基于尿苷二磷酸葡萄糖醛酸转移酶的抑制性药物相互作用的体外定量预测

Quantitative prediction of UGT-based inhibitory drug-drug interactions from in vitro information

尿苷二磷酸葡萄糖醛酸基转移酶(UDP-glucuronosyl-transferase,UGT)是一个结合酶超家族,催化了多种药物。已有许多与葡萄糖苷酸化相关的抑制性药物相互作用研究。体外实验方法和定量策略已经成功运用于体内葡萄糖醛酸化清除率以及抑制性药物相互作用的预测。该综述从这一领域相关基础知识和预测方法以及实验影响因素进行概述。

UDP-glucuronosyltransferase（UGT） is a family of conjugating enzymes that participate in the metabolism of many drugs.Inhibitory interactions involving glucuronidation have been described in a number of studies.Additionally,in vitro experimental approaches and scaling strategies have been successfully applied to the quantitative prediction of in vivo clearance via glucuronidation and inhibitory drug-drug interaction potential.In this overview,the methods,predictive models and newest advancement in this field have been summarized.