NCIt synonyms : Tegafur, mixture with Gimeracil and Potassium Oxonate; Tegafur/Gimeracil/Oteracil;
NCIt related terms : S-1; BMS-247616; Tegafur gimeracil oteracil;
NCIt definition : An orally bioavailable fluoropyrimidine antagonist composed of tegafur combined with
two modulators of 5-fluorouracil (5-FU) activity, gimeracil and potassium oxonate,
in a molar ratio of 1:0.4:1. Tegafur is a prodrug of 5-fluorouracil, an antimetabolite
that inhibits thymidylate synthase, DNA synthesis and cell division, and competes
with uridine triphosphate, thus inhibiting RNA and protein synthesis. Gimeracil is
a reversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the liver enzyme
responsible for rapid catabolism of 5-FU into inactive metabolites. Potassium oxonate
preferentially localizes in the gut and inhibits the enzyme orotate phosphoribosyl-transferase
(OPRT), thereby decreasing activation of 5-FU in the gut and activated 5-FU-related
gastrointestinal toxicity.;
Alternative definition : NCI-GLOSS: A drug that is being studied for its ability to enhance the effectiveness
of fluorouracil and prevent gastrointestinal side effects caused by fluorouracil.
It belongs to the family of drugs called antimetabolites.;