Drug intelligence / Profile preview

5-fluorouracil + leucovorin + bevacizumab

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

Overview

This combination regimen consists of three drugs: 5-fluorouracil, leucovorin (folinic acid), and bevacizumab. It is primarily used in the treatment of metastatic colorectal cancer, often as part of first-line or second-line therapy. **Mechanism of action:** - **5-fluorouracil** is a pyrimidine antagonist that interferes with nucleic acid metabolism by incorporating its active metabolites into RNA and DNA, causing damage to tumor cells. Its metabolite FdUMP irreversibly inhibits thymidylate synthase, leading to DNA synthesis inhibition and cell death[6]. - **Leucovorin** enhances the binding of 5-FU to thymidylate synthase, increasing its cytotoxic effect[6]. - **Bevacizumab** is a monoclonal antibody targeting vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis required for tumor growth[8][1][3]. The addition of bevacizumab to fluorouracil-based chemotherapy regimens has been shown in clinical trials to improve response rates and prolong survival in patients with metastatic colorectal cancer[1][2][3][4].

Brand names
Avastin (for bevacizumab)
Other names
5-FU + LV + bevacizumabfluorouracil + folinic acid (leucovorin) + bevacizumab
02

Targets

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