Tegafur / Gimeracil / Oteracil — Investigational Agent
Other · Approved Abroad / Investigational in US · Taiho Pharmaceutical
Mechanism of Action
Oral fluoropyrimidine combination of three agents in a fixed molar ratio: tegafur, a prodrug converted in vivo to 5-fluorouracil (5-FU); gimeracil (CDHP), a reversible inhibitor of dihydropyrimidine dehydrogenase (DPD) that blocks 5-FU degradation to prolong therapeutic plasma 5-FU levels; and oteracil (potassium oxonate), which localizes in the GI mucosa and inhibits orotate phosphoribosyltransferase to reduce 5-FU phosphorylation in the gut, mitigating gastrointestinal toxicity. The resulting active 5-FU exerts cytotoxicity via thymidylate synthase inhibition and incorporation into RNA/DNA.
Investigational Indications
- Advanced/metastatic gastric cancer (with cisplatin)
- Adjuvant therapy of resected gastric cancer
- Pancreatic cancer
- Colorectal cancer
- Head and neck cancer
- Biliary tract cancer