FGFR1 inhibitor

FGFR1 inhibitors are a class of targeted therapeutic agents designed to inhibit the activity of Fibroblast Growth Factor Receptor 1 (FGFR1), a member of the receptor tyrosine kinase family. FGFR1 plays a critical role in physiological processes such as embryonic development, cell proliferation, and angiogenesis; however, its dysregulation—often through gene amplification, mutations, or chromosomal translocations—is a driver in several malignancies, including squamous cell lung cancer, breast cancer, and certain myeloproliferative neoplasms. In the context of glioblastoma (GBM), recent research indicates that FGFR1 signaling regulates the transdifferentiation of glioblastoma stem cells (GSCs) into tumor-derived endothelial cells via interaction with transcription factors such as brachyury, SOX2, ZEB1, and YAP1. By blocking FGFR1, these inhibitors aim to suppress tumor neovascularization and growth, offering a potential therapeutic strategy for aggressive, highly vascularized tumors that are resistant to conventional therapies.

Other names

FGFR1 inhibitorsFGFR-1 inhibitorsFGFR 1 inhibitorsFibroblast growth factor receptor 1 inhibitor