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tegafur-gimeracil-oteracil
- Development stage
- Phase 3
- Lead developer
- Taiho Pharmaceutical
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Tegafur-gimeracil-oteracil is a fixed-dose oral combination chemotherapy primarily used for the treatment of advanced gastric cancer, often combined with cisplatin. It is also indicated for other cancers such as head and neck, colorectal, non–small-cell lung, breast, pancreatic, and biliary tract cancers. The drug consists of three components: * Tegafur (a prodrug of fluorouracil/5-FU) * Gimeracil (an inhibitor of dihydropyrimidine dehydrogenase to prevent 5-FU degradation) * Oteracil (which reduces gastrointestinal toxicity by inhibiting orotate phosphoribosyltransferase in the gut). Tegafur acts as an antimetabolite that interferes with DNA synthesis by mimicking pyrimidine bases; gimeracil increases systemic exposure to 5-FU; and oteracil limits local GI side effects. Developed by Taiho Pharmaceutical. It is administered orally and contraindicated during pregnancy.
- Brand names
- TeysunoTS-1TS1TS 1
- Other names
- tegafur/gimeracil/oteracil potassiumS 1S1S-1
02
Targets
DPYD (Dihydropyrimidine dehydrogenase)OPRT (Orotidine 5'-phosphate decarboxylase)TS (Thymidylate synthase)
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