Drug intelligence / Profile preview

brivanib + 5-fluorouracil + leucovorin + irinotecan

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

Overview

This is an **investigational multi-agent combination therapy** consisting of brivanib, 5-fluorouracil, leucovorin, and irinotecan, designed for the treatment of advanced cancers. **Brivanib** is a small molecule inhibitor targeting vascular endothelial growth factor (VEGF) and fibroblast growth factor receptors (FGFR), inhibiting tumor angiogenesis and cell proliferation[1][3][5][7]. **Irinotecan** is a DNA topoisomerase I inhibitor, leading to DNA damage and cell death, mainly used for solid tumors such as colorectal cancer[2][4][6]. **5-fluorouracil** (5-FU) is a pyrimidine analog antimetabolite that inhibits thymidylate synthase, thus blocking DNA synthesis. **Leucovorin** is used to enhance the cytotoxicity of 5-FU by stabilizing its binding to thymidylate synthase. This combination brings together **targeted antiangiogenic therapy and cytotoxic chemotherapy**. Brivanib has been studied for various solid tumors, including soft tissue sarcoma, ovarian, and endometrial cancer, while the combination of irinotecan, 5-FU, and leucovorin (known as FOLFIRI) is standard in colorectal and other gastrointestinal cancers[1][2].

02

Targets

TOP1 (DNA Topoisomerase I)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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