The First Affiliated Hospital, Clinical Pharmacology Research Center, Hengyang Medical School, University of South China, Hengyang, Hunan, China.
The First Affiliated Hospital, Hengyang Key Laboratory of Clinical Pharmacology, School of Pharmaceutical Science, Hengyang Medical School, University of South China, Hengyang, Hunan, China.
Expert Rev Clin Pharmacol. 2022 Sep;15(9):1107-1117. doi: 10.1080/17512433.2022.2118714. Epub 2022 Sep 5.
Metformin has been recognized as the first-choice drug for type 2 diabetes mellitus (T2DM). The potency of metformin in the treatment of type 2 diabetes has always been in the spotlight and shown significant individual differences. Based on previous studies, the efficacy of metformin is related to the single-nucleotide polymorphisms of transporter genes carried by patients, amongst which a variety of gene polymorphisms of transporter and target protein genes affect the effectiveness and adverse repercussion of metformin.
Here, we reviewed the current knowledge about gene polymorphisms impacting metformin efficacy based on transporter and drug target proteins.
The reason for the difference in clinical drug potency of metformin can be attributed to the gene polymorphism of drug transporters and drug target proteins in the human body. Substantial evidence shows that genetic polymorphisms in transporters such as organic cation transporter 1 (OCT1) and organic cation transporter 2 (OCT2) affect the glucose-lowering effectiveness of metformin. However, optimization of individualized dosing regimens of metformin is necessary to clarify the role of several polymorphisms.
二甲双胍已被认为是治疗 2 型糖尿病（T2DM）的首选药物。二甲双胍在治疗 2 型糖尿病方面的疗效一直备受关注，并表现出显著的个体差异。基于以往的研究，二甲双胍的疗效与患者携带的转运体基因的单核苷酸多态性有关，其中多种转运体和靶蛋白基因的基因多态性影响着二甲双胍的疗效和不良影响。
本文综述了基于转运体和药物靶蛋白的基因多态性对二甲双胍疗效影响的最新知识。
二甲双胍临床药物效力差异的原因可能归因于人体药物转运体和药物靶蛋白的基因多态性。大量证据表明，有机阳离子转运体 1（OCT1）和有机阳离子转运体 2（OCT2）等转运体的基因多态性影响着二甲双胍的降糖效果。然而，为了阐明几种多态性的作用，有必要优化个体化的二甲双胍给药方案。
