Pharmacokinetics and lipid-lowering efficacy affected by polymorphisms in genetic variability in statin therapy

HMG-CoA reductase inhibitors, commonly known as statins, are among the most widely prescribed and extensively studied drugs used in managing cardiovascular conditions by regulating lipid levels in the blood. Despite their broad use, there is considerable interindividual variability in therapeutic response. This heterogeneity may affect statin efficacy in lipid control and either increase the risk of adverse effects or reduce treatment benefits. Consequently, there is growing scientific interest in identifying genetic polymorphisms in enzymes and transporters involved in the pharmacokinetic pathways of statins. This review discusses clinically important genetic polymorphisms of statin metabolism and transport and their potential impact on treatment outcomes based on the patient’s genetic profile. Understanding these pharmacogenomic variations offers a translational opportunity to guide personalized statin therapy, optimize efficacy, and minimize adverse drug reactions.