新型截短侧耳素利福霉素（BC-3781）的活性及外排泵失活对耐多药和广泛耐药淋病奈瑟菌的影响。
Activity of the Novel Pleuromutilin Lefamulin (BC-3781) and Effect of Efflux Pump Inactivation on Multidrug-Resistant and Extensively Drug-Resistant Neisseria gonorrhoeae.
机构信息
WHO Collaborating Centre for Gonorrhoea and Other Sexually Transmitted Infections, National Reference Laboratory for Pathogenic Neisseria, Department of Laboratory Medicine, Faculty of Medicine and Health, Örebro University, Örebro, Sweden.
Nabriva Therapeutics AG, Vienna, Austria.
出版信息
Antimicrob Agents Chemother. 2017 Oct 24;61(11). doi: 10.1128/AAC.01497-17. Print 2017 Nov.
Abstract
We evaluated the activity of the novel semisynthetic pleuromutilin lefamulin, inhibiting protein synthesis and growth, and the effect of efflux pump inactivation on clinical gonococcal isolates and reference strains ( = 251), including numerous multidrug-resistant and extensively drug-resistant isolates. Lefamulin showed potent activity against all gonococcal isolates, and no significant cross-resistance to other antimicrobials was identified. Further studies of lefamulin are warranted, including selection and mechanisms of resistance, pharmacokinetics/pharmacodynamics, optimal dosing, and performance in randomized controlled trials.
摘要
我们评估了新型半合成截短侧耳素类利福霉素 lefamulin 的活性，该药物可抑制蛋白质合成和生长，并评估了外排泵失活对临床淋病奈瑟菌分离株和参考株（=251 株）的影响，包括许多多药耐药和广泛耐药的分离株。 lefamulin 对所有淋病奈瑟菌分离株均显示出强大的活性，且未发现与其他抗菌药物的显著交叉耐药性。 lefamulin 的进一步研究是必要的，包括耐药性的选择和机制、药代动力学/药效学、最佳剂量和随机对照试验中的表现。
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