Larotrectinib
Active Pharmaceutical Ingredients 2025-03-03
English Synonyms LOXO-101 (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
Catalog ID99712
CAS NO.1223403-58-4
Purity 98%
MDL NumberMFCD28902192
EINEC Molecular FormulaC21H22F2N6O2
Molecular Weight 428.435
| Category | Content |
|---|---|
| Generic Name | Larotrectinib |
| Brand Name | Vitrakvi |
| Drug Class | TRK (Tropomyosin Receptor Kinase) Inhibitor |
| Mechanism of Action | Larotrectinib is a highly selective inhibitor of TRK kinases (TRKA, TRKB, TRKC), which are activated by NTRK gene fusions. It blocks the activity of these kinases, leading to tumor cell death. |
| Indications | – Approved for adult and pediatric patients with solid tumors harboring NTRK gene fusions without a known acquired resistance mutation.<br>- Indicated for metastatic or locally advanced tumors where surgical resection would result in severe morbidity. |
| Dosage Forms | Capsules, oral solution |
| Administration | – Adults: 100 mg orally twice daily.<br>- Pediatric patients: 100 mg/m² orally twice daily (maximum of 100 mg per dose). |
| Pharmacokinetics | – High oral bioavailability.<br>- Elimination: Primarily hepatic metabolism.<br>- Half-life: Approximately 10 hours. |
| Side Effects | – Common: Fatigue, nausea, dizziness, vomiting, increased AST and ALT.<br>- Serious: Hepatotoxicity, increased intracranial pressure. |
| Precautions | – Monitor liver function tests regularly.<br>- Use with caution in patients with hepatic impairment. |
| Storage | Store at room temperature, protect from moisture. |
| Developer | Loxo Oncology Inc. and Bayer Pharmaceuticals |
| Approval Date | FDA approval on November 26, 2018. |
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