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Background  The genetic variation underlying atorvastatin (ATV) pharmacokinetics was evaluated in a Mexican population. Aims of this study were: 1) to reveal the frequency of 87 polymorphisms in 36 genes related to drug metabolism in healthy Mexican volunteers, 2) to evaluate the impact of these polymorphisms on ATV pharmacokinetics, 3) to classify the ATV metabolic phenotypes of healthy volunteers, and 4) to investigate a possible association between genotypes and metabolizer phenotypes.    Methods  A pharmacokinetic study of ATV (single 80-mg dose) was conducted in 60 healthy male volunteers. ATV plasma concentrations were measured by high-performance liquid chromatography mass spectrometry. Pharmacokinetic parameters were calculated by the non-compartmental method. The polymorphisms were determined with the PHARMAchip® microarray and the TaqMan® probes genotyping assay.    Results  Three metabolic phenotypes were found in our population: slow, normal, and rapid. Six gene polymorphisms were found to have a significant effect on ATV pharmacokinetics:  MTHFR  (rs1801133),  DRD3  (rs6280),  GSTM3  (rs1799735),  TNFα  (rs1800629),  MDR1  (rs1045642), and  SLCO1B1  (rs4149056). The combination of  MTHFR ,  DRD3  and  MDR1  polymorphisms associated with a slow ATV metabolizer phenotype.    Conclusion  Further studies using a genetic preselection method and a larger population are needed to confirm these polymorphisms as predictive biomarkers for ATV slow metabolizers.    Trial registration  Australian New Zealand Clinical Trials Registry:  ACTRN12614000851662 , date registered: August 8, 2014.    Electronic supplementary material  The online version of this article (doi:10.1186/s12885-016-2062-2) contains supplementary material, which is available to authorized users.

A pharmacogenetic pilot study reveals MTHFR, DRD3, and MDR1 polymorphisms as biomarker candidates for slow atorvastatin metabolizers