Drug intelligence / Profile preview

brivanib + 5-fluorouracil + leucovorin

Development stage
Phase 1
Lead developer
Zai Lab
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**Brivanib + 5-fluorouracil + leucovorin** is an experimental combination therapy comprising three active agents: brivanib, a selective small-molecule tyrosine kinase inhibitor of the vascular endothelial growth factor (VEGF) and fibroblast growth factor (FGF) signaling pathways; 5-fluorouracil, a pyrimidine analog antimetabolite that inhibits DNA synthesis; and leucovorin, a reduced folate that enhances the cytotoxic effects of 5-fluorouracil. This combination is being explored primarily as an antineoplastic regimen for advanced solid tumors, most notably in hepatocellular carcinoma and other malignancies refractory to standard treatment. Brivanib was developed by Bristol Myers Squibb and has shown activity in clinical trials as monotherapy, but there is limited clinical trial data specifically addressing its combination with 5-fluorouracil and leucovorin. The rationale behind this combination is to target angiogenesis (brivanib) and tumor cell proliferation (5-fluorouracil, with leucovorin potentiation) for potential additive or synergistic effects against cancer.

02

Targets

FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)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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