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Madurella mycetomatis Is Highly Susceptible to Ravuconazole

机译:霉菌性马杜氏菌对Ravuconazole高度敏感

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摘要

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.
机译:由于酮康唑的复发率高,因此目前使用酮康唑治疗杜鹃花瘤的效果不理想,这经常导致并发症和不必要的截肢,并且在流行地区其费用较高。因此,需要有效且负担得起的药物来改善治疗效果。 E1224是有效的口服广谱三唑,目前正在开发中,用于治疗南美锥虫病。 E1224是一种前药,可快速转化为拉伏康唑。 E1224的血浆水平低且短暂,其治疗活性部分拉伏康唑具有治疗活性。在本研究中,评估了拉伏康唑对杜仲马杜拉菌(杜仲最常见的病原体)的体外活性,并将其与酮康唑和伊曲康唑的活性进行了比较。 Ravuconazole表现出优异的活性,MIC范围在≤0.002至0.031 µg / ml之间,显着低于所报道的酮康唑和伊曲康唑的MIC。根据我们的发现,E1224及其产生的活性部分雷伏康唑可能是治疗杜仲的有效且负担得起的治疗选择。

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