烟曲霉素衍生物 MK-3118 对临床棘白菌素耐药的念珠菌属和曲霉属分离株显示出体外活性增强。
Enfumafungin derivative MK-3118 shows increased in vitro potency against clinical echinocandin-resistant Candida Species and Aspergillus species isolates.
机构信息
Public Health Research Institute, New Jersey Medical School, Rutgers, The State University of New Jersey, Newark, New Jersey, USA.
出版信息
Antimicrob Agents Chemother. 2014;58(2):1248-51. doi: 10.1128/AAC.02145-13. Epub 2013 Dec 9.
Abstract
MK-3118 is as an orally active new antifungal in the early stage of clinical development that inhibits the biosynthesis of β-(1,3)-glucan. We evaluated the in vitro activity of this compound against wild-type and echinocandin-resistant (ER) isolates containing mutations in the FKS gene(s) of Candida spp. and Aspergillus spp. MK-3118 demonstrated enhanced efficacy for most C. albicans and C. glabrata ER isolates relative to caspofungin, with decreased MICs and half-maximal inhibitory concentrations (IC50s).
摘要
MK-3118 是一种处于临床开发早期的新型口服抗真菌药物，可抑制β-（1,3）-葡聚糖的生物合成。我们评估了该化合物对野生型和棘白菌素耐药（ER）分离株的体外活性，这些分离株包含 Candida spp. 和 Aspergillus spp. 的 FKS 基因的突变。与卡泊芬净相比，MK-3118 对大多数 C. albicans 和 C. glabrata ER 分离株表现出增强的疗效，MIC 和半最大抑制浓度（IC50）降低。
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2
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