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本文介绍了药物转运体在药物排泄过程中的作用,探讨了其在新药研发和临床应用中的可能性.通过对药物转运体功能的了解和利用,可以开发出对某些器官有靶向性的药物,或避免药物分布到某些器官中,从而提高药物的疗效,降低其毒副作用;也可以通过对转运体介导的药物相互作用及肝肠循环的研究,指导临床更加安全有效的用药.在药物研发的初始阶段,就开始重视其药动学特性,这一观念近年来已被很多人所接受.对药物转运体的深入认识和利用,建立高通量的药物转运体筛选体系,对于加速新药研发的进程将具有极其重要的意义.“,”This review is mainly concerned about the effects of drug transporters on drug excretion and the possibility in the development and clinical application of new drugs. The understanding of the properties of transporters enables us to develop novel drugs, which can increase the site-directional drug delivery, or avoid the distribution to other organs, thereby increase the therapeutic effects and reduce the chance of toxic effects. Furthermore, the research of drug transporter-mediated drug-drug interactions and enterohepat-ic cycle, is able to guide us a more reasonable, safe and effective clinical medication. It is well accepted in recent years that the pharmacokinetic properties of a new drug should be studied in its early stage of development. Additionally, high-through screening system established on transporters is bound to be an effective tool to accelerate the development of new drugs.