Topotecan

HYCAMTIN

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Pronunciation: toe-poe-TEE-kan (hye-KAM-tin)

Topotecan ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Topotecan ballicule

Topotecan HYCAMTIN mascot mnemonic cartoon — Visual mnemonic: Topotecan mascot
**“High-Top toucan”**
Causes single-strand DNA breaks

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.

Topotecan molecular structure (skeletal formula) — Molecular structure: Topotecan

FDA-approved for

ovarian cancer (1996)
small cell lung cancer (1998)

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 mg
inj 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	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 entry2010

⚠ BOXED WARNING

Severe myelosuppression; start only with adequate baseline neutrophils and platelets and monitor blood counts

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.

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Memory aids: interaction avatars

BCRP substrate

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