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霉酚酸是器官移植和自身免疫性疾病治疗中常用的免疫抑制药,其药效学、药动学及毒性存在明显个体差异,原因包括遗传和非遗传因素,其中基因多态性是重要原因之一。检索近20年关于霉酚酸相关基因多态性的临床研究,选择其中样本量较大的随机对照试验和队列研究,综述霉酚酸相关基因多态性对其药动学和药效学的影响,对霉酚酸临床个体化给药方案的设计、药物疗效的提高和毒性的降低具有参考意义。基因多态性通过影响尿苷二磷酸葡萄糖醛酸基转移酶、多药耐药相关蛋白2、有机阴离子转运多肽和次黄嘌呤单核苷酸脱氢酶的活性,进而可能影响霉酚酸药物代谢、疗效及毒性。
Mycophenolic acid, a commonly used immunosuppressive drug used in the treatment of organ transplant and autoimmune diseases, has significant individual differences in pharmacodynamics, pharmacokinetics and toxicity due to genetic and non-genetic factors, of which genetic polymorphisms are important one. To search for the clinical research on mycophenolic acid-related gene polymorphism in recent 20 years, select randomized controlled trials and cohorts of large sample size to review the mycophenolic acid-related gene polymorphism on its pharmacokinetics and pharmacodynamics Impact on the mycophenolic acid clinical individualized dosing regimen design, improve the efficacy of drugs and reduce toxicity has reference value. Genetic polymorphisms affect the activity of uridine diphosphate glucuronyltransferase, multidrug resistance-associated protein 2, organic anion transport polypeptide and hypoxanthine mononucleotide dehydrogenase, which may in turn affect mycophenolic acid drug Metabolism, Efficacy and Toxicity.