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Delafloxacin: Place in Therapy and Review of Microbiologic, Clinical and Pharmacologic Properties

机译：德拉福沙星：在治疗中的地位以及微生物学，临床和药理学性质的综述

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Delafloxacin (formerly WQ-3034, ABT492, RX-3341) is a novel fluoroquinolone chemically distinct from currently marketed fluoroquinolones with the absence of a protonatable substituent conferring a weakly acidic character to the molecule. This property results in increased intracellular penetration and enhanced bactericidal activity under acidic conditions that characterize the infectious milieu at a number of sites. The enhanced potency and penetration in low pH environments contrast what has been observed for other zwitterionic fluoroquinolones, which tend to lose antibacterial potency under acidic conditions, and may be particularly advantageous against methicillin-resistant Staphylococcus aureus , for which the significance of the intracellular mode of survival is increasingly being recognized. Delafloxacin is also unique in its balanced target enzyme inhibition, a property that likely explains the very low frequencies of spontaneous mutations in vitro. Delafloxacin recently received US Food and Drug Administration approval for the treatment of acute bacterial skin and skin structure infections and is currently being evaluated in a phase 3 trial among patients with community-acquired pneumonia. In the current era of a heightened awareness pertaining to collateral ecologic damage, safety issues and antimicrobial stewardship principles, it is critical to describe the unique properties of delafloxacin and define its potential role in therapy. The purpose of this article is to review available data pertaining to delafloxacin’s biochemistry, pharmacokinetic/pharmacodynamics characteristics, in vitro activity and potential for resistance selection as well as current progress in clinical trials to ultimately assist clinicians in selecting patients who will benefit most from the distinctive properties of this agent.
机译：Delafloxacin（以前的WQ-3034，ABT492，RX-3341）是一种新型的氟喹诺酮，在化学上与目前市售的氟喹诺酮类药物不同，没有可质子化的取代基赋予该分子弱酸性。这种特性导致在酸性条件下增加细胞内渗透性并增强杀菌活性，而酸性条件是许多部位感染环境的特征。在低pH环境中增强的效力和渗透性与其他两性离子氟喹诺酮类药物所观察到的相反，两性离子氟喹诺酮类药物在酸性条件下往往会失去抗菌效力，并且可能特别有利于耐甲氧西林的金黄色葡萄球菌，因为胞内模式的重要性生存越来越被认可。德拉福沙星还具有独特的平衡靶酶抑制特性，这一特性很可能解释了体外自发突变的频率非常低。 Delafloxacin最近获得了美国食品和药物管理局的批准，用于治疗急性细菌性皮肤和皮肤结构感染，目前正在社区获得性肺炎患者的3期试验中进行评估。在当前有关附带生态损害，安全问题和抗菌管理原则的认识日益提高的时代，描述德拉福沙星的独特特性并确定其在治疗中的潜在作用至关重要。本文的目的是审查与德拉福沙星的生物化学，药代动力学/药效学特征，体外活性和耐药选择潜力以及临床试验的最新进展有关的可用数据，以最终帮助临床医生选择将从该独特药物中受益最大的患者该代理的属性。

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