OncoMatch/Clinical Trials/Entrectinib

Entrectinib (Rozlytrek) Clinical Trials

Entrectinib (Rozlytrek, RXDX-101) is an oral, CNS-penetrant tyrosine kinase inhibitor that targets ROS1 and TRK fusions (TRKA/B/C, encoded by NTRK1/2/3). It received FDA approval in August 2019 for ROS1-positive metastatic NSCLC and for NTRK fusion-positive solid tumors regardless of cancer type, the second NTRK-targeting agent to receive tumor-agnostic approval after larotrectinib. In the pooled STARTRK analyses, entrectinib produced objective response rates of approximately 67% in ROS1-positive NSCLC and 57% across NTRK fusion-positive solid tumors, with demonstrated intracranial activity in patients with CNS metastases. The active trial landscape now includes next-generation ROS1 inhibitors such as repotrectinib (FDA-approved November 2023) for patients who progress on entrectinib or crizotinib, and ongoing NTRK fusion basket trials enrolling adults and children across solid tumor types. Eligibility requires a confirmed ROS1 fusion (NSCLC indication) or NTRK1/2/3 gene fusion (tumor-agnostic indication) by an approved assay.