Department of Medical Microbiology and Infectious Diseases, Max Rady College of Medicine, University of Manitoba, Winnipeg, Canada.
Paratek Pharmaceuticals, Inc., King of Prussia, Pennsylvania.
Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S6-S15. doi: 10.1093/cid/ciz395.
Omadacycline is a novel aminomethylcycline antimicrobial and semisynthetic derivative of tetracycline. In vitro, omadacycline displays potent activity against gram-positive and many gram-negative bacteria, including methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, β-hemolytic streptococci, vancomycin-resistant Enterococcus, and Enterobacteriaceae. Omadacycline is also active against atypical and anaerobic pathogens, including Legionella pneumophila, Mycoplasma spp., Ureaplasma spp., Bacteroides spp., and Clostridioides difficile. This review outlines the microbiology and preclinical studies of omadacycline, including its mechanism of action; spectrum of activity; protein binding; activity in the presence of surfactant, serum, normal, and pH-adjusted urine, or bacterial biofilms; postantibiotic effect; pharmacodynamic properties; and in vitro and in vivo efficacy. The results of in vitro and in vivo animal studies support the observations made in phase III clinical trials and the clinical development of omadacycline.
奥马环素是一种新型的氨甲基环素类抗菌药物，是四环素的半合成衍生物。体外研究显示，奥马环素对革兰阳性菌和许多革兰阴性菌具有强大的活性，包括耐甲氧西林金黄色葡萄球菌、肺炎链球菌、β-溶血性链球菌、万古霉素耐药肠球菌和肠杆菌科细菌。奥马环素对非典型病原体和厌氧菌也具有活性，包括嗜肺军团菌、支原体属、脲原体属、拟杆菌属和艰难梭菌。本文概述了奥马环素的微生物学和临床前研究，包括其作用机制、活性谱、蛋白结合率、在表面活性剂、血清、正常和 pH 调整尿液或细菌生物膜存在时的活性、抗生素后效应、药效学特性以及体外和体内疗效。体外和体内动物研究的结果支持了 III 期临床试验和奥马环素临床开发中的观察结果。
