Drug intelligence / Profile preview

BMS-690514 + letrozole

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

Overview

BMS-690514 + letrozole is an investigational oral combination therapy consisting of BMS-690514, a small molecule, potent reversible inhibitor of the tyrosine kinases epidermal growth factor receptor (EGFR/HER-1), HER-2, HER-4, and vascular endothelial growth factor receptors (VEGFR-1/-2/-3), and letrozole, a nonsteroidal aromatase inhibitor that blocks estrogen synthesis. The combination is designed to provide broad, multi-targeted inhibition of tumor growth, angiogenesis, and estrogen-driven breast cancer cell proliferation. The primary evaluation has been for metastatic breast cancer, particularly in hormone receptor-positive settings and other advanced solid tumors[3][1][5].

02

Targets

GAK (Cyclin G-associated kinase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)VEGFR2 (Vascular endothelial growth factor receptor 2)CYP19A1 (Aromatase)ERBB4 (Erb-b2 receptor tyrosine kinase 4)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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