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

ABSTRACTIntroduction: Statins are used in the treatment of dyslipidemia promoting primary and secondary prevention against detrimental cardiovascular events. ATP-binding cassette (ABC) and solute carrier (SLC) membrane transporters transport statins across the cell membrane. Differences in drug transporter tissue expression and activity contribute to variability in statin pharmacokinetics (PK) and response.Areas covered: The purpose of this review is to discuss factors impacting transporter expression and the effect this has on statin efficacy and safety. Previous studies have demonstrated that genetic polymorphisms, drug–drug interactions (DDI), nuclear receptors, and microRNAs affect statin PK and pharmacodynamics.Expert opinion: Genetic variants of ABCG2 and SLCO1B1 transporters affect statin PK 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...