Drug intelligence / Profile preview

BMS-690514

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

Overview

BMS‑690514 is a pyrrolotriazine-based small molecule that acts as a potent and reversible oral inhibitor of multiple receptor tyrosine kinases. Specifically, it targets the epidermal growth factor receptor (EGFR/HER‑1), HER‑2 and HER‑4 receptors (members of the ERBB family), as well as vascular endothelial growth factor receptors VEGFR‑1 to VEGFR‑3. By inhibiting these pathways simultaneously, BMS‑690514 was designed to block tumor cell proliferation and angiogenesis in cancer. It was developed by Bristol Myers Squibb for use as an oral antineoplastic agent in cancers such as non-small cell lung cancer and breast cancer; however, clinical development for these indications has been discontinued after phase II trials.[7][8][5][6]

Other names
(3R,4R)-4-Amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol(3R,4R)-4-amino-1-{4-[3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin–5–yl}methyl)piperidin–3–ol
02

Targets

LCK (Proto-oncogene tyrosine-protein kinase Lck)VEGFR2 (Vascular endothelial growth factor receptor 2)EGFR (Epidermal growth factor receptor)PKA (Cyclic amp-dependent protein kinase)ERBB4 (Erb-b2 receptor tyrosine kinase 4)VEGFR-1 (Vascular endothelial growth factor receptor 1)ERBB2 (Erb-b2 receptor tyrosine kinase 2)FLT3 (Fms related receptor tyrosine kinase 3)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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