Updated: 4/23/2019

Antitumor Antibiotics

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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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