抗结核药物研究进展  

Research progress on anti-tubercular drugs

作　　者：朱子豪 张文轩 李天磊 吴松 ZHU Zi-hao;ZHANG Wen-xuan;LI Tian-lei;WU Song(State Key Laboratory of Bioactive Substance and Function of Natural Medicines,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China;State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medicinal University,Guiyang 550025,China)

机构地区：[1]中国医学科学院、北京协和医学院药物研究所,天然药物活性物质与功能国家重点实验室,北京100050 [2]贵州医科大学,省部共建药用植物功效与利用国家重点实验室,贵州贵阳550025

出　　处：《药学学报》2022年第4期892-902,共11页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81703364);贵州医科大学省部共建药用植物功效与利用国家重点实验室2019年开放课题项目(FAMP201903K);贵州省科技基金项目(黔科合平台人才[2017] 5101);中国医学科学院医学与健康科技创新工程重大协同创新项目(2021-I2M-1-069)。

摘　　要：全球结核病耐药性形势日益严峻,结核病尤其是耐多药结核病(multidrug-resistant tuberculosis, MDR-TB)的临床治疗面临着严峻的挑战。自2012年至今,已经有3个抗结核的新化药上市,并有23个新化学实体药物处于临床试验阶段,其中有4个新药由中国研发,分别为TBI-223、吡法齐明(TBI-166)、澳利莫迪(aulimanid)和WX-081。本文针对近年来被批准上市和正在临床试验的新化学实体按照临床研究阶段进行分类,分别从作用机制、体内外药理活性研究、药代动力学及临床研究等角度论述当前研究进展,希望为后续抗结核药物研发提供参考。Tuberculosis(TB) is an enduring threat to global health. The epidemic persists with growing drug resistance, especially for extensively drug-resistant TB. Therefore, the treatment for TB and its associated multidrug resistance has been an ongoing challenge. Due to the greater attention and investment in the elimination of this disease, significant progress has been achieved. Bedaquiline, delamanid, and pretomanid have been approved for the clinical use. In addition, two dozens new anti-TB drugs are currently in clinical testing. China has contributed four new drugs TBI-223, TBI-166, aulimanid, and WX-081. The aim of this review is to summarize the recent advances in anti-TB drug development. Based on the different clinical stages of these anti-TB drugs, we mainly focus on mechanism of action, in vitro and in vivo pharmacological studies, pharmacokinetics and clinical studies.

关 键 词：抗结核药物 新化学实体 新药研究 临床阶段 多药耐药结核 

分 类 号：R966[医药卫生—药理学]