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Tegafur is an oral chemotherapeutic prodrug of 5-fluorouracil (5-FU), classified as a pyrimidine analogue antimetabolite. It is gradually converted to the active drug fluorouracil in the liver, where it inhibits thymidylate synthase, disrupting DNA synthesis and function, and intercalates into RNA, leading to cytotoxicity in tumor cells. Tegafur is primarily used for the treatment of advanced gastric and colorectal cancers, often in combination with other agents such as uracil (as tegafur/uracil or UFT) or gimeracil and oteracil (as S‑1). These combinations enhance its bioavailability by inhibiting dihydropyrimidine dehydrogenase-mediated degradation of 5-FU. Tegafur was patented in 1967 and approved for medical use in 1972[2][4][5].
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