Difference between revisions of "Tegafur, gimeracil, oteracil (S-1)"
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==Diseases for which it is used== | ==Diseases for which it is used== | ||
*[[Breast cancer]] | *[[Breast cancer]] | ||
+ | *[[Cholangiocarcinoma]] | ||
*[[Colon cancer]] | *[[Colon cancer]] | ||
*[[Gastric cancer]] | *[[Gastric cancer]] | ||
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[[Category:Breast cancer medications]] | [[Category:Breast cancer medications]] | ||
+ | [[Category:Cholangiocarcinoma medications]] | ||
[[Category:Colon cancer medications]] | [[Category:Colon cancer medications]] | ||
[[Category:Gastric cancer medications]] | [[Category:Gastric cancer medications]] |
Revision as of 01:46, 23 April 2019
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
- Breast cancer
- Cholangiocarcinoma
- Colon cancer
- Gastric cancer
- Non-small cell lung cancer
- Pancreatic cancer
- Rectal cancer
Also known as
- Brand name: Teysuno