Entrectinib: A New Selective Tyrosine Kinase Inhibitor Approved for the Treatment of Pediatric and Adult Patients with NTRK Fusion-positive, Recurrent or Advanced Solid Tumors

Osman H. M., Tuncbilek M.

CURRENT MEDICINAL CHEMISTRY, vol.29, no.15, pp.2602-2616, 2022 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Review
  • Volume: 29 Issue: 15
  • Publication Date: 2022
  • Doi Number: 10.2174/0929867328666210914121324
  • Journal Name: CURRENT MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, CAB Abstracts, Chemical Abstracts Core, EMBASE, MEDLINE
  • Page Numbers: pp.2602-2616
  • Keywords: Entrectinib, indazol benzamide, Trk ABC, ALK, ROS1 inhibitor, NTRK fusion-positive tumors, ALK INHIBITOR, TRK INHIBITOR, PAN-TRK, ACQUIRED-RESISTANCE, INTEGRATED ANALYSIS, ANTITUMOR-ACTIVITY, POTENT INHIBITOR, OPEN-LABEL, ROS1, CANCER
  • Ankara University Affiliated: Yes

Abstract

Background: Entrectinib is a highly potent ATP-competitive and selective inhibitor of tyrosine kinases - Trk A B C, ALK, and ROS1. It was developed by Roche and initially approved in Japan in 2019 to treat pediatric and adult patients with NTRK fusion-positive, recurrent, or advanced solid tumors. In August 2019, entrectinib received accelerated approval by the U.S FDA for this indication. It is also the first FDA-approved drug designed to target both NTRK and ROS1.