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enzastaurin + 5-fluorouracil + leucovorin + bevacizumab
- Development stage
- Preclinical
- Lead developer
- Eli Lilly
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
Enzastaurin + 5-fluorouracil + leucovorin + bevacizumab is an investigational combination regimen composed of four anticancer agents: - **Enzastaurin**: a small molecule inhibitor of protein kinase C beta (PKCβ), investigated for anti-angiogenic and antiproliferative effects in cancers. - **5-fluorouracil (5-FU)**: an antimetabolite chemotherapy agent that inhibits thymidylate synthase, disrupting DNA synthesis and inducing cell death in rapidly dividing cells. - **Leucovorin (folinic acid)**: a chemoprotectant and enhancer of 5-FU efficacy, increases 5-FU binding to thymidylate synthase. - **Bevacizumab**: a recombinant humanized monoclonal IgG1 antibody that targets vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis to prevent tumor blood vessel growth[1][3][4][5]. This combination is primarily under investigation for **metastatic colorectal cancer** and other solid tumors, leveraging multiple mechanisms: anti-angiogenesis, direct cytotoxicity, and enhanced DNA synthesis inhibition.
- Other names
- enzastaurin + 5-fluorouracil + leucovorin + bevacizumab
02
Targets
PRKCB (Protein kinase C beta)PRKCG (Protein kinase C gamma)TS (Thymidylate synthase)PRKCA (Protein kinase C alpha)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)PRKCE (Protein Kinase C epsilon)VEGFA (Vascular endothelial growth factor A)
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