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. 2017 Oct 24;61(11):e01497-17.
doi: 10.1128/AAC.01497-17. Print 2017 Nov.

In Vitro Activity of the Novel Pleuromutilin Lefamulin (BC-3781) and Effect of Efflux Pump Inactivation on Multidrug-Resistant and Extensively Drug-Resistant Neisseria gonorrhoeae

Susanne Jacobsson  1 , Susanne Paukner  2 , Daniel Golparian  1 , Jörgen S Jensen  3 , Magnus Unemo  4
Affiliations

In Vitro Activity of the Novel Pleuromutilin Lefamulin (BC-3781) and Effect of Efflux Pump Inactivation on Multidrug-Resistant and Extensively Drug-Resistant Neisseria gonorrhoeae

Susanne Jacobsson et al. Antimicrob Agents Chemother. .

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 (n = 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 in vitro selection and mechanisms of resistance, pharmacokinetics/pharmacodynamics, optimal dosing, and performance in randomized controlled trials.

Keywords: MtrCDE efflux pump; antimicrobial resistance; gonorrhea; pleuromutilin; treatment.

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Figures

FIG 1
FIG 1
(a) MIC distribution for the novel pleuromutilin lefamulin and the macrolide azithromycin, including clinical Neisseria gonorrhoeae isolates (n=217) and international reference strains (n=34). (b) Comparison of the MICs of azithromycin and lefamulin for the identical material.
See this image and copyright information in PMC

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