Difference between revisions of "Tegafur, gimeracil, oteracil (S-1)"
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*[[Breast cancer]] | *[[Breast cancer]] | ||
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[[Category:EMA approved drugs]] | [[Category:EMA approved drugs]] | ||
[[Category:PMDA approved drugs]] | [[Category:PMDA approved drugs]] | ||
Revision as of 16:33, 2 January 2018
Note: this drug is approved in Japan and Europe but not the US. References will be gradually added.
Mechanism of action
From the NCI Drug Dictionary: An orally bioavailable fluoropyrimidine antagonist composed of tegafur combined with two modulators of 5-flurouracil (5-FU) activity, 5-chloro-2,4-dihydroxypyridine (CDHP) 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. CDHP 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.
Diseases for which it is used
Also known as
- Brand name: Teysuno