利奈唑啉
基岩
肺结核
结核分枝杆菌
微生物学
体内
药理学
体外
抗生素
医学
生物
细菌
金黄色葡萄球菌
生物化学
病理
遗传学
万古霉素
作者
Deepak Almeida,Si-Yang Li,Jin Liu,Barry Hafkin,Khisimuzi Mdluli,Nader Fotouhi,Eric Nuermberger
摘要
ABSTRACT Contezolid is a new oxazolidinone with in vitro and in vivo activity against Mycobacterium tuberculosis comparable to that of linezolid. Pre-clinical and clinical safety studies suggest it may be less toxic than linezolid, making contezolid a potential candidate to replace linezolid in the treatment of drug-resistant tuberculosis. We evaluated the dose-ranging activity of contezolid, alone and in combination with bedaquiline and pretomanid, and compared it with linezolid at similar doses, in an established BALB/c mouse model of tuberculosis. Contezolid had an MIC of 1 µg/mL, similar to linezolid, and exhibited similar bactericidal activity in mice. Contezolid-resistant mutants selected in vitro had 32- to 64-fold increases in contezolid MIC and harbored mutations in the mce3R gene. These mutants did not display cross-resistance to linezolid. Our results indicate that contezolid has the potential to replace linezolid in regimens containing bedaquiline and pretomanid and likely other regimens.
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