Despite statin therapy being effective in the primary and secondary prevention of coronary heart disease, the benefit of treatment varies between individuals. Interindividual variations in pharmacokinetics play a central role in the cause of variability of drug disposition, and, in turn, the drug's clinical efficacy. Exploring genetic variations that influence pharmacokinetics may lead clinicians to apply the most efficient and safe drug therapy. So far, variants in eight candidate genes related to pharmacokinetics of statins have been investigated as the potential determinant of drug responsiveness or adverse event risk. All reported data remains inconclusive, but it has been suggested that combined analysis of more than two different polymorphisms, or a combination of genetic association and studies using in vitro recombinant expression techniques, may be more informative in predicting the specific phenotype of a genetic variant. Future studies using these approaches could provide more striking evidence, which may be sufficient to justify genetic analysis regarding pharmacokinetic variants in the clinical practice of statin therapy.