| Stereochemistry | ACHIRAL |
| Molecular Formula | C5H4ClNO2 |
| Molecular Weight | 145.544 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC1=CC(=O)NC=C1Cl
InChI
InChIKey=ZPLQIPFOCGIIHV-UHFFFAOYSA-N
InChI=1S/C5H4ClNO2/c6-3-2-7-5(9)1-4(3)8/h1-2H,(H2,7,8,9)
Gimeracil is a component of an oral fixed combination known under the name Teysuno or S-1 (tegafur, gimeracil and oteracil potassium at a molar ratio of 1:0.4:1). The formulation was approved in Asia and Europe for the treatment of a rare condition of gastric cancer. Given in combination, gimeracil enhances the efficacy of tegafur by inhibiting dihydropyrimidine dehydrogenase, an enzyme involved in metabolism of tegafur and its active metabolite 5-fluorouracil.
CNS Activity
Originator
Approval Year
Doses
AEs
Sample Use Guides
The recommended dose of gimeracil is 10 mg/m2 (as a part of oral combination consisting of tegafur, gimeracil and oteracil potassium at a molar ratio of 1:0.4:1) twice a day, for 21 consecutive days followed by 7 days rest.
Route of Administration:
Oral
TE-5 and TE-5R cells were plated in a 96-well plate and cultured for 24 h, and then they were treated with the indicated concentrations of 5-FU in the presence of gimeracil for 72 h at a molar ratio of 1:0.2 (5-FU:gimeracil). IC50 values with and without gimeracil in TE-5 cells were 4.9 and 4.8 uM, respectively, and those in TE-5R cells were 20.8 and 59.0 uM, respectively.
ACTIVE MOIETY
