Drug intelligence / Profile preview

brivanib alaninate + cetuximab

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Brivanib alaninate + cetuximab is a combination therapy investigated for the treatment of advanced and metastatic colorectal cancer (particularly KRAS wild-type), as well as other advanced gastrointestinal malignancies. Brivanib alaninate is an oral prodrug that converts to brivanib (BMS-540215), a small molecule dual tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR). Cetuximab is a chimeric monoclonal antibody that targets the epidermal growth factor receptor (EGFR). The rationale for combining these agents is to simultaneously inhibit tumor angiogenesis and EGFR-mediated signaling pathways. Clinical trials have shown that while this combination can improve progression-free survival and objective response rates compared to cetuximab alone in chemotherapy-refractory metastatic colorectal cancer, it does not significantly improve overall survival and increases toxicity with worsened quality of life[1][2][3][4].

Brand names
Erbitux
Other names
brivanib + cetuximabcetuximab + brivanib alaninate
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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