According to the WHO, coronary artery disease (CAD) has become one of the greatest „killers“ of the modern world. Dyslipidemia, or elevated levels of total cholesterol, low-density lipoprotein (LDL), triglycerides (TG), or decreased levels of high density lipoprotein (HDL), is considered one of the critical factors for the development of CAD. Recently, statins have been the most widely prescribed drugs in the prevention and treatment of CAD and of ischemic stroke. Moreover, it is proved that they reduce morbidity and mortality by lowering LDL cholesterol levels in the blood plasma. On the other side, statins may cause many serious side effects, such as myopathy and rabdomyolysis. Moreover, as statins are used in the long-term therapy of chronic diseases, there is a high risk of side effects as a consequence of interactions with other drugs in polytherapy. Also, great interindividual differences were found in the reduction of LDL-cholesterol levels and in the incidence of ADR during statin therapy. There is a strong scientific evidence of the importance of OATP1B1 and BCRP membrane transporters in statin pharmacokinetics. Both transporters show significant genetic variability, and the frequency of polymorphisms SLCO1B1 521T>C and ABCG2 421C>A has great both population and racial variability. The variant allele SLCO1B1 521C is most common in the European (16 %), Asian (12 %) and African (1 %) population, while the ABCG2 421A variant allele is most common in Asians (30 %), followed by the white population (10 – 15 %), while it is the rarest in the African population (2 %). The results established in this study are accordant to the results obtained for other European, white populations. Gene polymorphisms are associated with variable kinetics, but also the susceptibility to the development of adverse drug reactions of the substrate, because variable activity in drug transport across barriers in the digestive system, liver-bile barrier, renal tubules in case of BCRP, and drug intake in the liver via OATP1B1 can significantly modulate the absorption, distribution and excretion of substrate drugs. Therefore, the analysis of SLCO1B1 and ABCG2 polymorphisms can serve to individualize and optimize statin treatment and minimize the risk of side effects, primarily myotoxicity and hepatotoxicity.