Pfaller M A, Bale M J, Buschelman B, Rhomberg P
Department of Pathology, University of Iowa College of Medicine, Iowa City 52242.
Diagn Microbiol Infect Dis. 1994 Jun;19(2):75-80. doi: 10.1016/0732-8893(94)90116-3.
D0870 is a new triazole agent with potent, broad-spectrum antifungal activity. We investigated the in vitro activity of D0870, fluconazole, itraconazole, amphotericin B, and 5-fluorocytosine (5FC) against 319 clinical isolates of Candida spp. and Torulopsis glabrata. In vitro susceptibility testing was performed using a microdilution broth method performed according to NCCLS guidelines. D0870 was very active (MIC90 of 0.12 microgram/ml and 0.5 microgram/ml at 24 and 48 h incubation, respectively) against all of the yeast isolates. D0870 was 2- to 32-fold more active than amphotericin B and 2- to 8500-fold more active than 5FC. By comparison with the other triazoles, D0870 was generally 2- to 16-fold more active than itraconazole and > or = 16-fold more active than fluconazole. More than half (53%) of C. albicans isolates with elevated fluconazole and itraconazole MICs (> or = 128 micrograms/ml and > 8.0 micrograms/ml, respectively) were inhibited by < or = 1.0 microgram/ml of D0870. Based on these studies, D0870 has promising antifungal activity and warrants further in vitro and in vivo investigation.
D0870是一种新型三唑类药物,具有强大的广谱抗真菌活性。我们研究了D0870、氟康唑、伊曲康唑、两性霉素B和5-氟胞嘧啶(5FC)对319株念珠菌属和光滑球拟酵母菌临床分离株的体外活性。体外药敏试验采用根据美国国家临床实验室标准委员会(NCCLS)指南进行的微量肉汤稀释法。D0870对所有酵母分离株都非常有效(在孵育24小时和48小时时,MIC90分别为0.12微克/毫升和0.5微克/毫升)。D0870的活性比两性霉素B高2至32倍,比5FC高2至8500倍。与其他三唑类药物相比,D0870的活性通常比伊曲康唑高2至16倍,比氟康唑高≥16倍。超过一半(53%)氟康唑和伊曲康唑MIC升高(分别≥128微克/毫升和>8.0微克/毫升)的白色念珠菌分离株被≤1.0微克/毫升的D0870抑制。基于这些研究,D0870具有良好的抗真菌活性,值得进一步进行体外和体内研究。