Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors

Abstract

Dazhi Liu,1 Michael Offin,2 Stephen Harnicar,1 Bob T Li,2 Alexander Drilon2 1Department of Pharmacy, Memorial Sloan Kettering Cancer Center, New York, NY, USA; 2Thoracic Oncology Service, Division of Solid Tumor Oncology, Department of Medicine, Memorial Sloan Kettering Cancer Center, Weill Cornell Medical College, New York, NY, USA Abstract: Entrectinib is a potent small-molecule tyrosine kinase inhibitor that targets oncogenic rearrangements in NTRK, ROS1, and ALK. The consolidated results of 2 Phase I trials demonstrated activity in tyrosine kinase inhibitor-naïve patients along with substantial intracranial activity. In ROS1-rearranged lung cancers, entrectinib results in durable disease control and prolonged progression-free survival. The drug is well tolerated and has a safety profile that includes adverse events mediated by on-target tropomyosin-related kinase A/B/C inhibition. Keywords: entrectinib, lung cancer, NSCLC, TRK, ALK, ROS1

Keywords

• entrectinib
• lung cancer
• TRK
• ALK
• ROS1