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Tegafur + gimeracil + oteracil is an oral fixed-dose combination chemotherapy used primarily for the treatment of advanced gastric cancer and other solid tumors. Tegafur is a prodrug of fluorouracil (5-FU), a cytotoxic antimetabolite that inhibits DNA synthesis by mimicking pyrimidine and interfering with thymidylate synthase. Gimeracil inhibits dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for 5-FU degradation, thereby increasing systemic exposure to 5-FU. Oteracil acts locally in the gut to inhibit orotate phosphoribosyltransferase and reduce gastrointestinal toxicity by limiting 5-FU activation in GI tissues. The combination allows for effective systemic anticancer activity with reduced GI side effects compared to traditional fluoropyrimidine therapy[1][6][9]. It is approved as first-line therapy in advanced gastric cancer (often combined with cisplatin) and has indications or clinical use in head and neck cancer, colorectal cancer, non–small-cell lung cancer, breast cancer, pancreatic cancer, biliary tract cancers[1][3][4][5].
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