Potassium oxonate is an inhibitor of orotate phosphoribosyltransferase (OPRT) that is an enzyme involved in the biosynthesis of pyrimidine nucleotides and catalyzes the phosphorylation of 5-FU [
F0151] to an active metabolite 5-fluorouridine-5'-monophosphate (FUMP). The gastrointestinal toxicity (GIT) of the oral administration of 5-FU is also caused by the phosphorylation by OPRT in the gut wall. Potassium oxonate selectively and competitively inhibits OPRT. As a result, 5-FU associated gastrointestinal toxic effects are reduced. Potassium oxonate is often used as combined agents to enhance the antitumor activity of fluoropyrimidines, such as S-1 (tegafur [
F0635] a prodrug of 5-FU, gimeracil [
C2243] and potassium oxonate at a molar ratio of 1:0.4:1). (The product is for research purpose only.)