Influence of CYP3A and CYP2C19 genetic polymorphisms on the pharmacokinetics of cilostazol in healthy subjects.
The objective of this study was to investigate the influence of genetic polymorphisms in the CYP3A and CYP2C19 genes on cilostazol pharmacokinetics, with the drug being administered orally as a 50-mg single dose in healthy subjects. CYP2C19 genotypes in individuals with the CYP3A5*3/*3 genotype were associated with statistically significant differences (P < 0.05) in cilostazol pharmacokinetics parameters (apparent oral clearance (CL/F) and terminal half-life (t(1/2))). This indicates that CYP2C19 polymorphisms play an important role in the metabolism of cilostazol only in individuals with the CYP3A5*3/*3 genotype, which has low metabolic activity.
Yoo
H-D
HD
College of Pharmacy and Institute of Bioequivalence and Bridging Study, Chonnam National University, Gwangju, Korea.
Park
S-A
SA
Cho
H-Y
HY
Lee
Y-B
YB
D000328:Adult; D019540:Area Under Curve; D001189:Aryl Hydrocarbon Hydroxylases / Q000235:genetics*; D000077407:Cilostazol; D065731:Cytochrome P-450 CYP2C19; D051544:Cytochrome P-450 CYP3A / Q000235:genetics*; D005787:Gene Frequency; D005838:Genotype; D006207:Half-Life; D006801:Humans; D007723:Korea / Q000453:epidemiology; D008297:Male; D010975:Platelet Aggregation Inhibitors / Q000493:pharmacokinetics*; D011110:Polymorphism, Genetic / Q000235:genetics; D013777:Tetrazoles / Q000493:pharmacokinetics*; D014665:Vasodilator Agents / Q000493:pharmacokinetics*; D055815:Young Adult
D010975:Platelet Aggregation Inhibitors; D013777:Tetrazoles; D014665:Vasodilator Agents; D001189:Aryl Hydrocarbon Hydroxylases; C045793:CYP2C19 protein, human; D065731:Cytochrome P-450 CYP2C19; D051544:Cytochrome P-450 CYP3A; D000077407:Cilostazol