Entrectinib
Active Pharmaceutical Ingredients 2025-03-03
English Synonyms RXDX101 NMS-E628 N-[5-[(3,5-Difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]benzamide
Catalog ID100841
CAS NO.1108743-60-7
Purity 95%
MDL NumberMFCD28129099
EINEC Molecular FormulaC31H34F2N6O2
Molecular Weight 560.646”
| Category | Content |
|---|---|
| Generic Name | Entrectinib |
| Brand Name | Rozlytrek |
| Drug Class | Tyrosine Kinase Inhibitor |
| Mechanism of Action | Entrectinib is a selective inhibitor of TRKA, TRKB, TRKC (encoded by NTRK1, NTRK2, NTRK3), ROS1, and ALK. It acts as an ATP competitor to block these kinases, suppressing cancer cell proliferation and promoting apoptosis. |
| Indications | – Treatment of ROS1-positive metastatic non-small cell lung cancer (NSCLC) in adults.<br>- Treatment of NTRK gene fusion-positive solid tumors in adults and children aged 1 month and older.<br>- Effective against primary and metastatic central nervous system (CNS) diseases. |
| Dosage Forms | Capsules, oral suspension, or oral pellets. |
| Administration | – Adults: 600 mg orally once daily.<br>- Children (12 years and older): 300 mg/m² orally once daily.<br>- Can be taken with or without food. |
| Pharmacokinetics | – Tmax: 4-5 hours.<br>- Half-life: 20 hours (parent drug), 40 hours (active metabolite M5).<br>- Crosses the blood-brain barrier. |
| Side Effects | – Common: Fatigue, nausea, constipation, increased liver enzymes.<br>- Serious: Severe liver toxicity, seizures. |
| Developer | Roche |
| Approval Date | Approved by the FDA in August 2019. |
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