The effect of CYP3A41G allele on the pharmacokinetics of atorvastatin in Chinese han patients with coronary heart disease

The present study aimed to evaluate the impact of CYP3A4*1G allele on the pharmacokinetics of atorvastatin in the Chinese Han patients with coronary heart disease (CHD). Twenty male patients of CHD with different CYP3A4*1G genotypes were orally administered a single 20 mg dose of atorvastatin. Plasma concentrations of atorvastatin and 2‐hydroxyatorvastatin were measured by high‐performance liquid chromatography tandem mass spectrometry. The mean area under the plasma concentration–time curve from 0 to infinity (AUC0–∞) of atorvastatin in subjects with the CYP3A4*1G/*1G genotype were 36% or 25% lower than in those with the wild‐type or the *1/*1G genotype, respectively. The time to peak plasma concentration (Tmax) and oral clearance of atorvastatin (CL/F) were significantly different between subjects with the CYP3A4*1G/*1G genotype and the wild‐type. The AUC0–∞ for 2‐hydroxyatorvastatin in subjects with the CYP3A4*1G/*1G genotype was 44% or 31% lower than in those with the wild‐type or the *1/*1G genotype, respectively. The peak plasma concentration, Tmax and apparent clearance of 2‐hydroxyatorvastatin (CL/Fm) were significantly different between subjects with the CYP3A4*1G/*1G genotype and the wild‐type. This study indicates that the CYP3A4*1G allele is associated with the pharmacokinetics of atorvastatin and its metabolites in those Chinese Han patients with CHD after a single oral dose.