Drug intelligence / Profile preview

brivanib alaninate + 5-fluorouracil + leucovorin + oxaliplatin

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

Overview

- **Brivanib alaninate (BMS-582664)** is an oral small molecule prodrug converted in vivo to brivanib (BMS-540215), a selective dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) tyrosine kinases. Its principal mechanism is inhibition of tumor angiogenesis and proliferation via VEGFR and FGFR blockade. - **5-Fluorouracil (5-FU)** is a pyrimidine analog antimetabolite that inhibits thymidylate synthase, disrupting DNA/RNA synthesis and leading to cell death, especially in rapidly dividing cells. - **Leucovorin (folinic acid)** potentiates the effects of 5-FU by stabilizing its binding to thymidylate synthase, enhancing cytotoxicity. - **Oxaliplatin** is a platinum-based chemotherapeutic that forms DNA adducts, inhibiting DNA replication and transcription, resulting in apoptosis. - This combination is experimental—primarily studied for **metastatic colorectal cancer** in clinical trials. - **Brivanib alaninate** was developed by Bristol Myers Squibb.

Brand names
brivanib alaninate
Other names
brivanib alaninateBMS-582664BMS582664BMS 582664brivanib5-fluorouracilleucovorinoxaliplatin
02

Targets

DNATS (Thymidylate synthase)VEGFR (VEGFR family)FGFR (Fibroblast growth factor receptor)

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