Telacebec Inhibitor of cytochrome bc1 complex cytochrome b subunit (QcrB) Treatment of tuberculosis Treatment of M. ulcerans infection (Buruli ulcer)

被引:0
|
作者
Saxena, D. [1 ]
Kaul, G. [1 ]
Dasgupta, A. [1 ]
Chopra, S. [1 ]
机构
[1] CSIR Cent Drug Res Inst, Div Microbiol, Sect 10,Sitapur Rd, Lucknow 226031, Uttar Pradesh, India
关键词
Telacebec; Q-203; QcrB; Tuberculosis; Buruli ulcer; CLINICAL CANDIDATE; Q203; ANALOGS; ARYL;
D O I
10.1358/dof.2021.46.5.3235210
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Tuberculosis is a contagious infectious disease caused by Mycobacterium tuberculosis and is one of the biggest causes of significant morbidity and mortality worldwide. A very long treatment protocol and poor patient compliance among other reasons have resulted in the rapid emergence of drug-resistant tuberculosis, which is resistant to all therapeutic options. In this context, new compounds with novel mechanisms of action are an urgent unmet medical need. Telacebec (Q-203) is an orally bioavailable imidazo[1,2-a]pyridine amide that is being developed by Qurient Co., Ltd. and is currently in a phase II trial for the treatment of tuberculosis. Telacebec displayed strong potency against M. tuberculosis by targeting cytochrome bc(1) complex of bacterial respiratory chain. The drug has displayed activity against both extracellular and intracellular M. tuberculosis as well as a good safety and pharmacokinetic profile. Additionally, it has successfully completed 2 phase I and 1 phase II clinical trials and is considered safe with no severe adverse events. Telacebec has received orphan drug designation and fast track designation from the U.S. Food and Drug Administration.
引用
收藏
页码:371 / 381
页数:11
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