Drug intelligence / Profile preview

gimeracil + oteracil potassium

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Gimeracil and oteracil potassium are components of an oral combination chemotherapy regimen most commonly used with tegafur (as in the product S-1 or Teysuno) for the treatment of advanced gastric cancer and other solid tumors. Gimeracil is a potent reversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for degrading 5-fluorouracil (5-FU), thereby increasing systemic exposure to 5-FU. Oteracil potassium inhibits orotate phosphoribosyltransferase (OPRT) in gastrointestinal tissues, reducing local activation of 5-FU and thus decreasing gastrointestinal toxicity. This combination is designed to enhance antitumor efficacy while minimizing side effects when administered with a fluoropyrimidine prodrug such as tegafur[6][8][9]. The primary indication is advanced gastric cancer in combination with cisplatin; it has also been studied or used off-label for colorectal, pancreatic, breast, esophageal, and cervical cancers[7][10].

Brand names
TeysunoS-1S1S 1TS-1TS1TS 1
Other names
gimeracil + oteracil potassium
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)OPRT (Orotidine 5'-phosphate decarboxylase)

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