Importance of the field: The ABCG2 efflux transporter is expressed in multiple tissues and plays an important role in the disposition of many statins. The functional 421C>A polymorphism in ABCG2 that reduces transporter activity has been found to be associated with increased systemic exposures to certain statins.
Areas covered in this review: We review and evaluate the associations of the ABCG2 polymorphism on the pharmacokinetics and clinical efficacy of statins.
What the reader will gain: This article gives a detailed overview of the ABCG2 transporter and extensively reviews its relations with the pharmacokinetics and lipid-lowering effects of statins. This review also discusses the potential role of the ABCG2 polymorphism in the clinical outcomes in statin-treated patients and statin-drug interactions.
Take home message: The impact of the ABCG2 421C>A polymorphism on the disposition of the statins varies between different drugs and the effect on systemic exposure was greater in the case of rosuvastatin than other statins. This genetic variant was associated with greater low-density lipoprotein cholesterol response to rosuvastatin in Chinese and caucasian patients. The effect of the ABCG2 421C>A polymorphism on the lipid response to other substrate statins and clinical outcomes need to be evaluated in future studies.