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. Lim, John; Stopatschinskaja, Shanna; M. Hyman, David; C. Doebele, Robert; Jean Cui, J.; T. Shaw, Alice

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

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

Shared by NobleBlocks on Oct 1, 2018 • 12:00 AM UTC

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...

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