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Article

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

Cancer discovery - 1 Oct 2018

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

Abstract excerpt

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 mutations represents a major mechanism of acquired resistance. Solvent-front substitutions such as ALKG1202R, ROS1G2032R or...

Read the complete abstract on PubMed

Topics

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Share to ALK gene
Share to NTRK1 gene

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to NTRK3 gene

Share to ROS1 gene

Share to Mutation

Share to Protein Kinase Inhibitors

Share to Protein-Tyrosine Kinases

Share to Proto-Oncogene Proteins

Source

Identifiers

PMID: 30093503
DOI: 10.1158/2159-8290.CD-18-0484

Genes

ROS1
ALK
NTRK1
NTRK3

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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