Selamectin Is the Avermectin with the Best Potential for Buruli Ulcer Treatment.

Abstract:

:A comprehensive analysis was done to evaluate the potential use of anti-parasitic macrocyclic lactones (including avermectins and milbemycins) for Buruli ulcer (BU) therapy. A panel containing nearly all macrocyclic lactones used in human or in veterinary medicine was analyzed for activity in vitro against clinical isolates of Mycobacterium ulcerans. Milbemycin oxime and selamectin were the most active drugs against M. ulcerans with MIC values from 2 to 8 μg/mL and 2 to 4 μg/mL, respectively. In contrast, ivermectin and moxidectin, which are both in clinical use, showed no significant activity (MIC> 32 μg/mL). Time-kill kinetic assays showed bactericidal activity of selamectin and in vitro pharmacodynamic studies demonstrated exposure-dependent activity. These data together with analyses of published pharmacokinetic information strongly suggest that selamectin is the most promising macrocyclic lactone for BU treatment.

journal_name

PLoS Negl Trop Dis

authors

Scherr N,Pluschke G,Thompson CJ,Ramón-García S

doi

10.1371/journal.pntd.0003996

subject

Has Abstract

pub_date

2015-08-13 00:00:00

pages

e0003996

issue

8

eissn

1935-2727

issn

1935-2735

pii

PNTD-D-15-00710

journal_volume

9

pub_type

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