entrectinib

Overview

Entrectinib (RXDX-101) is an orally available, CNS-penetrant inhibitor of TRKA/B/C (encoded by NTRK1/2/3), ROS1, and ALK kinases. It is FDA-approved in a tumor-agnostic indication for solid tumors harboring NTRK gene fusions and for ROS1-positive non-small cell lung cancer.

Evidence in the corpus

  • FDA-recognized level 1 (OncoKB) biomarker: NTRK1 fusions (e.g., LMNA::NTRK1) predict response to entrectinib across solid tumor types including gallbladder carcinoma; 1 patient in the MSK GBC cohort (n=233) harbored an actionable NTRK1 fusion PMID:36228155
  • NTRK fusion-positive CCA (~0.2% overall, up to 3.6% iCCA): pooled analysis of 121 NTRK-positive patients ORR 61.2%, mPFS 13.8 mo, mOS 33.8 mo across tumor types; NTRKs reported in ~0.2% of CCA PMID:25526346
  • TRK/ROS1/ALK inhibitor; ETV6-NTRK3 fusion identified by MSK-IMPACT in 2 tumors reclassified from acinic cell carcinoma to MASC; both patients enrolled on TRK inhibitor basket study with major/near-complete responses PMID:27442865

Resistance mechanisms

Cancer types (linked)

  • GBC — tumor-agnostic indication applies; NTRK1 fusions identified in gallbladder carcinoma

Sources

This page was processed by crosslinker on 2026-05-14. - PMID:25526346

This page was processed by crosslinker on 2026-05-14. - PMID:27442865

This page was processed by wiki-cli on 2026-05-14.