Drug intelligence / Profile preview

metformin + fluorouracil

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Metformin + fluorouracil is a combination drug consisting of metformin, an oral hypoglycemic agent primarily used for type 2 diabetes, and fluorouracil (5-FU), a widely used chemotherapeutic antimetabolite. Metformin has been found to have antitumor effects by inhibiting cancer cell proliferation and enhancing the efficacy of chemotherapy agents. Fluorouracil works mainly by inhibiting thymidylate synthase, thereby interfering with DNA synthesis and RNA function in rapidly dividing cancer cells. The combination has been studied particularly in colorectal cancer (CRC) where metformin enhances the therapeutic effects of 5-FU by increasing inhibition of cell proliferation, colony formation, migration, and inducing cell cycle arrest more effectively than either agent alone. Clinical trials have shown modest but promising activity in refractory CRC patients with manageable toxicity profiles. This combination is under investigation to improve outcomes especially in gastrointestinal cancers including colorectal and gastric cancers.[1][2][3][4]

02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)TS (Thymidylate synthase)

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