tegafur + gimeracil

tegafur + gimeracil is an oral combination chemotherapy agent consisting of tegafur, a prodrug of the antimetabolite 5-fluorouracil (5-FU), and gimeracil, a potent inhibitor of dihydropyrimidine dehydrogenase (DPD). Tegafur is bioactivated in vivo to 5-FU, which exerts its antitumor effects by inhibiting thymidylate synthase and incorporating into RNA and DNA, thereby disrupting nucleic acid synthesis and cell proliferation. Gimeracil functions by blocking the DPD-mediated degradation of 5-FU, which significantly increases the systemic exposure and half-life of the active drug. This combination is primarily investigated and used for the treatment of gastrointestinal malignancies, including gastric and esophageal cancers, and is most commonly encountered as a component of the triple-drug formulation S-1 (also known as TS-1), which additionally includes oteracil potassium to reduce gastrointestinal toxicity.

Other names

Tegafur-Gimeracil