新药研发中基于转运体的药物-药物相互作用研究进展  

Research Progress of Transporter-Mediated Drug-Drug Interaction Studies in New Drug Development

作　　者：付淑军 夏滨 斯陆勤[2] 黄建耿[2] FU Shujun;XIA Bin;SI Luqin;HUANG Jiangeng(Center for Drug Evaluation,National Medical Products Administration,Beijing 100163,China;School of Pharmacy,Tongji Medical College,Huazhong University of Science and Technology,Wuhan 430030,China)

机构地区：[1]国家药品监督管理局药品审评中心,北京100163 [2]华中科技大学同济医学院药学院,武汉430030

出　　处：《医药导报》2025年第4期596-602,共7页Herald of Medicine

基　　金：国家自然科学基金资助项目(81773811);湖北省科技厅重点研发计划项目(2020BCB045);湖北省中医药管理局重点项目(ZY2023Z019)。

摘　　要：药物转运体种类众多,广泛分布于人体各组织器官,参与众多内源性物质、毒物和药物的膜转运。转运体介导的跨膜转运不仅在维持机体内环境稳态发挥重要作用,也与药物吸收、分布、代谢及排泄过程密切相关。临床上基于药物转运体的药物-药物/内源性分子相互作用可能影响药效或导致毒副作用。因此,在药物开发及上市进程中密切关注并评估在研药物基于转运体的药物相互作用风险,对药物在临床实践中的安全应用尤为重要。该文介绍了新药研发中常见药物转运体的分类、功能、组织分布、底物特异性等特征,综述美国食品药品监督管理局2023年批准上市的55种新药共涉及24种转运体的药物-药物相互作用研究进展并探讨其对新药研发的意义,以期为新药研发过程中药物-药物相互作用研究提供参考。There are a large number of drug transporters widely distributed in various tissues and organs in the human body.They are involved in the membrane transport of numerous endogenous substances,toxins,and drugs.The transmembrane transport mediated by transporters not only plays an important role in maintaining the homeostasis of the internal environment,but also closely related to drug absorption,distribution,metabolism,and excretion processes.In clinical practice,drug-drug and drug-endogenous molecule interactions based on drug transporters may affect therapeutic efficacy or lead to toxic side effects.Therefore,it is particularly important to closely monitor and evaluate the risks of transporters mediated drug-drug interactions in the drug development and marketing process.This review summarized the classification,functions,tissue distribution and substrate specificity of typical drug transporters in new drug development.Subsequently,the research progress regarding drug-drug interactions involving 24 drug transporters for 55 newly approved drugs by the US Food and Drug Administration in 2023 is comprehensively reviewed.The aim is to provide reference for further drug-drug interaction research together with its scientific significance during new drug development stage.

关 键 词：转运体 药物-药物相互作用 新药研发 

分 类 号：R969.2[医药卫生—药理学]