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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.

DOI:10.1128/AAC.02145-13
PMID:24323472
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3910825/
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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本文引用的文献

1
In vitro activity of a new oral glucan synthase inhibitor (MK-3118) tested against Aspergillus spp. by CLSI and EUCAST broth microdilution methods.CLSI 和 EUCAST 肉汤微量稀释法检测新型口服葡聚糖合成酶抑制剂（MK-3118）对曲霉菌属的体外活性。
Antimicrob Agents Chemother. 2013 Feb;57(2):1065-8. doi: 10.1128/AAC.01588-12. Epub 2012 Dec 10.
2
Activity of MK-3118, a new oral glucan synthase inhibitor, tested against Candida spp. by two international methods (CLSI and EUCAST).新型口服葡聚糖合成酶抑制剂 MK-3118 的活性，经两种国际方法（CLSI 和 EUCAST）检测对念珠菌属的作用。
J Antimicrob Chemother. 2013 Apr;68(4):858-63. doi: 10.1093/jac/dks466. Epub 2012 Nov 28.
3
Improved detection of Candida sp. fks hot spot mutants by using the method of the CLSI M27-A3 document with the addition of bovine serum albumin.通过使用添加牛血清白蛋白的 CLSI M27-A3 文档方法，提高对 Candida sp. fks 热点突变体的检测。
Antimicrob Agents Chemother. 2011 May;55(5):2245-55. doi: 10.1128/AAC.01350-10. Epub 2011 Mar 7.
4
Effect of Candida glabrata FKS1 and FKS2 mutations on echinocandin sensitivity and kinetics of 1,3-beta-D-glucan synthase: implication for the existing susceptibility breakpoint.光滑念珠菌FKS1和FKS2突变对棘白菌素敏感性及1,3-β-D-葡聚糖合酶动力学的影响：对现有药敏折点的意义
Antimicrob Agents Chemother. 2009 Sep;53(9):3690-9. doi: 10.1128/AAC.00443-09. Epub 2009 Jun 22.
5
Clinical practice guidelines for the management of candidiasis: 2009 update by the Infectious Diseases Society of America.念珠菌病管理临床实践指南：美国传染病学会2009年更新版
Clin Infect Dis. 2009 Mar 1;48(5):503-35. doi: 10.1086/596757.
6
Correlating echinocandin MIC and kinetic inhibition of fks1 mutant glucan synthases for Candida albicans: implications for interpretive breakpoints.白色念珠菌棘白菌素最低抑菌浓度（MIC）与fks1突变体葡聚糖合酶动力学抑制的相关性：对解释性断点的影响
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Effects of serum on in vitro susceptibility testing of echinocandins.血清对棘白菌素体外药敏试验的影响。
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Serum differentially alters the antifungal properties of echinocandin drugs.血清可不同程度地改变棘白菌素类药物的抗真菌特性。
Antimicrob Agents Chemother. 2007 Jun;51(6):2253-6. doi: 10.1128/AAC.01536-06. Epub 2007 Apr 9.