II. Indications

  1. FDA Approved (often combined with other agents)
    1. Ovarian Cancer
    2. Cervical Cancer
  2. Off-Label
    1. Acute Myelogenous Leukemia (AML)
    2. CNS Malignancy (including CNS Lymphoma)
    3. Ewing Sarcoma
    4. Neuroblastoma
    5. Ovarian Cancer (metastatic)
    6. Rhabdomyosarcoma

III. Mechanism

  1. See Mitotic Inhibitor Chemotherapy
  2. Irinotecan is a semisynthetic derivative of camptothecin with antineoplastic activity
    1. Camptothecin extracted from the Asian tree Camptotheca acuminata ("Happy Tree")
    2. Camptothecin is a cytotoxic quinoline-based alkaloid
  3. Topotecan is active without metabolism
    1. Contrast with Irinotecan, a similar drug, but that requires metabolism to SN-38 for activity
    2. Topotecan is considered less potent than SN-38, the active metabolite of Irinotecan
  4. Topotecan is a Topoisomerase Inhibitor
    1. Binds to topoisomerase 1, inhibiting DNA ligation
    2. DNA breaks accumulate
    3. Inhibits DNA Replication and transcription
    4. Arrests cell cycle in S phase
    5. Results in cell apoptosis and death

IV. Medications

  1. Oral Capsules: 0.25 mg and 1 mg
  2. Powder for IV Injection Solution: 4 mg

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Adverse Effects

  1. Myelosuppression (Bone Marrow suppression)
    1. Neutropenia
  2. Bleeding (may be severe)
  3. Interstitial Lung Disease

VII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception (including one month after Chemotherapy completed)
  3. Monitoring
    1. Complete Blood Count

IX. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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