HS-10375, a selective EGFR C797S tyrosine kinase inhibitor, in advanced non-small cell lung cancer.

doi:10.1186/s12967-025-06613-0

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Article

HS-10375, a selective EGFR C797S tyrosine kinase inhibitor, in advanced non-small cell lung cancer.

Journal of translational medicine - 4 Jun 2025

Zhan Jianhua, Xue Jinhui, Wu Lin, Zhang Zhiye, Wang Qiming, Ma Yuxiang, Huang Yan, Yang Yunpeng, Zhao Yuanyuan, Fang Wenfeng, Zhang Yang, Liu Qianwen, Xu Wen, Yang Yan, Chen Zhenming, Song Baili, Sun Danni, Sun Xia, Gao Peng, Zhao Hongyun, Zhang Li

Abstract excerpt

BACKGROUND: The C797S mutation is one of the most common mechanisms of acquired resistance to third generation EGFR TKIs, yet no approved therapies have been available to target it. Here we developed a novel selective EGFR C797S inhibitor, HS-10375, and report the results of pre-clinical research and the first-in-human phase 1 trial. METHODS: Ba/F3 cell lines and patient-derived cells expressing mutant EGFR were...

Topics

Humans
ErbB Receptors
Protein Kinase Inhibitors
Animals
Carcinoma, Non-Small-Cell Lung
Cell Line, Tumor
Lung Neoplasms
Xenograft Model Antitumor Assays
Female

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Male

Mice

Mutation

Phosphorylation

Middle Aged

Mice, Nude

Aged

Tyrosine Kinase Inhibitors

Source

Open in PubMed Open full text

Identifiers

PMID: 40468352
DOI: 10.1186/s12967-025-06613-0
PMCID: PMC12135467

Genes

EGFR
F3

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 30 Aug 2026.

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