An update on efflux and uptake transporters as determinants of statin response
2018
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...
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