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地拉米定(OPC-67683)用于治疗耐多药结核病。

Delamanid (OPC-67683) for treatment of multi-drug-resistant tuberculosis.

作者信息

Sotgiu Giovanni, Pontali Emanuele, Centis Rosella, D'Ambrosio Lia, Migliori Giovanni Battista

机构信息

Clinical Epidemiology and Medical Statistics Unit, Department of Biomedical Sciences - University of Sassari, - Research, Medical Education and Professional Development Unit, AOU Sassari, Italy.

出版信息

Expert Rev Anti Infect Ther. 2015 Mar;13(3):305-15. doi: 10.1586/14787210.2015.1011127. Epub 2015 Feb 3.

Abstract

The research and development of delamanid was carried out by Otsuka Pharmaceutical Development and Commercialization (Osaka, Tokyo, Japan). It belongs to the group of nitroimidazoles. It inhibits the synthesis of mycolic acids, crucial component of the cell wall of the Mycobacterium tuberculosis complex. It is insoluble in water and its activity was proven in several in vitro and in vivo studies. Its market approval was obtained in April 2014 in Europe. Its bactericidal activity was demonstrated in individuals with drug-susceptible and drug-resistant tuberculosis (MDR- and XDR-TB). The safety and tolerability profile was good; the notified increased QT interval was not clinically relevant. It was approved for adults but ongoing clinical trials and clinical experiences have been proving its efficacy in the pediatric population.

摘要

地拉米啶由大冢制药开发与商业化公司(日本东京大阪)研发。它属于硝基咪唑类。它抑制分枝菌酸的合成,而分枝菌酸是结核分枝杆菌复合群细胞壁的关键组成部分。它不溶于水,并且其活性已在多项体外和体内研究中得到证实。2014年4月它在欧洲获得市场批准。其杀菌活性在药物敏感和耐药结核病(耐多药结核病和广泛耐药结核病)患者中得到了证实。安全性和耐受性良好;报告的QT间期延长在临床上并无关联。它已被批准用于成人,但正在进行的临床试验和临床经验已证明其在儿科人群中的疗效。

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