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Gimeracil and oteracil potassium are components of an oral combination chemotherapy regimen most commonly used with tegafur (as in the product S-1 or Teysuno) for the treatment of advanced gastric cancer and other solid tumors. Gimeracil is a potent reversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for degrading 5-fluorouracil (5-FU), thereby increasing systemic exposure to 5-FU. Oteracil potassium inhibits orotate phosphoribosyltransferase (OPRT) in gastrointestinal tissues, reducing local activation of 5-FU and thus decreasing gastrointestinal toxicity. This combination is designed to enhance antitumor efficacy while minimizing side effects when administered with a fluoropyrimidine prodrug such as tegafur[6][8][9]. The primary indication is advanced gastric cancer in combination with cisplatin; it has also been studied or used off-label for colorectal, pancreatic, breast, esophageal, and cervical cancers[7][10].
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