Drug intelligence / Profile preview

cyclophosphamide + fluorouracil + leucovorin + methotrexate

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous, Oral (for Some Components Such As Methotrexate Or Leucovorin)
01

Overview

This is a combination chemotherapy regimen consisting of four agents: cyclophosphamide, fluorouracil (5-FU), leucovorin (folinic acid), and methotrexate. Each drug has a distinct mechanism of action targeting cancer cell proliferation: - Cyclophosphamide is an alkylating agent that crosslinks DNA, leading to cell death. - Fluorouracil is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis. - Methotrexate inhibits dihydrofolate reductase, blocking folic acid metabolism and DNA synthesis. - Leucovorin enhances the cytotoxicity of fluorouracil by stabilizing its binding to thymidylate synthase and also serves as a "rescue" agent to reduce methotrexate toxicity. This combination has been studied primarily in metastatic breast cancer and advanced colorectal cancer. The addition of leucovorin can preserve antitumor activity while decreasing serious infections associated with the regimen[1][2][8]. The drugs act synergistically by targeting different pathways involved in nucleotide synthesis and cell division.

Other names
CMFFCMF with folinic acid
02

Targets

DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)DNA

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