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Tegafur is the actual chemotherapeutic agent. It is a prodrug of the active substance fluorouracil (5-FU).Gimeracil inhibits the degradation of fluorouracil by reversibly blocking a dehydrogenase enzyme. This results in higher 5-FU levels and a prolonged half-life of the substance.Oteracil mainly stays in the gut because of its low permeability, where it reduces the production of 5-FU by blocking the enzyme orotate phosphoribosyltransferase. Lower 5-FU levels in the gut result in a lower gastrointestinal toxicity.
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