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S-1 is an oral fluoropyrimidine combination chemotherapy agent composed of tegafur, gimeracil, and oteracil potassium in a molar ratio of 1:0.4:1. Tegafur is a prodrug that is converted into 5-fluorouracil (5-FU) in the body. Gimeracil (5-chloro-2,4-dihydroxypyridine) is a potent inhibitor of dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for 5-FU degradation, thereby maintaining high plasma concentrations of 5-FU. Oteracil potassium (monopotassium 1,2,4-triazine-3,5-dione-6-carboxylate) selectively inhibits the phosphorylation of 5-FU by orotate phosphoribosyltransferase (OPRT) in the gastrointestinal tract, which reduces the gastrointestinal toxicity associated with 5-FU. Originally developed by Taiho Pharmaceutical, S-1 is primarily used for the treatment of various solid tumors, including gastric, colorectal, and esophageal cancers. In clinical research, it is often studied as a component of concurrent chemoradiotherapy regimens.
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