期刊
INFECTION AND DRUG RESISTANCE
卷 16, 期 -, 页码 217-224出版社
DOVE MEDICAL PRESS LTD
DOI: 10.2147/IDR.S390187
关键词
tuberculosis; sudapyridine; bedaquiline; antibacterial activity
This study evaluated the in vitro activity of WX-081 against clinical isolates of drug-resistant Mycobacterium tuberculosis (Mtb) and its intracellular bactericidal activity against a reference strain. WX-081 showed potent efficacy against the tested isolates, with 95.6% of strains having a minimum inhibitory concentration (MIC) of ≤0.25 μg/mL. The intracellular killing effect of WX-081 supports its potential efficacy in treating TB patients.
Background: Sudapyridine (WX-081) has exhibited equivalent efficacy than its counterpart parent drug bedaquiline (BDQ) but better safety profile against Mycobacterium tuberculosis (Mtb). Our study was aimed to evaluate in vitro activity of WX-081 against the clinical isolates of Mtb with different drug-resistance profiles and the intracellular bactericidal activity against the reference strain.Methods: The minimum inhibitory concentrations (MICs) of WX-081 and BDQ were tested against 114 Mtb clinical isolates. The intracellular activity of WX-081 and BDQ against the Mtb reference strain H37Rv in THP-1 cells was also evaluated in parallel.Results: The MICs for WX-081 of the enrolled isolates ranged from 0.0156 mu g/mL to 1 mu g/mL. The MIC50 and MIC90 of WX-081 were, respectively, 0.25 mu g/mL and 0.5 mu g/mL, with 95.6% of the enrolled strains having MICs <= 0.25 mu g/mL. For a given strain, the MIC value of WX-081 was generally equivalent to or 2-fold than MIC of BDQ. The intracellular bacterial killing was acquired with the tested drug concentrations that were presumed attainable during clinical usage.Conclusion: WX-081 exhibited potent efficacy against the clinical isolates in vitro. The intracellular killing effect of sudapyridine against the reference strain supports its potential efficacy in treating TB patients.
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