Song I S, Shin H J, Shim E J, Jung I S, Kim W Y, Shon J H, Shin J G
Department of Pharmacology and Pharmacogenomics Research Center, Inje University College of Medicine, Busan, Korea.
Clin Pharmacol Ther. 2008 Nov;84(5):559-62. doi: 10.1038/clpt.2008.61. Epub 2008 Apr 9.
Genetic variants of the organic cation transporter 2 (protein, OCT2; gene, SLC22A2) were evaluated for their contribution to the variations in the pharmacokinetics of metformin, especially to its renal elimination. Genetic variants of SLC22A2 (c.596C>T, c.602C>T, and c.808G>T) showed significant differences in metformin pharmacokinetics when compared with the reference genotype, with higher peak plasma concentration (C(max)) and area under the curve (AUC) and lower renal clearance (Cl(renal)), thereby suggesting that a decrease in transport function associated with the SLC22A2 variants results in reduced Cl(renal) of metformin and consequently leads to increased plasma concentrations.
对有机阳离子转运体2（蛋白质，OCT2；基因，SLC22A2）的基因变异体进行了评估，以确定它们对二甲双胍药代动力学变化的影响，尤其是对其肾脏清除的影响。与参考基因型相比，SLC22A2的基因变异体（c.596C>T、c.602C>T和c.808G>T）在二甲双胍药代动力学方面表现出显著差异，血浆峰浓度（C(max)）和曲线下面积（AUC）更高，肾脏清除率（Cl(renal)）更低，从而表明与SLC22A2变异体相关的转运功能降低导致二甲双胍的Cl(renal)降低，进而导致血浆浓度升高。
