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  • A modulator of 5-fluorouracil (5-FU) activity and inhibitor of the enzyme orotate phosphoribosyl-transferase (OPRT), with chemoprotective activity. Oteracil preferentially localizes in the gastrointestinal (GI) tract where it inhibits OPRT, thereby decreasing metabolism of 5-FU into its active metabolite 5-fluorouridine-5\'-monophosphate (FUMP). This decreases activated 5-FU-related gastrointestinal toxicity.
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