Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations

Drilon, Alexander; Ignatius Ou, Sai‐Hong; Chul Cho, Byoung; Kim, Dong‐Wan; Lee, Jeeyun; J. Lin, Jessica; W. Zhu, Viola; Ahn, Myung‐Ju; Ross Camidge, D.; Nguyen, Judy; Zhai, Dayong; Deng, Wei; Huang, Zhongdong; Rogers, Evan; Liu, Juliet; Whitten, Jeff; K. C. Lim, John; Stopatschinskaja, Shanna; M. Hyman, David; C. Doebele, Robert; Jean Cui, J.; T. Shaw, Alice

doi:10.1158/2159-8290.cd-18-0484

Public

Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations

Published in Cancer Discovery • Aug 9, 2018

Authors:

Alexander Drilon

Sai‐Hong Ignatius Ou

Byoung Chul Cho

Abstract

Abstract The use of tyrosine kinase inhibitors (TKI) with activity against ALK, ROS1, or TRKA–C can result in significant clinical benefit in patients with diverse tumors harboring ALK, ROS1, or NTRK1–3 rearrangements; however, resistance invariably develops. The emergence of on-target kinase domain...

Subject

ROS1

Trk receptor

Tropomyosin receptor kinase A

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