Topotecan
Vue déterministe de l'entité source de la LJAM. L'autorité clinique demeure avec les ID de la source cités et l'état d'approbation de l ́examinateur.
| ID | DRUG-TOPOTECAN |
|---|---|
| Type | Médicament |
| Alias | 9-dimethylaminomethyl-10-hydroxy-camptothecinHycamtineSKF-104864Топотекан |
| État | reviewed 2026-04-27 | pending_clinical_signoff |
| Maladies | DIS-OVARIAN DIS-SCLC |
| Sources | SRC-ESMO-OVARIAN-2024 SRC-NCCN-OVARIAN-2025 |
Faits sur les drogues
| Catégorie | Inhibiteur de la topoisomérase I (camptothécine semisynthétique) |
|---|---|
| Mécanisme | 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 typique | 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. |
| Ukraine enregistrée | Vrai |
| NSZU remboursé | Vrai |
| Ukraine vérifiée pour la dernière fois | 2026-04-27 |
Avertissements
- Suppression sévère de la moelle osseuse (en boîte) — surveillance fréquente de la CBC requise; peut mettre la vie en danger; ne devrait être administrée que par des cliniciens ayant subi une chimiothérapie cytotoxique
Notes
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.
Utilisé par
Protocole thérapeutique
REG-TOPOTECAN-OVARIAN- Topotecan mono-agent (ovar récurrent résistant à la platine)REG-TOPOTECAN-SCLC-RR- Topotecan (SCLC récidive/ réfractaire)