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Drug intelligence / Profile preview
enzastaurin + 5-fluorouracil + leucovorin + bevacizumab
- Development stage
- Phase 2
- 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.
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
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