JMI Laboratories, North Liberty, IA 52317, USA.
Diagn Microbiol Infect Dis. 2010 Apr;66(4):393-401. doi: 10.1016/j.diagmicrobio.2009.10.013.
CEM-101 is a novel fluoroketolide with reported high potency against diverse groups of Gram-positive (Micrococcus spp., viridans group streptococci, Corynebacterium spp. Listeria monocytogenes, Clostridium spp., etc.) and Gram-negative bacteria (Neisseria gonorrhoeae, Campylobacter jejuni, Helicobacter pylori, Bacteroides fragilis, Shigella spp., etc.), including mycoplasma and ureaplasma, as well as bacteria commonly associated with community-acquired respiratory tract infections and skin and skin structure infections. In this study, CEM-101 and comparator antimicrobials were tested against a collection of very low prevalence aerobic and anaerobic bacteria collected via the SENTRY Antimicrobial Surveillance Program platform. CEM-101 was highly active against all Gram-positive organisms (MIC(50), 0.015 microg/mL) as compared with telithromycin (MIC(50), 0.06 microg/mL), clarithromycin (MIC(50), 0.12 microg/mL), and erythromycin (MIC(50), 0.25 microg/mL). Among Gram-negative pathogens, CEM-101 also displayed a high potency against most strains (MIC(50), 4 microg/mL) but was found to be equivalent or less active when compared with other antimicrobials tested with MIC(50) values ranging from < or =0.12 microg/mL for levofloxacin to 8 microg/mL for telithromycin. Among the strict anaerobic species, CEM-101 activity mirrored that of the aerobic species: high activity against the Gram-positive anaerobes (MIC(50) results ranging from < or =0.03 microg/mL to 0.12 microg/mL) and equivalent or less susceptible against Gram-negative anaerobes. Our in vitro antimicrobial susceptibility results for CEM-101 demonstrate better activity compared with other MLS(B) class agents among a diverse group of uncommonly isolated bacterial pathogens; these results provide an impetus for possible expanded indications during Phase 2 and 3 clinical trials.
CEM-101 是一种新型氟酮内酯，据报道对多种革兰阳性（微球菌属、草绿色链球菌、棒状杆菌属、李斯特菌属、梭菌属等）和革兰阴性细菌（淋病奈瑟菌、空肠弯曲菌、幽门螺杆菌、脆弱拟杆菌、志贺菌属等）具有高活性，包括支原体和脲原体，以及与社区获得性呼吸道感染和皮肤及皮肤结构感染相关的常见细菌。在这项研究中，CEM-101 和对照抗菌药物对通过 SENTRY 抗菌监测计划平台收集的一组非常低流行的需氧和厌氧细菌进行了测试。与克拉霉素（MIC50，0.12μg/mL）和红霉素（MIC50，0.25μg/mL）相比，CEM-101 对所有革兰阳性菌均具有高度活性（MIC50，0.015μg/mL）。在革兰阴性病原体中，CEM-101 对大多数菌株也表现出高活性（MIC50，4μg/mL），但与其他测试的抗菌药物相比，其活性相当或较低，MIC50 值范围从左氧氟沙星的<或=0.12μg/mL 到克拉霉素的 8μg/mL。在严格的厌氧菌中，CEM-101 的活性与需氧菌相似：对革兰阳性厌氧菌具有高活性（MIC50 结果范围为<或=0.03μg/mL 至 0.12μg/mL），对革兰阴性厌氧菌的敏感性相当或较低。我们对 CEM-101 的体外抗菌药敏结果表明，与 MLS(B)类其他药物相比，在一组不同的罕见分离细菌病原体中具有更好的活性；这些结果为 2 期和 3 期临床试验中可能扩大的适应症提供了动力。
