Repotrectinib Exhibits Potent Antitumor Activity in Treatment-Naive and Solvent-Front-Mutant ROS1-Rearranged Non-Small Cell Lung Cancer.

ABSTRACT:

Purpose

Although first-line crizotinib treatment leads to clinical benefit in ROS1⁺ lung cancer, high prevalence of crizotinib-resistant ROS1-G2032R (ROS1^G2032R) mutation and progression in the central nervous system (CNS) represents a therapeutic challenge. Here, we investigated the antitumor activity of repotrectinib, a novel next-generation ROS1/TRK/ALK-tyrosine kinase inhibitor (TKI) in ROS1⁺ patient-derived preclinical models.

Experimental design

Antitumor activity of repotrectinib was evaluated in ROS1⁺ patient-derived preclinical models including treatment-naïve and ROS1^G2032R models and was further demonstrated in patients enrolled in an on-going phase I/II clinical trial (NCT03093116). Intra

SUBMITTER: Yun MR 

PROVIDER: S-EPMC10283448 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature