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Updated: Apr 23 2019

Antitumor Antibiotics

  • Dactinomycin (Actinomycin D)
    • Mechanism
      • intercalate between strands of DNA
    • Clinical use
      • Wilms' tumor
      • Ewing's sarcoma
      • rhabdomyosarcoma
      • childhood tumors
    • Toxicity
      • myelosuppression
  • Doxorubicin (Adriamycin) and Daunorubicin
    • Mechanism
      • intercalate between strands of DNA
        • noncovalent
        • breaks DNA → decreased replication
      • free radical generation
      • inhibit topoisomerase
    • Clinical use
      • Hodgkin's lymphomas
        • part of the ABVD combination regimen
          • Adriamycin
          • Bleomycin
          • Vinblastine
          • Dacarbazine
      • solid tumors
        • breast, endometrial, ovary, and lung
      • myelomas
      • sarcomas
    • Toxicity
      • cardiotoxicity
        • dilated cardiomyopathy
        • dexrazoxane used to prevent cardiotoxicity
          • iron chelating agent
          • prevents formation of free radicals
            • does not "trap" free radicals
      • myelosuppression
      • alopecia
      • tissue damage if extravasates into extravascular space
  • Bleomycin
    • Mechanism
      • free radical generation
        • complexes with Fe and O2
        • breaks DNA → decreased replication
      • G2-phase specific
    • Clinical use
      • Hodgkin's lymphoma
        • part of ABVD regimen for Hodgkin's
      • testicular cancer
      • head and neck cancer
      • skin cancer
    • Toxicity
      • pulmonary fibrosis
      • pneumonitis
      • skin changes
      • myelosuppression is relatively insignificant
  • Etoposide (VP-16) and Teniposide
    • Mechanism
      • inhibits DNA topoisomerase II (think eTWOposide)
        • breaks DNA → decreased replication
      • late S- to G2-phase specific
    • Clinical use
      • small cell carcinoma
        • lung
        • prostate
      • testicular carcinoma
    • Toxicity
      • myelosuppression
      • GI upset
      • alopecia
  • Irinotecan and Topotecan
    • Mechanism
      • inhibits DNA topoisomerase I (think 1rinotecan)
        • prevents DNA replication by inhibiting DNA unwinding
    • Clinical use
      • colon, ovarian, and small cell lung cancer
    • Toxicity
      • myelosuppression
      • diarrhea
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