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Entrectinib can induce nerve cell damage by inhibiting PI3K-AKT and TGF-β signaling pathways.


ABSTRACT:

Background

The tyrosine receptor kinase inhibitor (TRKi) entrectinib is used to treat neurotrophic tyrosine receptor kinase (NTRK) fusion-positive solid tumors and ROS1-positive patients. Despite its impressive efficacy against cancer, the clinical application is still limited by the central nervous system (CNS)-related toxicities. However, the precise mechanism of such CNS-related toxicities remains elusive.

Methods

The effect of entrectinib-induced nerve cell damage was evaluated by the nerve cells (PC12, HT22 and SK-N-SH) based in vitro models. Various assays, including CCK-8, colony formation and EdU incorporation assays were utilized to estimate the cellular viability and proliferation ability. Cell apoptosis was measured by flow cytometry. Next, transcriptome se

SUBMITTER: Tang Q 

PROVIDER: S-EPMC11865199 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature