SLCO1B1基因多态性对甲氨蝶呤治疗的影响

SLCO1B1 polymorphism associated with methotrexate disposition and clinical outcome

有机阴离子转运多肽1B1(OATP1B1,编码基因SLCO1B1)在许多内源性物质和外源性药物的转运过程中发挥着重要的调控作用,其遗传多态性可改变药物的体内药代动力学特征,继而影响药物疗效和安全性。SLCO1B1多个基因位点的多态性(如rs4149056和rs2306283)对甲氨蝶呤的药代动力学和毒性有显著的影响。本文对此进行综述,以期为甲氨蝶呤的临床合理使用提供理论依据。

Organic anion transporting polypeptide 1B1 （ OATP1B1, en-coded by SLCO1B1 gene） plays a crucial role in the hepatic uptake of many endogenous compounds and xenobiotics.It has been demonstrated that SLCO1B1 polymorphism could change the pharmacokinetics charac-teristics of many clinically used drugs , which has influenced their out-come and safety.However , inter-individual variant of methotrexate re-sults in vastly different clinical effectiveness and toxicity.Herein, we re-view the current knowledge about this topic to provide theoretical guid-ance for the clinical use of methotrexate.