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Public Library of Science, PLoS Neglected Tropical Diseases, 8(9), p. e0003996, 2015

DOI: 10.1371/journal.pntd.0003996

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

Journal article published in 2015 by Nicole Scherr, Gerd Pluschke, Charles J. Thompson, Santiago Ramón-García ORCID
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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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.