Topotecan
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| ID | DRUG-TOPOTECAN |
|---|---|
| Tipo | Fármaco |
| Alegais | 9-dimethylaminomethyl-10-hydroxy-camptothecinHicamtinaSKF-104864Топотекан |
| Estado | reviewed 2026-04-27 | pending_clinical_signoff |
| Doenças | DIS-OVARIAN DIS-SCLC |
| Fontes | SRC-ESMO-OVARIAN-2024 SRC-NCCN-OVARIAN-2025 |
Fatos sobre as drogas
| Classe | Inibidor da topoisomerase I (camptotecina semissintética) |
|---|---|
| Mecanismo | Semisynthetic water-soluble camptothecin analog that binds and stabilizes the covalent topoisomerase I–DNA cleavable complex, preventing religation of the single-strand DNA nick generated by the enzyme. When a replication fork encounters the trapped complex, the single-strand break is converted to a lethal double-strand break → S-phase-specific apoptosis. Crosses the blood-brain barrier modestly. Active in platinum-resistant ovarian cancer, sensitive-relapse small-cell lung cancer (SCLC; the only cytotoxic approved post-platinum monotherapy), recurrent cervical cancer (in combination with cisplatin), and rare hematologic malignancies. |
| Dose típica | IV classical (most common): 1.5 mg/m²/day IV over 30 minutes for 5 consecutive days every 21 days. Weekly schedule: 4 mg/m² IV over 30 minutes on Days 1, 8, 15 every 28 days (better tolerated in pre-treated / older patients). Oral: 2.3 mg/m²/day for 5 consecutive days every 21 days (lower neutropenia, more diarrhea). Cervical (combo cisplatin): topotecan 0.75 mg/m²/day Days 1-3 + cisplatin 50 mg/m² Day 1 every 21 days. Renal adjustment: CrCl 20-39 → 50% dose reduction; CrCl <20 not recommended. Hepatic adjustment usually not required (predominantly renal clearance). Hold for ANC <1.5, plt <100; G-CSF support indicated for recurrent febrile neutropenia. |
| Ucrânia registada | Verdade |
| NSZU reembolsado | Verdade |
| Ucrânia verificada pela última vez | 2026-04-27 |
Avisos
- Supressão grave da medula óssea (encaixada) — monitorização frequente da CBC; pode pôr a vida em risco; deve ser administrada apenas por clínicos com quimioterapia citotóxica
Notas
Renal dose adjustment is mandatory and frequently overlooked — CrCl 20-39 requires 50% dose reduction; CrCl <20 not recommended. Weekly schedule (4 mg/m² Days 1, 8, 15) is better tolerated than the 5-day continuous schedule in older / pretreated patients — cross-trial efficacy comparable in ovarian salvage. Oral formulation has more diarrhea, less neutropenia; convenient for outpatient use but logistics of oral cytotoxic handling apply (PPE for caregivers, avoid pregnancy / breastfeeding contact). Vesicant on extravasation — administer through central or large peripheral vein; have extravasation kit available. G-CSF support after first febrile neutropenia event. Baseline + serial CBC weekly. Premedicate with 5-HT3 antagonist + dexamethasone for nausea. UA: generic, available, НСЗУ-reimbursed for indicated uses.
Usado por
Esquema terapêutico
REG-TOPOTECAN-OVARIAN- Topotecan single-agent (platinum-resistant recurrent ovarian)REG-TOPOTECAN-SCLC-RR- Topotecan (SCLC relapsed/refractory)