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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors
entrectinib
L01EX14
Forms & Strengths
- Capsules: 100mg
- Capsules: 200mg
Adult Dosing
- 600mg orally once daily
- Dose reduction for adverse reactions: 400mg or 200mg orally once daily
- Dose increase for inadequate response: 800mg orally once daily, if tolerated
Pediatric Dosing
- For pediatric patients 12 years and older with body surface area of at least 1.51m^2: 600mg orally once daily
- For pediatric patients 12 years and older with body surface area less than 1.51m^2: 500mg orally once daily
- Dose reduction for adverse reactions: 400mg or 200mg orally once daily
Indications
- Treatment of adult and pediatric patients 12 years and older with solid tumors that have a Neurotrophic Receptor Tyrosine Kinase (NTRK) gene fusion
- Treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are ROS1-positive
Mechanism of Action
- Inhibits the activity of the TRK kinase and the ROS1 kinase
- Blocks the signaling of the TRK and ROS1 pathways, leading to decreased tumor cell growth and survival
Contraindications
- Hypersensitivity to entrectinib or any of its components
- None other specified in clinical labeling
Adverse Reactions
- Most common: fatigue, dizziness, dysgeusia, constipation, diarrhea, nausea, vomiting, edema, cognitive impairment, weight gain, pyrexia
- Serious: neutropenia, anemia, thrombocytopenia, increased AST, increased ALT, increased creatinine, cognitive impairment, mood disturbances
Drug Interactions
- Avoid coadministration with strong CYP3A4 inhibitors
- Avoid coadministration with strong CYP3A4 inducers
- Monitor for increased entrectinib exposure with CYP3A4 inhibitors or decreased exposure with CYP3A4 inducers
Curated Content: Needs Vetting Before Put to Clinical Use