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新型酮内酯 RBx 14255 对艰难梭菌的体外和体内活性。

In vitro and in vivo activities of the novel Ketolide RBx 14255 against Clostridium difficile.

机构信息

Department of Infectious Diseases, New Drug Discovery Research, Ranbaxy Research Laboratories, Gurgaon, India.

出版信息

Antimicrob Agents Chemother. 2012 Nov;56(11):5986-9. doi: 10.1128/AAC.00015-12. Epub 2012 Aug 6.

DOI:10.1128/AAC.00015-12
PMID:22869573
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3486553/
Abstract

The MIC(90) of RBx 14255, a novel ketolide, against Clostridium difficile was 4 μg/ml (MIC range, 0.125 to 8 μg/ml), and this drug was found to be more potent than comparator drugs. An in vitro time-kill kinetics study of RBx 14255 showed time-dependent bacterial killing for C. difficile. Furthermore, in the hamster model of C. difficile infection, RBx 14255 demonstrated greater efficacy than metronidazole and vancomycin, making it a promising candidate for C. difficile treatment.

摘要

新型酮内酯 RBx 14255 对艰难梭菌的 MIC(90)为 4 μg/ml（MIC 范围为 0.125 至 8 μg/ml），该药物的活性强于对照药物。RBx 14255 的体外时间杀菌动力学研究显示，其对艰难梭菌具有时间依赖性杀菌作用。此外，在艰难梭菌感染的仓鼠模型中，RBx 14255 的疗效优于甲硝唑和万古霉素，使其成为艰难梭菌治疗的有希望的候选药物。

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