Anticancer Drugs

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Anticancer Drugs
2011-09-09 12:50:04
IMR pharmacology

Anticancer Drugs
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  1. Vincristine, vinblastine
    Target the mitotic spindle by inhibiting microtubule formation

    Side effects include pripheral neuropathy
  2. Paclitaxel
    taxane from the Pacific yew that enhances microtubule formation by preventing the depolymerization of microtubules to tubulin
  3. Nitrogen Mustard (Mechlorethamine)
    Alkylates DNA leading to cross-linking of DNA and breakage

    Used to treat Hodgkin's lymphoma due to its ability to cause lympocytopenia
  4. Cyclophosphamide
    • -C in CMF
    • -used to treat breast cancer, lymphomas and leukemia
    • -prodrug that is activated by P450 into inactive metabolites and toxic active metabolites includine phosphoramide mustard (alkylating agent that causes DNA to cross-link) and acrolein (causes cystitis)
    • -decreases WBC and platelets
  5. Cisplatin
    • -Alkylating agent that contains platinum (will effect different tissues than cyclophosphamide) and cross-links neighboring molecules
  6. Carboplatin
    • -More compelx DNA alkylating/cross-linking agent than cisplatin
    • -used to treat lung and ovarian cancer
  7. Doxorubicin (Adriamycin)
    • -topoisomerase inhibitor used to treat breast cancer
    • -side effects include cardiotoxicity and women are more sensitive than men
  8. Irinotecan
    -topoisomerase inhibitor used to treat colorectal cancer in the FOLFIRI combination (5-FU + leucovorin + irinotecan)
  9. Methotrexate
    • -Anti-metabolite, prevents methyl groups from being donated to purine synthesis
    • -derivative of folic acid that binds dihydrofolate (FH2) and prevents the regeneration of CH2THF by preventing dihydrofolate reductase (DHFR) from adding a methyl group (because it has an aromatic ring)
  10. 5-Fluoro-Uracil
    • -anti-metabolite
    • -binds thymidylate synthetase and prevents the addition of an activated methyl group necessary for the conversion of U in RNA to T in DNA
  11. Capecitabine
    • -anti-metabolite = prevents the addition of a methyl croup required for purine synthesis
    • - prodrug that is orally active
  12. Trastuzumab
    • -mAb that targets GF receptor HER2 = anti-HER2
    • -HER-2+ breast cancers have a poor prognosis but adjuvant treatment with trastuzumab restores outcome to that of HER-2 negative cancers
    • -cardiac side effects - cardiomyocytes contain HER2
  13. Cetuximab
    • -mAb that targets Epidermal GF Receptor-1 (EGF-R) = anti-EGF-R
    • -Colorectal cancer: only works in wild-type KRAS cancers
    • -Cutaneous and GI side effects: diarrhea, skin rash
  14. Rituximab
    • -anti-CD20 (cell surface Ag on B cells)
    • -used to treat B cell leukemia
  15. Bevacizumab
    • -anti-VEGF
    • -binds VEGF so it is unavailable to signal angiogenesis = tumor cell death
    • -Colon cancer pts gained only 4 months of overall survival and all eventually died
    • -Alternate use: macular degeneration and diabetic retinopathy = restores vision
  16. Gefitinib, Erlotinib
    • -small molecule EGFR inhibitors
    • -associated with skin toxicity (rashes) - similar to cetuximab (KRAS) - used to dose
    • -T790M mutation confers gefitinib resistance
  17. Imatinib
    • -trade name is Gleevac
    • -ABL inhibitor
    • -Used to treat CML (BCR-ABL fusion and Philadelphia chromosome)
    • -Resistance happens quickly
  18. Sorafenib, Sunitinib
    • -VEGF-R, PDGF-R, kit inhibitors
    • -Not very selective = many side effects
  19. Bortezomib
    • -reversible proteasome inhibitor that causes cancer cell apoptosis
    • -targets machinery present in all cells = side effects similar to borad cytotoxicity drugs (GI, sensorineural, neutropenia)
    • -Used to treat multiple myeloma
  20. Lapatinib
    • -Selective inhibitor of Her-2
    • -10x less active at an EGFR than at Her-2, no other KIs are this selective
  21. Azathioprine
    • Immunosuppressant
    • -originally an anti-cancer drug (not very effective)
    • -prodrug and purine analogue = interrupts purine synthesis and you can’t produce DNA
  22. Cyclosporine, tacrolimus
    • immunosuppressant
    • binds calcineurin
    • inhibits T cell activation
  23. Sirolimus (rapamycin)
    • binds mTOR (mammalian target of rapamycin)
    • inhibits T cell activation
  24. Basiliximab,daclizmab
    • mAbs that target CD25 = IL-2R
    • IL-2 is third signal in T cell activation