Aim The aim of this study was to evaluate the pharmacogenetic variability in the disposition of felodipine in healthy Chinese subjects.Methods A single oral dose of 5 mg felodipine was orally administered to 45healthy Chinese subjects.The serum concentrations of felodipine were measured by using LC/MS/MS.We detected the SNPs of CYP450 enzymes and transporters, which play vital roles in drug metabolism and are with a high frequency of mutation in Chinese.Results The area under the plasma concentrationtime curve (AUC) within the time points 0 to 72 h (AUC (072)) after felodipine administration was significantly higher in the subjects possessing the CYP3A5 * 1/* 3 alleles than in those with the CYP3A5 * 1/* 1 alleles (P =0.021).The BCRP 421A allele was associated with a trend of reduced pharmacokinetic exposure (P =0.034).The mean Tmax in subjects with the CYP3A4 * 1/* 18B carriers was longer than in those with the CYP3A4 * 1/* 1.The pharmacokinetics characteristics of felodipine were not associated with other SNPs we investigated.Conclusion This study showed that the genetic polymorphisms of CYP3A5 * 3 and BCRPC421A might explain the variability in the pharmacokinetics of felodipine in the Chinese population.