Department of Medicine and Therapeutics, The Chinese University of Hong Kong, Prince of Wales Hospital, Shatin, Hong Kong.
Clin Pharmacol Ther. 2010 May;87(5):558-62. doi: 10.1038/clpt.2009.232. Epub 2010 Feb 3.
The ATP-binding cassette G2 (ABCG2) c.421C>A (rs2231142) polymorphism influences the pharmacokinetics of rosuvastatin. We examined whether this polymorphism influences the low-density lipoprotein cholesterol (LDL-C)-lowering efficacy of the drug. In 305 Chinese patients with hypercholesterolemia who were treated with rosuvastatin at a dosage of 10 mg daily, the c.421A variant was found to be significantly associated with greater reduction in LDL-C level, in a gene-dose-dependent manner. As compared with subjects with the c.421CC genotype, those with the c.421AA genotype showed a 6.9% greater reduction in LDL-C level, which would be equivalent to the effect obtained by doubling the dose of rosuvastatin.
三磷酸腺苷结合盒转运蛋白 G2（ABCG2）c.421C＞A（rs2231142）多态性影响瑞舒伐他汀的药代动力学。我们研究了这种多态性是否影响药物的降低低密度脂蛋白胆固醇（LDL-C）的功效。在 305 名接受每日 10 毫克瑞舒伐他汀治疗的中国高胆固醇血症患者中，发现 c.421A 变异与 LDL-C 水平的降低呈基因剂量依赖性显著相关。与 c.421CC 基因型的受试者相比，c.421AA 基因型的受试者 LDL-C 水平降低了 6.9%，相当于将瑞舒伐他汀的剂量增加一倍所获得的效果。
