Antineoplastic drugs

  1. MTX: MOA
    Folic acid analog inhibits dihydrofolate reductase, decreasing dTMP
  2. MTX: how to rescue patient from myelosuppression
    Leucovorin (folinic acid)
  3. 5-FU: MOA
    • Pyrimidine analog covalently complexes folic acid
    • Inhibits thymidylate synthase and decreases dTMP
  4. 5-FU: overdose rescue
  5. 6-MP: MOA
    • Purine analog decreases purine synthesis
    • Activated by HGPRTase
  6. 6-thioguanine (6-TG): MOA
    Purine analog like 6-MP but can be given with allopurinol
  7. Cytarabine (ara-C): MOA
    Pyrimidine antagonist inhibits DNA polymerase
  8. Dactinomycin: MOA
    Intercalates in DNA to inhibit DNA dependent RNA polymerase
  9. Dactinomycin: use
    Kids' tumors e.g. Ewing's, Wilms', Rhabdo
  10. Doxorubicin (Adriamycin): MOA
    • Generates free radicals
    • Nocovalently intercalates in DNA and puts breaks in it
  11. Doxorubicin: Toxicity
    • Cardio
    • Alopecia
  12. Bleomycin: MOA
    • G2 phase induction of free radicals, causing DNA strand breaks
    • Combines with Fe2+
  13. Bleomycin: toxicity
    • Pulmonary fibrosis
    • sin changes
    • Uniquely, causes little myelosuppression
  14. Etoposide: MOA
    • Inhibits DNA topoisomerase II-DNA complex
    • Causes dsDNA breaks during replication
  15. Cyclophosphamide and ifosfamide: MOA
    Activated in P-450 system (liver) then covalently X-link DNA at guanine N-7
  16. Cyclophosphamide and ifosfamide: toxicity
    • Hemorrhagic cystitis, minimized with MESNA
    • Neurotox with ifosfamide
  17. Nitrosureas (-mustine and streptozocin): MOA
    Require bioactivation, then alkylate DNA
  18. Nitrosureas (-mustine): use
    CNS tumors
  19. Busulfan: MOA
    Cross-links DNA
  20. Busulfan: use
  21. Busulfan: toxicity
    • pulmonary fibrosis
    • hyperpigmentation
  22. Name the alkylating agents
    • Cyclophosphamide
    • -mustines (nitrosureas)
    • streptozocin
    • cisplatin
    • busulfan
    • dacarbazine/procarbazine
    • mechlorethamine
  23. Paclitaxel: MOA
    Bind beta-tubulin subunit of microtubules to prevent their disassembly
  24. Vincristine, vinblastine: MOA
    Bind tubulin to prevent microtubule assembly
  25. Vinblastine: toxicity
    bone marrow suppression
  26. Vincristine: toxicity
    neurotoxicity, paralytic ileus
  27. Cisplatin: toxicity
    • Nephrotoxicity
    • Ototoxicity
  28. Hydroxyurea: MOA
    • Urea analogue inhibits ribonucleotide reductase
    • S phase specific
  29. Name the selective estrogen receptor modulators
    • Tamoxifen
    • Raloxifene
  30. Which SERM increases the risk of endometrial carcinoma?
  31. Trastuzumab (herceptin): MOA
    • Monoclonal antibody against HER-2 (erb-B2)
    • Encourages antibody-dependent cytotoxicity
  32. Trastuzumab: toxicity
  33. Imatinib: MOA
    Tyrosine kinase inhibitor for bcr-abl
Card Set
Antineoplastic drugs
from FA 2010, cancer drugs