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Title: Tegafur/gimeracil/oteracil  
Author: World Heritage Encyclopedia
Language: English
Subject: Tegafur, Chemotherapy, Cell-cycle nonspecific antineoplastic agents, Hazardous drugs, Thiopurine
Collection: Combination Drugs, Pyrimidine Antagonists
Publisher: World Heritage Encyclopedia


Combination of
Tegafur Antineoplastic drug
Gimeracil Enzyme inhibitor
Oteracil Enzyme inhibitor
Clinical data
Trade names Teysuno
Licence data EMA:
  • Contraindicated
Legal status
Routes of
CAS Registry Number
ATC code L01
PubChem CID:

The combination drug tegafur/gimeracil/oteracil (trade name Teysuno, and TS-1 in Japan[1]) is used for the treatment of advanced gastric cancer.[2] It is also being developed for the treatment of hepatocellular carcinoma.[3]

Mechanism of action

Tegafur is the actual chemotherapeutic agent. It is a prodrug of the active substance fluorouracil (5-FU).

Gimeracil inhibits the degradation of fluorouracil by reversibly blocking a dehydrogenase enzyme. This results in higher 5-FU levels and a prolonged half-life of the substance.

Oteracil mainly stays in the gut because of its low permeability, where it reduces the production of 5-FU by blocking the enzyme orotate phosphoribosyltransferase. Lower 5-FU levels in the gut result in a lower gastrointestinal toxicity.[4]

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