Drug intelligence / Profile preview

5-fluorouracil + folic acid + capecitabine + bevacizumab

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

Overview

This is a combination regimen used primarily in the treatment of metastatic colorectal cancer and other gastrointestinal cancers. It includes: - **5-fluorouracil**: An antimetabolite that disrupts DNA and RNA synthesis by inhibiting thymidylate synthase, leading to cell death. It is often administered with a folate cofactor to enhance its activity[1][2][6]. - **Folic acid** (often given as leucovorin/folinic acid): Potentiates the effect of 5-FU by stabilizing the binding of its active metabolite to thymidylate synthase[4]. - **Capecitabine**: An oral prodrug converted enzymatically into 5-FU preferentially within tumor tissue, mimicking continuous infusion pharmacokinetics while allowing oral administration[1][2]. - **Bevacizumab**: A monoclonal antibody targeting vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis required for tumor growth. This combination exploits synergistic mechanisms—antimetabolite cytotoxicity and antiangiogenic effects—to improve outcomes in advanced cancers, especially metastatic colorectal cancer. Capecitabine serves as an alternative or adjunct to intravenous 5-FU, offering similar efficacy with greater convenience[1][2][4][5]. Bevacizumab adds an antiangiogenic component that has been shown to further improve progression-free survival when combined with fluoropyrimidine-based chemotherapy.

Brand names
Xeloda (capecitabine)Avastin (bevacizumab)
Other names
5-FU (for 5-fluorouracil)leucovorin (for folic acid/folinic acid)
02

Targets

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