Abstract：
Acute bacterial skin and skin structure infections (ABSSSIs) are one of the most common types of infections due to methicillin-resistant Staphylococcus aureus (MRSA). The standard of care for ABSSSI includes glycopeptides such as vancomycin, teicoplanin, oxazolidinones and fluoroquinolones, which are potent broad-spectrum antibacterial agents. Unfortunately, due to indiscriminate utilization, resistance to these agents is rising and identification of novel agents is an urgent unmet medical need. In this context, levonadifloxacin (WCK-771) is a novel, hydrate arginine salt of nadifloxacin with improved bactericidal activity against MRSA as well as fluoroquinolone-resistant S. aureus by targeting bacterial DNA supercoiling enzymes DNA gyrase and topoisomerase IV. Levonadifloxacin displays a broad-spectrum bactericidal activity against Gram-positive and Gram-negative bacteria, atypical bacteria, anaerobic bacteria and bioterror pathogens with a very low frequency of mutation. Levonadifloxacin also displays improved activity under low pH biofilm environments. The drug has successfully completed phase I, phase II and phase III clinical trials in India. The U.S. Food and Drug Administration (FDA) granted a Qualified Infectious Disease Product (QIDP) designation to levonadifloxacin for the treatment of MRSA infections in August 2014.
摘要：
急性细菌性皮肤和皮肤结构感染(ABSSSI)是由于耐甲氧西林金黄色葡萄球菌(MRSA)引起的最常见的感染类型之一。ABSSSI的护理标准包括糖肽，如万古霉素，替考拉宁,恶唑烷酮和氟喹诺酮,是有效的广谱抗菌剂。不幸的是,由于滥用，对这些药物的耐药性正在上升，新药物的鉴定是一个迫切的未满足的医学需求。在这种情况下，左旋阿霉素（WCK-771）是一种新型的，通过靶向细菌DNA超螺旋酶DNA旋转酶和拓扑异构酶IV，水合纳迪沙星的精氨酸盐对MRSA和氟喹诺酮抗性金黄色葡萄球菌具有改善的杀菌活性。左旋阿霉素对革兰氏阳性和革兰氏阴性细菌具有广谱杀菌活性，非典型细菌，厌氧菌和生物恐怖病原体具有非常低的突变频率。在低pH生物膜环境下，左旋阿霉素还显示出改善的活性。该药已成功完成第一阶段，印度的II期和III期临床试验。2014年8月，美国食品和药物管理局（FDA）授予左旋阿霉素用于治疗MRSA感染的合格传染病产品（QIDP）称号。
