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Madurella mycetomatis Is Highly Susceptible to Ravuconazole

The current treatment of eumycetoma utilizing ketoconazole is unsatisfactory because of high recurrence rates, which often leads to complications and unnecessary amputations, and its comparatively high cost in endemic areas. Hence, an effective and affordable drug is required to improve therapeutic...

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Autores principales: Ahmed, Sarah Abdalla, Kloezen, Wendy, Duncanson, Frederick, Zijlstra, Ed E., de Hoog, G. Sybren, Fahal, Ahmed H., van de Sande, Wendy W. J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4063742/
https://www.ncbi.nlm.nih.gov/pubmed/24945848
http://dx.doi.org/10.1371/journal.pntd.0002942
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author Ahmed, Sarah Abdalla
Kloezen, Wendy
Duncanson, Frederick
Zijlstra, Ed E.
de Hoog, G. Sybren
Fahal, Ahmed H.
van de Sande, Wendy W. J.
author_facet Ahmed, Sarah Abdalla
Kloezen, Wendy
Duncanson, Frederick
Zijlstra, Ed E.
de Hoog, G. Sybren
Fahal, Ahmed H.
van de Sande, Wendy W. J.
author_sort Ahmed, Sarah Abdalla
collection PubMed
description The current treatment of eumycetoma utilizing ketoconazole is unsatisfactory because of high recurrence rates, which often leads to complications and unnecessary amputations, and its comparatively high cost in endemic areas. Hence, an effective and affordable drug is required to improve therapeutic outcome. E1224 is a potent orally available, broad-spectrum triazole currently being developed for the treatment of Chagas disease. E1224 is a prodrug that is rapidly converted to ravuconazole. Plasma levels of E1224 are low and transient, and its therapeutically active moiety, ravuconazole is therapeutically active. In the present study, the in vitro activity of ravuconazole against Madurella mycetomatis, the most common etiologic agent of eumycetoma, was evaluated and compared to that of ketoconazole and itraconazole. Ravuconazole showed excellent activity with MICs ranging between ≤0.002 and 0.031 µg/ml, which were significantly lower than the MICs reported for ketoconazole and itraconazole. On the basis of our findings, E1224 with its resultant active moiety, ravuconazole, could be an effective and affordable therapeutic option for the treatment of eumycetoma.
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spelling pubmed-40637422014-06-25 Madurella mycetomatis Is Highly Susceptible to Ravuconazole Ahmed, Sarah Abdalla Kloezen, Wendy Duncanson, Frederick Zijlstra, Ed E. de Hoog, G. Sybren Fahal, Ahmed H. van de Sande, Wendy W. J. PLoS Negl Trop Dis Research Article The current treatment of eumycetoma utilizing ketoconazole is unsatisfactory because of high recurrence rates, which often leads to complications and unnecessary amputations, and its comparatively high cost in endemic areas. Hence, an effective and affordable drug is required to improve therapeutic outcome. E1224 is a potent orally available, broad-spectrum triazole currently being developed for the treatment of Chagas disease. E1224 is a prodrug that is rapidly converted to ravuconazole. Plasma levels of E1224 are low and transient, and its therapeutically active moiety, ravuconazole is therapeutically active. In the present study, the in vitro activity of ravuconazole against Madurella mycetomatis, the most common etiologic agent of eumycetoma, was evaluated and compared to that of ketoconazole and itraconazole. Ravuconazole showed excellent activity with MICs ranging between ≤0.002 and 0.031 µg/ml, which were significantly lower than the MICs reported for ketoconazole and itraconazole. On the basis of our findings, E1224 with its resultant active moiety, ravuconazole, could be an effective and affordable therapeutic option for the treatment of eumycetoma. Public Library of Science 2014-06-19 /pmc/articles/PMC4063742/ /pubmed/24945848 http://dx.doi.org/10.1371/journal.pntd.0002942 Text en © 2014 Ahmed et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Ahmed, Sarah Abdalla
Kloezen, Wendy
Duncanson, Frederick
Zijlstra, Ed E.
de Hoog, G. Sybren
Fahal, Ahmed H.
van de Sande, Wendy W. J.
Madurella mycetomatis Is Highly Susceptible to Ravuconazole
title Madurella mycetomatis Is Highly Susceptible to Ravuconazole
title_full Madurella mycetomatis Is Highly Susceptible to Ravuconazole
title_fullStr Madurella mycetomatis Is Highly Susceptible to Ravuconazole
title_full_unstemmed Madurella mycetomatis Is Highly Susceptible to Ravuconazole
title_short Madurella mycetomatis Is Highly Susceptible to Ravuconazole
title_sort madurella mycetomatis is highly susceptible to ravuconazole
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4063742/
https://www.ncbi.nlm.nih.gov/pubmed/24945848
http://dx.doi.org/10.1371/journal.pntd.0002942
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