Drug intelligence / Profile preview

cetuximab + bevacizumab + fluorouracil + leucovorin

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

This is a combination regimen consisting of **cetuximab**, **bevacizumab**, **fluorouracil**, and **leucovorin**. Cetuximab is a chimeric monoclonal antibody targeting the epidermal growth factor receptor (EGFR), blocking EGFR-mediated signaling and cellular proliferation. Bevacizumab is a humanized monoclonal antibody targeting vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis. Fluorouracil (5-FU) is a pyrimidine antimetabolite that inhibits thymidylate synthase, resulting in impaired DNA synthesis. Leucovorin (folinic acid) is used to enhance the efficacy of fluorouracil by stabilizing the binding of its active metabolite to thymidylate synthase. This combination is primarily investigated as a first-line or experimental therapy in metastatic colorectal cancer, particularly in patients with KRAS wild-type tumors. Large randomized studies have investigated this combination, but it is not standard of care due to a lack of proven superiority to established doublet or triplet regimens and potential for increased toxicity[1][3][5].

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TS (Thymidylate synthase)VEGFA (Vascular endothelial growth factor A)

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