gimeracil

Gimeracil is a small molecule enzyme inhibitor used as an adjunct in antineoplastic therapy. Its primary role is to inhibit the enzyme dihydropyrimidine dehydrogenase (DPD), which is responsible for the degradation of fluorouracil (5-FU). By blocking DPD reversibly, gimeracil increases and prolongs systemic exposure to 5-FU when administered as part of oral chemotherapy regimens such as Teysuno or TS-1. This enhances the cytotoxic effect against cancer cells by maintaining higher concentrations of active drug. Gimeracil itself does not have direct antitumor activity but potentiates the efficacy and duration of action for fluoropyrimidine-based chemotherapies[1][2][3][6].

Brand names

Gimeracil (as an ingredient, not a standalone brand)Teysuno (as part of combination)TS-1 (as part of combination)S-1 (as part of combination)

Other names

5-chloro-2,4-dihydroxypyridine5-chloro-4-hydroxy-2(1H)-pyridinonegimestat5-chloro-pyridine 2,4-diolGIMERACIL [INN]GIMERACIL [JAN]