Tegafur/gimeracil/oteracil

From WikiMD


The combination drug tegafur/gimeracil/oteracil (trade name Teysuno, and TS-1 in Japan[1]), also known as S-1,[2] is used for the treatment of advanced gastric cancer.[3] It is labelled for use in combination with cisplatin in many European countries, and for head and neck cancer, colorectal cancer, non–small-cell lung, breast, pancreatic, and biliary tract cancers in several countries in Asia.[4]:213 It has not been approved by the FDA.[4]:213

It is also being developed for the treatment of hepatocellular carcinoma.[5] and has activity in esophageal,(Perry Chapter 33) breast,[citation needed] cervical,[citation needed] and colorectal cancer.[6]

Within the medication, the molar ratio of the three components (tegafur:gimeracil:oteracil) is 1:1:0.4.[7]

The maximum tolerated dose differed between Asian and Caucasian populations (80 mg/m2 and 25 mg/m2 respectively), perhaps due to differences in CYP2A6 genotype.[4]:213

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 the dehydrogenase enzyme dihydropyrimidine dehydrogenase (DPD). This results in higher 5-FU levels and a prolonged half-life of the substance.[8]

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.[8]

References


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