|AHFS/Drugs.com||UK Drug Information|
The combination drug tegafur/gimeracil/oteracil (trade name Teysuno, and TS-1 in Japan), also known as S-1, is used for the treatment of advanced gastric cancer. 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.:213 It has not been approved by the FDA.:213
It is also being developed for the treatment of hepatocellular carcinoma. and has activity in esophageal,(Perry Chapter 33) breast, cervical, and colorectal cancer.
Within the medication, the molar ratio of the three components (tegafur:gimeracil:oteracil) is 1:1:0.4.
Mechanism of action
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.
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.
- TS-1.jp, Taiho Pharmaceutical
- Liu TW, Chen LT (201). "S-1 with leucovorin for gastric cancer: how far can it go?". Lancet Oncol. 17: 12–4. PMID 26640038. doi:10.1016/S1470-2045(15)00478-7.
- UK Drug Information
- DeVita, DeVita; Lawrence, TS; Rosenberg, SA (2015). DeVita, Hellman, and Rosenberg's Cancer: Principles and Practice of Oncology (10th ed.). LWW. ISBN 978-1451192940.
- Miyamoto Y, Sakamoto Y, Yoshida N, Baba H (2014). "Efficacy of S-1 in colorectal cancer". Expert Opin Pharmacother. 15 (12): 1761–70. PMID 25032886. doi:10.1517/14656566.2014.937706.
- Peters GJ, Noordhuis P, Van Kuilenburg AB et al. (2003). "Pharmacokinetics of S-1, an oral formulation of ftorafur, oxonic acid and 5-chloro-2,4-dihydroxypyridine (molar ratio 1:0.4:1) in patients with solid tumors". Cancer Chemother. Pharmacol. 52 (1): 1–12. PMID 12739060. doi:10.1007/s00280-003-0617-9.
- A. Klement (22 July 2013). "Dreier-Kombination gegen Magenkrebs: Teysuno". Österreichische Apothekerzeitung (in German) (15/2013): 23.
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