Drug intelligence / Profile preview

BMS-817378

Development stage
Phase 2
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

BMS-817378 is a novel prodrug of the small molecule dual Met/VEGFR-2 inhibitor BMS-794833. It acts as an oral inhibitor targeting multiple receptor tyrosine kinases including c-Met (hepatocyte growth factor receptor), Axl, Ron, and Tyro3 with high selectivity. The drug was developed for oncology indications and has been investigated in advanced solid tumors such as papillary carcinoma, squamous cell carcinoma, renal cell carcinoma, prostate cancer, esophageal cancer, gastrointestinal cancer, and head and neck cancer. Its mechanism involves antagonism of c-Met (hepatocyte growth factor receptor) and vascular endothelial growth factor receptor 2 (VEGFR-2), thereby inhibiting pathways involved in tumor proliferation and angiogenesis. Development was led by Bristol Myers Squibb with Simcere Pharmaceutical Group co-developing for the Chinese market[1][2][3][4][5].

Other names
N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
02

Targets

AXL (AXL receptor tyrosine kinase)MST1R (Recepteur d'origine nantais)VEGFR2 (Vascular endothelial growth factor receptor 2)FLT3 (Fms related receptor tyrosine kinase 3)MET (Mesenchymal-epithelial transition factor receptor)

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