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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, gene SLCO1B1) plays an important regulatory role in the transport of many endogenous substances and exogenous drugs, and its genetic polymorphism can change the in vivo pharmacokinetic characteristics of the drug, Then affect the drug efficacy and safety. Polymorphisms at SLCO1B1 multiple loci (such as rs4149056 and rs2306283) have a significant effect on the pharmacokinetics and toxicity of methotrexate. This article reviews this, in order to provide a theoretical basis for the clinical rational use of methotrexate.