TS-1 (Tegafur, Gimeracil, Oteracil Potassium) Distributor
An orally bioavailable fluoropyrimidine antagonist composed of tegafur combined with two modulators of 5-flurouracil (5-FU) activity, 5-chloro-2,4-dihydroxypyridine (CDHP) and potassium oxonate, in a molar ratio of 1:0.4:1. Tegafur is a prodrug of 5-fluorouracil, an antimetabolite that inhibits thymidylate synthase, DNA synthesis and cell division, and competes with uridine triphosphate, thus inhibiting RNA and protein synthesis. CDHP is a reversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the liver enzyme responsible for rapid catabolism of 5-FU into inactive metabolites. Potassium oxonate preferentially localizes in the gut and inhibits the enzyme orotate phosphoribosyl-transferase (OPRT), thereby decreasing activation of 5-FU in the gut and activated 5-FU-related gastrointestinal toxicity.
TS-1 is the world’s first anticancer agent in orally disintegrating tablet form that can be ingested without water since it quickly disintegrates upon contact with saliva in the mouth. The drug was developed in order to meet the needs of the many patients who have difficulty swallowing capsules or whose water intake is being restricted. The tablets are dry-coated to contain the active ingredients of the anticancer agent in the inner core, coated with an outer shell. The coating has the dual purpose of preventing the active ingredients from leaking out before administration while allowing quick disintegration in the mouth. Together with existing capsules and granulated formulation, the addition of OD tablets gives three options that can be chosen in accordance with each patient’s needs.
Gastric cancer, colorectal cancer, head and neck cancers, non-small-cell lung cancer, inoperable or recurrent breast cancer, pancreatic cancer, and biliary tract cancer.
