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brivanib alaninate + 5-fluorouracil + leucovorin + oxaliplatin
- Development stage
- Discontinued
- 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.
- Other names
- brivanib alaninateBMS-582664BMS582664BMS 582664brivanib5-fluorouracilleucovorinoxaliplatin
02
Targets
DNAFGFR (Fibroblast growth factor receptor)TS (Thymidylate synthase)VEGFR (VEGFR family)FGFR (FGFR family)
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