Objective Statins are the most commonly prescribed drugs for Atherosclerotic cardiovascular disease worldwide and long-term medication is necessary for patients at high risk of cardiovascular events.However, the correlation of their pharmacokinetic characteristics and drug safety is limited.So there is an urgent need to further understanding and exploring of the contribution of pharmacokinetics factors on drug safety and tolerance in order to promote TDM strategies and guide treatment with statins.Methods We collected and analyzed reference information on individualized statins therapy based on the new guidelines for the treatment ofhypercholesterolemia announced by AHA/ACC in 2013, and clinical instructions of statins, including simvastatin, lovastatin, atorvastatin, pravastatin, rosuvastatin, fluvastatin and pitavastatin, as well as searching on MEDLINE and PubMed using the term "statins, safety, pharmacokinetics" and screening materials up to February 2013 in high correlation.Results Changes in the drug exposure increase the risk of side effects, especially muscle and kidney-related adverse events.In addition, statins metabolism and transport in the liver are significantly affected by genetic factors, such as gene polymorphism of CYP3A4 enzyme and OATP 1B 1 transporter protein.Considering the great individual differences in pharmacokinetics and the complication in risk factors for adverse events, individualized statins therapy possesses great potential.Conclusions TDM should be applied in statins treatment.The basic TDM strategy is that considering the recommended dose, CYP3A4 and OATP1B1 polymorphisms, and drug combination, which are the three main factors, the specific initial dose could be determined.Continuous plasma sampling for drug concentration analysis after administration at steady state should be taken into account to adjust drug exposure level.As a result, other two studies are needed for implementing TDM.One is the medication based on the correlation between plasma concentration (Ct) at sampling point and drug exposure (AUC).The other is the relationship between drug exposure and clinical efficacy, which determines the therapeutic window.