An update on efflux and uptake transporters as determinants of statin response

ABSTRACTIntroduction: Statinsare used in the treatment of dyslipidemiapromoting primary and secondary prevention against detrimental cardiovascular events. ATP-binding cassette (ABC) and solute carrier (SLC) membrane transporterstransport statinsacross the cell membrane. Differences in drug transporter tissue expression and activity contribute to variability in statinpharmacokinetics (PK) and response.Areas covered: The purpose of this review is to discuss factors impacting transporter expression and the effect this has on statinefficacy and safety. Previous studies have demonstrated that genetic polymorphisms, drug–drug interactions(DDI), nuclear receptors, and microRNAs affect statinPK and pharmacodynamics.Expert opinion: Genetic variants of ABCG2and SLCO1B1transporters affect statinPK and, as a result, the intended lipid-lowering response. However, the effect size is small, limiting its applicability in clinical practice. Furthermore, genetic variants do not totally explain the observed inte...