Rozlytrek
Solid tumors with NTRK gene fusion — adult and pediatric (≥12 years) with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation, that are metastatic or where surgical resection is likely to result in severe morbidity, and who have no satisfactory alternative treatments or whose cancer has progressed following treatment; ROS1-positive metastatic NSCLC.
Adults: 600 mg orally once daily
Pediatric (BSA >1.50 m²): 600 mg once daily
Pediatric (BSA 1.11-1.50 m²): 400 mg once daily
Pediatric (BSA 0.91-1.10 m²): 300 mg once daily
Take with or without food. Swallow whole.
Capsules: 100 mg, 200 mg
None listed.
- Heart Failure: CHF in 3.4% (Grade 3-4: 1.7%). Monitor LVEF at baseline and during treatment.
- CNS Effects: Cognitive impairment (24%), dizziness (28%), ataxia (15%), mood disorders (7%). Occurs due to brain penetration.
- Skeletal Fractures: In 8% of adults (without trauma or fall). Monitor bone health.
- Hepatotoxicity: Grade 3-4 ALT in 5%. Monitor LFTs monthly.
- Hyperuricemia: In 13%. Monitor uric acid.
- QT Prolongation: Monitor ECGs.
- Vision Disorders: In 24%.
Fatigue (48%), constipation (39%), dysgeusia (33%), edema (32%), dizziness (28%), diarrhea (27%), nausea (27%), cognitive impairment (24%), vision disorders (24%), weight gain (21%), increased creatinine (20%), elevated AST (18%), myalgia (18%), cough (17%), vomiting (17%)
Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.
Entrectinib is an inhibitor of tropomyosin receptor kinases (TRKA/TRKB/TRKC, encoded by NTRK1/2/3), ROS1, and ALK. NTRK gene fusions create chimeric oncoproteins with constitutive kinase activity that drive tumor proliferation across multiple tumor types. Entrectinib was specifically designed with CNS penetrance to treat brain metastases, which are common in ROS1+ NSCLC and NTRK fusion cancers.
Tmax: 4-6 hours. Half-life: approximately 20 hours. Protein binding: >99%. Brain-to-plasma ratio: 0.4-0.6 (effective CNS penetration). Metabolized by CYP3A4. Steady-state by Day 7-8. Excreted in feces (83%) and urine (3%).
Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.
- STARTRK-2 / ALKA — Entrectinib in NTRK fusion-positive solid tumors and ROS1+ NSCLC. Phase I/II basket.