Rozlytrek

Rozlytrek is the brand name for entrectinib, an oral multi-target tyrosine kinase inhibitor developed by Roche/Genentech. It targets several kinases implicated in cancer, most notably the tropomyosin receptor kinase (TRK) receptors TRKA, TRKB, and TRKC (encoded by NTRK1-3), as well as ROS1 and ALK. By inhibiting these fusion kinases, entrectinib aims to block oncogenic signaling and slow or halt tumor growth. The drug is designed to cross the blood–brain barrier, providing potential activity against central nervous system involvement in fusion-positive cancers.

Entrectinib was developed for tumors driven by gene fusions, and its mechanism supports tumor-agnostic use in specific molecular contexts. In clinical practice, it has demonstrated activity in solid tumors harboring NTRK gene fusions and in ROS1 fusion–positive non-small cell lung cancer, with ongoing evaluation in broader settings and in pediatric populations. Its CNS activity has been a notable feature in trials involving brain metastases or primary CNS tumors.

Regulatory status and indications have included approvals for adult and pediatric patients with NTRK gene fusion–positive solid tumors that are metastatic or where surgical resection is not feasible, as well as for ROS1 gene fusion–positive metastatic NSCLC. The safety profile generally includes common adverse effects such as fatigue, dizziness, dysgeusia (taste disturbance), constipation, edema, and liver enzyme elevations; more serious events can occur and require monitoring, including potential hepatotoxicity and other laboratory abnormalities. As with all targeted therapies, treatment decisions depend on tumor genetics and individual patient factors.