What it isTopoisomerase I inhibitor; relapsed small-cell lung, ovarian, and cervical cancers.
Why this oneOral and IV formulations provide salvage options after preferred platinum-based regimens fail.
What limits itSevere neutropenia, thrombocytopenia, and anemia require counts; renal impairment raises exposure, and oral use adds diarrhea.
FDA-approved for
- ovarian cancer (1996)
- small cell lung cancer (1998)
FDA label
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BOXED WARNING Severe myelosuppression; administer first cycle only if baseline ANC >=1,500/mm3 and platelets >=100,000/mm3; monitor blood counts.
| FDA dosing | Population | Start | Target | Max |
| Relapsed small cell lung cancer (oral) | Adult | 2.3 mg/m2/day PO x5 days per 21-day cycle | | |
Renal Reduce dose if CrCl <50 mL/min
Hepatic Undefined
5 consecutive days per 21-day cycle
Instructions
- Swallow capsules whole; do not chew, crush, or divide.
- Round dose to nearest 0.25 mg.
- If a dose is missed or vomiting occurs, do not take an extra dose.
- Do not start subsequent cycles until ANC >1,000, platelets >100,000, Hgb >=9 g/dL.
Cautions
- Myelosuppression incl. fatal typhlitis (neutropenic enterocolitis)
- Severe diarrhea
- Interstitial lung disease (can be fatal)
- Embryo-fetal toxicity
Adverse reactions
- Neutropenia
- Anemia
- Thrombocytopenia
- Nausea
- Diarrhea
- Vomiting
- Alopecia
- Fatigue
- Anorexia
Pregnancy Can cause fetal harm (animal embryolethality, fetotoxicity, teratogenicity)
Lactation Do not breastfeed during and for 1 week after the last dose
⚠ BOXED WARNING
- Severe myelosuppression; start only with adequate baseline neutrophils and platelets and monitor blood counts
Cost, est. cash$50–$10,000/month or cycle
Generic entry2010
Classes and tags
Clinical profile
Therapeutic safety burden3 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk3 / 4
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Topotecan ballicule
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Memory aids: mascots and interaction avatars
“High-Top toucan”
Causes single-strand DNA breaks
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