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5-fluorouracil + folinic acid + pyridoxine

Development stage: Preclinical
Modality: Small Molecules
Administration: Intravenous

Overview

A combination regimen consisting of 5-fluorouracil (FUra), folinic acid (leucovorin, FA), and high-dose pyridoxine (vitamin B6). This combination enhances the cytotoxic effects of 5-fluorouracil through synergistic mechanisms. The primary mechanism involves fluorodeoxyuridine monophosphate (FdUMP), the active metabolite of 5-fluorouracil, binding to thymidylate synthase and the folate cofactor to form a TS-inactivating ternary complex. High-dose pyridoxine further potentiates this cytotoxicity. Clinical studies have shown promising results in digestive tract carcinomas and breast cancer.

Targets

TS (Thymidylate synthase)

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