新型螺旋嘧啶三酮类DNA促旋酶抑制剂AZD0914对多重耐药淋病奈瑟菌分离株具有较高的体外活性，这为淋病的口服治疗提供了一种新的有效选择。
High in vitro activity of the novel spiropyrimidinetrione AZD0914, a DNA gyrase inhibitor, against multidrug-resistant Neisseria gonorrhoeae isolates suggests a new effective option for oral treatment of gonorrhea.
作者信息
Jacobsson Susanne, Golparian Daniel, Alm Richard A, Huband Michael, Mueller John, Jensen Jorgen Skov, Ohnishi Makoto, Unemo Magnus
机构信息
WHO Collaborating Centre for Gonorrhoea and other Sexually Transmitted Infections, National Reference Laboratory for Pathogenic Neisseria, Department of Laboratory Medicine, Clinical Microbiology, Örebro University Hospital, Örebro, Sweden.
Infection iMed, AstraZeneca R&D Boston, Waltham, Massachusetts, USA.
出版信息
Antimicrob Agents Chemother. 2014 Sep;58(9):5585-8. doi: 10.1128/AAC.03090-14. Epub 2014 Jun 30.
Abstract
We evaluated the activity of the novel spiropyrimidinetrione AZD0914 (DNA gyrase inhibitor) against clinical gonococcal isolates and international reference strains (n=250), including strains with diverse multidrug resistance and extensive drug resistance. The AZD0914 MICs were substantially lower than those of most other currently or previously recommended antimicrobials. AZD0914 should be further evaluated, including in vitro selection, in vivo emergence and mechanisms of resistance, pharmacokinetics/pharmacodynamics in humans, optimal dosing, and performance, in appropriate randomized and controlled clinical trials.
摘要
我们评估了新型螺嘧啶三酮类化合物AZD0914（DNA促旋酶抑制剂）对临床淋球菌分离株和国际参考菌株（n = 250）的活性，这些菌株包括具有多种耐药性和广泛耐药性的菌株。AZD0914的最低抑菌浓度（MIC）显著低于目前或以前推荐的大多数其他抗菌药物。应在适当的随机对照临床试验中对AZD0914进行进一步评估，包括体外筛选、体内耐药性的产生及机制、人体药代动力学/药效学、最佳给药剂量和效能。
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