CYP2C19 681G > A polymorphism and pharmacokinetics of clopidogrel in Chinese healthy volunteers

The aim of this study was to investigate the contribution of the most frequent single nucleotide polymorphism of CYP2C19 681G >A to the pharmacokinetics of clopidogrel in 20 healthy Chinese volunteers after administration of a single dose of clopidogrel 75 mg. The peak plasma concentration (C _max) was higher in the 681GA + 681AA group than that in the 681GG group (1.93 ± 1.77 vs. 1.65 ± 1.56 ng/mL, P= 0.613). The area under the curve to the last measurable concentration (AUC0-36 ) and area under the curve extrapolated to infinity (AUC _0-∞) of clopidogrel were lower in the 681GG group than that in the 681GA + 681AA group (2.25 ± 1.64 vs. 2.64 ± 1.69 ng h/mL, P= 0.465; 2.26 ± 1.65 vs. 2.67 ± 1.71 ng h/mL, P= 0.455) respectively. The oral clearance (Cl/F) was lower in the 681GA + 681AA group than that in the 681GG group (51.96 ± 36.13 vs. 54.47 ± 35.21 × 10 ³ L/h, P= 0.829). The genetic polymorphism of CYP2C19 681G > A does not cause significant alterations in the pharmacokinetics of clopidogrel at a clinically relevant therapeutic dose in healthy Chinese volunteers.