which promotes
                                                 cell survival. Disrupts ubiquitin-                               Thrombocytopenia, neutropenia,
                       Anti-proteosome                                                    Multiple myelome                                                              --
                                                proteosome regulation, leading to                                            fatigue
                                                   apoptosis (p53 mediated?)
                                                                                                Acute        Dry skin, cheilitis, hyperlipidemia,
                                             Binds to RAR. This receptor is responsible
                                                                                            promyelocytic     retinoic acid syndrom (dyspnea,
                        Tretoin (ATRA)         for inhibition of differentation, and by                                                                                Oral
                                                                                         leukemia (curative weight gain, hypotension, pulmonary
                                             binding, ATRA allows cells to differentiate
                                                                                         with anthracycline)              infiltrates)

 Differentiating
                                                Arsenic trioxide promotes free radical
     agents                                                                               Multiple myeloma
                                               production. It induces maturation and
                                                                                                 and               Hyperglycemia, hypokalemia,
                                              promotes apoptosis , has antiangiogenic
                       Arsenic trioxide                                                    myelodysplastic       pulmonary distress, prolonged QT                       --
                                             effects, up-regulating p53 and other gene
                                                                                          syndrome, acute             interval, arrhythmias
                                              products, including caspases, associated
                                                                                             leukemias
                                                            with apoptosis.



                                          5-aza-cytidine and 2'-deoxy-5-azacytidine
                                               can also increase transcription of
                                          genes "silenced" during the pathogenesis
                    DNA methyltransferase                                                  Myeldysplastic
      Uh…                                  of a tumor by causing demethylation of                                                 --                                    --
                         inhibitors                                                         syndrome
                                              the methylated cytosines that are
                                          acquired as an "epigenetic" (i.e., after the
                                           DNA is replicated) modification of DNA.



   Neoplasia /        5-HT3 antagonists        Inhibit chemotherapy induced nausea
treatment related
    therapies           NK1 receptor
                                                          Same as above
                         antagonist

				
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posted:7/27/2011
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