Difference between revisions of "Tegafur, gimeracil, oteracil (S-1)"
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*[[Pancreatic cancer]] | *[[Pancreatic cancer]] | ||
*[[Rectal cancer]] | *[[Rectal cancer]] | ||
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| + | ==History of changes in EMA indication== | ||
| + | *3/14/2011: Initial marketing authorization as Teysuno. | ||
==Also known as== | ==Also known as== | ||
*'''Code name:''' S-1 | *'''Code name:''' S-1 | ||
| − | *'''Brand name:''' Teysuno | + | *'''Brand name:''' Teysuno, TS-One |
[[Category:Drugs]] | [[Category:Drugs]] | ||
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[[Category:Rectal cancer medications]] | [[Category:Rectal cancer medications]] | ||
| − | [[Category:EMA approved | + | [[Category:EMA approved in 2011]] |
[[Category:PMDA approved drugs]] | [[Category:PMDA approved drugs]] | ||
Revision as of 16:36, 4 December 2021
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
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