The Chinese University of Hong Kong, Prince of Wales Hospital, Department of Medicine and Therapeutics, Shatin, Hong Kong SAR.
Expert Opin Drug Metab Toxicol. 2011 Jan;7(1):49-62. doi: 10.1517/17425255.2011.538383. Epub 2010 Nov 23.
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.
We review and evaluate the associations of the ABCG2 polymorphism on the pharmacokinetics and clinical efficacy of statins.
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.
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.
ABCG2 外排转运体在多种组织中表达，在许多他汀类药物的处置中发挥重要作用。ABCG2 中降低转运体活性的功能性 421C>A 多态性已被发现与某些他汀类药物的全身暴露增加有关。
我们综述和评估了 ABCG2 多态性对他汀类药物药代动力学和临床疗效的影响。
本文详细介绍了 ABCG2 转运体，并广泛综述了其与他汀类药物的药代动力学和降脂作用的关系。本综述还讨论了 ABCG2 多态性在他汀类药物治疗患者的临床结局和他汀类药物相互作用中的潜在作用。
ABCG2 421C>A 多态性对他汀类药物处置的影响因不同药物而异，在 rosuvastatin 中比其他他汀类药物对全身暴露的影响更大。这种遗传变异与中国和高加索患者对 rosuvastatin 的低密度脂蛋白胆固醇反应增加有关。ABCG2 421C>A 多态性对其他底物他汀类药物的脂质反应和临床结局的影响需要在未来的研究中进行评估。
