Biedenbach D J, Bouchillon S K, Hackel M, Miller L A, Scangarella-Oman N E, Jakielaszek C, Sahm D F
International Health Management Associates, Inc., Schaumburg, Illinois, USA
International Health Management Associates, Inc., Schaumburg, Illinois, USA.
Antimicrob Agents Chemother. 2016 Jan 4;60(3):1918-23. doi: 10.1128/AAC.02820-15.
Gepotidacin inhibits bacterial DNA replication through a mode different from that of fluoroquinolones. Gepotidacin and comparators were tested by broth and agar dilution against clinical isolates. The in vitro activities of gepotidacin were comparable against methicillin-susceptible and -resistant Staphylococcus aureus (MSSA and MRSA, respectively) isolates (MIC90, 0.5 μg/ml). The gepotidacin MIC90s were as follows (in micrograms per milliliter) for the indicated bacteria: Streptococcus pyogenes, 0.25; Escherichia coli, 2; Moraxella catarrhalis, ≤ 0.06; Streptococcus pneumoniae (0.25), Haemophilus influenzae, 1; Clostridium perfringens, 0.5; and Shigella spp., 1, including levofloxacin-resistant subsets. Gepotidacin warrants further investigation for clinical development.
格帕沙星通过一种不同于氟喹诺酮类药物的方式抑制细菌DNA复制。采用肉汤稀释法和琼脂稀释法对格帕沙星及对照药物进行了针对临床分离株的测试。格帕沙星对甲氧西林敏感和耐药金黄色葡萄球菌（分别为MSSA和MRSA）分离株的体外活性相当（MIC90为0.5μg/ml）。格帕沙星对以下所示细菌的MIC90（以微克每毫升计）如下：化脓性链球菌，0.25；大肠杆菌，2；卡他莫拉菌，≤0.06；肺炎链球菌（0.25），流感嗜血杆菌，1；产气荚膜梭菌，0.5；以及志贺菌属，1，包括耐左氧氟沙星亚组。格帕沙星值得进一步开展临床开发研究。
