Drug intelligence / Profile preview

BMS-690514 + folinic acid + 5-fluorouracil + oxaliplatin

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This drug is a **combination regimen** consisting of BMS-690514, folinic acid (leucovorin), 5-fluorouracil (5-FU), and oxaliplatin. - **BMS-690514** is a potent, reversible oral inhibitor targeting **epidermal growth factor receptor (EGFR/HER-1), HER-2 and HER-4, and vascular endothelial growth factor receptors (VEGFR) 1–3**. It blocks tumor growth and angiogenesis by inhibiting these receptor tyrosine kinases[1][3]. - **Folinic acid** (leucovorin) is used to enhance the effectiveness of 5-fluorouracil by stabilizing its binding to thymidylate synthase. - **5-fluorouracil** is an antimetabolite chemotherapeutic agent that inhibits thymidylate synthase, impairing DNA synthesis. - **Oxaliplatin** is a platinum-based chemotherapy drug that forms DNA crosslinks, leading to cell death. This combination is designed for **anticancer therapy** by targeting tumor cell signaling, DNA synthesis, and DNA integrity, potentially used for advanced solid tumors or colorectal cancer. BMS-690514 was originally developed by Bristol Myers Squibb as a targeted therapy, whereas folinic acid, 5-fluorouracil, and oxaliplatin are established chemotherapeutics.

02

Targets

DNAEGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)TS (Thymidylate synthase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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