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

Authors Liu D, Offin M, Harnicar S, Li BT, Drilon A

Received 9 April 2018

Accepted for publication 11 May 2018

Published 20 July 2018 Volume 2018:14 Pages 1247—1252

DOI https://doi.org/10.2147/TCRM.S147381

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Andrew Yee

Peer reviewer comments 3

Editor who approved publication: Professor Garry Walsh


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


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