Difference between revisions of "Tegafur, gimeracil, oteracil (S-1)"
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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. | 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 | + | ==Diseases for which it is established== |
*[[Breast cancer]] | *[[Breast cancer]] | ||
*[[Cholangiocarcinoma]] | *[[Cholangiocarcinoma]] | ||
| − | *[[Colon cancer]] | + | *[[Colorectal cancer]] |
| + | **[[Colon cancer]] | ||
| + | **[[Rectal cancer]] | ||
*[[Gallbladder cancer]] | *[[Gallbladder cancer]] | ||
*[[Gastric cancer]] | *[[Gastric cancer]] | ||
| + | *[[Head and neck cancer]] | ||
*[[Non-small cell lung cancer]] | *[[Non-small cell lung cancer]] | ||
**[[Non-small cell lung cancer, squamous]] | **[[Non-small cell lung cancer, squamous]] | ||
*[[Pancreatic cancer]] | *[[Pancreatic cancer]] | ||
| − | *[[ | + | |
| + | ==Diseases for which it is used== | ||
| + | *[[Esophageal cancer]] | ||
==History of changes in EMA indication== | ==History of changes in EMA indication== | ||
*2011-03-14: Initial marketing authorization as Teysuno. | *2011-03-14: Initial marketing authorization as Teysuno. | ||
==History of changes in PMDA indication== | ==History of changes in PMDA indication== | ||
| − | *2005-11-14: | + | *2005-11-14: New indication for the treatment of inoperable or recurrent [[breast cancer]]. |
| − | *2006-08-10: | + | *2006-08-10: New indication for [[pancreatic cancer]]. |
| − | *2007-08-23: | + | *2007-08-23: New indication for the treatment of [[:Category:Biliary tract cancers|biliary cancer]] in addition to [[gastric cancer]], [[colorectal cancer]], [[head and neck cancer]], [[non-small cell lung cancer]], and [[pancreatic cancer]]. |
| − | *2007-08-23: | + | *2007-08-23: New indication for the treatment of inoperable or relapsed [[breast cancer]]. |
| − | *2022-11-24: | + | *2022-11-24: New indication and a new dosage for the postoperative adjuvant treatment of hormone receptor(HR)-positive and human epidermal growth factor receptor 2 (HER2)-negative [[breast cancer]] with a high risk of recurrence. |
==Also known as== | ==Also known as== | ||
| Line 37: | Line 42: | ||
[[Category:Cholangiocarcinoma medications]] | [[Category:Cholangiocarcinoma medications]] | ||
[[Category:Colon cancer medications]] | [[Category:Colon cancer medications]] | ||
| + | [[Category:Colorectal cancer medications]] | ||
| + | [[Category:Esophageal cancer medications]] | ||
[[Category:Gallbladder cancer medications]] | [[Category:Gallbladder cancer medications]] | ||
[[Category:Gastric cancer medications]] | [[Category:Gastric cancer medications]] | ||
Latest revision as of 00:26, 7 November 2023
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 established
- Breast cancer
- Cholangiocarcinoma
- Colorectal cancer
- Gallbladder cancer
- Gastric cancer
- Head and neck cancer
- Non-small cell lung cancer
- Pancreatic cancer
Diseases for which it is used
History of changes in EMA indication
- 2011-03-14: Initial marketing authorization as Teysuno.
History of changes in PMDA indication
- 2005-11-14: New indication for the treatment of inoperable or recurrent breast cancer.
- 2006-08-10: New indication for pancreatic cancer.
- 2007-08-23: New indication for the treatment of biliary cancer in addition to gastric cancer, colorectal cancer, head and neck cancer, non-small cell lung cancer, and pancreatic cancer.
- 2007-08-23: New indication for the treatment of inoperable or relapsed breast cancer.
- 2022-11-24: New indication and a new dosage for the postoperative adjuvant treatment of hormone receptor(HR)-positive and human epidermal growth factor receptor 2 (HER2)-negative breast cancer with a high risk of recurrence.
Also known as
- Code name: S-1
- Brand name: Teysuno, TS-One, TS-1
Categories:
- Drugs
- Combination drugs
- Oral medications
- Fluoropyrimidines
- Breast cancer medications
- Cholangiocarcinoma medications
- Colon cancer medications
- Colorectal cancer medications
- Esophageal 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