Abstract：
Gepotidacin (GSK2140944) is a novel, bactericidal, first in class triazaacenaphthylene bacterial type II topoisomerase inhibitor in development for the treatment of uncomplicated urinary tract infections and gonorrhea. The performance of several antimicrobial susceptibility methods (broth microdilution, gradient diffusion, and disk diffusion) for gepotidacin were evaluated using over 5800 recent Escherichia coli and Staphylococcus saprophyticus clinical isolates. Reference broth microdilution gepotidacin MICs showed an essential agreement of 95.9 % and 98.1 % with MICs by gradient diffusion for E. coli and S. saprophyticus isolates, respectively. Gepotidacin susceptibility using disks produced by 2 manufacturers had good agreement with an R2 values of 0.95 and 99.2 % of overall zone diameters agreeing within 3 mm. A correlation with an overall R2 value of 0.72 between MICs by broth microdilution and zone diameters by disk diffusion was observed. This data should assist in the clinical development of gepotidacin and provide reliable susceptibility methods to evaluate its activity.
摘要：
Gepotidacin(GSK2140944)是一种新型的,杀菌,一类三氮杂萘并二烯类细菌II型拓扑异构酶抑制剂正在开发中，用于治疗无并发症的尿路感染和淋病。几种抗菌敏感性方法的性能(肉汤微量稀释，梯度扩散,和圆盘扩散）使用5800多个最近的大肠杆菌和腐生葡萄球菌临床分离株对gapotidacin进行了评估。参考肉汤微量稀释gepotidacinMIC通过梯度扩散对大肠杆菌和腐生链球菌分离株的MIC显示出95.9%和98.1%的基本一致性，分别。使用由2个制造商生产的圆盘对地皮沙星的敏感性具有良好的一致性，R2值为0.95，总区域直径的99.2％在3mm以内。观察到通过肉汤微量稀释的MIC与通过圆盘扩散的区域直径之间的总R2值为0.72的相关性。这些数据应有助于吉泊地星的临床开发，并提供可靠的药敏方法来评估其活性。
