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新型水溶性棘白菌素样脂肽FK463的体外抗真菌活性

In vitro antifungal activity of FK463, a new water-soluble echinocandin-like lipopeptide.

作者信息

Mikamo H, Sato Y, Tamaya T

机构信息

Department of Obstetrics and Gynaecology, School of Medicine, Gifu University, 40 Tsukasa-machi, Gifu City, Gifu 500-8705, Japan.

出版信息

J Antimicrob Chemother. 2000 Sep;46(3):485-7. doi: 10.1093/jac/46.3.485.

Abstract

The antifungal activity of FK463 against 72 recent clinical isolates of Candida albicans (24), Candida glabrata (17), Candida tropicalis (11), Candida krusei (8) and Candida parapsilosis (12) was compared with those of amphotericin B, fluconazole and itraconazole by means of a broth microdilution method specified by the National Committee for Clinical Laboratory Standards (NCCLS) document M27-A. The lowest drug concentration at which 90% of the population was inhibited (MIC(90)) of FK463 against C. albicans, C. glabrata, C. tropicalis, C. krusei and C. parapsilosis was 0.0156, 0. 0156, 0.0313, 0.125 and 1 mg/L, respectively. FK463 exhibited broad-spectrum activity against clinically important Candida spp. (MIC range < or =0.0039-2 mg/L), and its MICs for such fungi were lower than those of other antifungal agents tested. The minimum fungicidal concentrations for Candida spp. did not differ by more than two-fold from the MICs. Results from pre-clinical evaluations performed to date indicate that FK463 should be a potent parenteral antifungal agent.

摘要

采用美国国家临床实验室标准委员会(NCCLS)M27-A文件规定的肉汤微量稀释法,将FK463对72株近期临床分离的白色念珠菌(24株)、光滑念珠菌(17株)、热带念珠菌(11株)、克柔念珠菌(8株)和近平滑念珠菌(12株)的抗真菌活性,与两性霉素B、氟康唑和伊曲康唑进行比较。FK463对白色念珠菌、光滑念珠菌、热带念珠菌、克柔念珠菌和近平滑念珠菌的最低抑菌浓度(MIC90)分别为0.0156、0.0156、0.0313、0.125和1mg/L。FK463对临床上重要的念珠菌属表现出广谱活性(MIC范围≤0.0039 - 2mg/L),且其对这些真菌的MIC低于所测试的其他抗真菌药物。念珠菌属的最低杀菌浓度与MIC相差不超过两倍。迄今为止进行的临床前评估结果表明,FK463应是一种有效的胃肠外抗真菌药物。

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