Ballicules › Drugs › Topotecan
Pronunciation: toe-poe-TEE-kan (hye-KAM-tin)
Mechanism of action: Topotecan ballicule
Visual mnemonic: Topotecan mascot“High-Top toucan” Causes single-strand DNA breaks
What it is Topoisomerase I inhibitor; relapsed small-cell lung, ovarian, and cervical cancers.
Why this one Oral and IV formulations provide salvage options after preferred platinum-based regimens fail.
What limits it Severe neutropenia, thrombocytopenia, and anemia require counts; renal impairment raises exposure, and oral use adds diarrhea.
Molecular structure: Topotecan
FDA-approved for
ovarian cancer (1996) small cell lung cancer (1998)
Classes and tags
Clinical profile
Therapeutic safety burden 3 / 4
Overdose danger 2 / 4
Weight-gain liability 0 / 4
Sedation liability 0 / 4
QT / Torsades 0 / 4
Direct muscarinic antagonism 0 / 4
Embryofetal risk 3 / 4
Legacy pregnancy category D
Defining liability Myelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
FDA label
Read the full label on DailyMed ↗
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.
Available strengths
cap 0.25, 1 mginj 1 mg/mL
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
Cost Topotecan (HYCAMTIN)
Strength #/mo generic $/unit CostPlus 0.25 mg cap per unit not offered 1 mg cap per unit not offered 1 mg/mL inj per unit not offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Topotecan is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.
Generic entry 2010
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Memory aids: interaction avatars
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Self-check Which topoisomerase does topotecan inhibit? Topoisomerase I.What organ impairment raises topotecan exposure? Renal impairment.