Difference between revisions of "Tegafur, gimeracil, oteracil (S-1)"
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[[Category:Rectal cancer medications]] | [[Category:Rectal cancer medications]] |
Revision as of 18:37, 5 May 2022
Note: this drug is approved in Japan and Europe but not the US.
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
- Gallbladder cancer
- Gastric cancer
- Non-small cell lung cancer
- Pancreatic cancer
- Rectal cancer
History of changes in EMA indication
- 3/14/2011: Initial marketing authorization as Teysuno.
Also known as
- Code name: S-1
- Brand name: Teysuno, TS-One
- Drugs
- Combination drugs
- Oral medications
- Fluoropyrimidines
- Breast cancer medications
- Cholangiocarcinoma medications
- Colon cancer medications
- Gallbladder cancer medications
- Gastric cancer medications
- Non-small cell lung cancer medications
- Non-small cell lung cancer, squamous medications
- Pancreatic cancer medications
- Rectal cancer medications
- EMA approved in 2011
- PMDA approved drugs