Dow Pharmaceutical Sciences, a Division of Valeant Pharmaceuticals North America LLC, Petaluma, California, USA.
Antimicrob Agents Chemother. 2013 Apr;57(4):1610-6. doi: 10.1128/AAC.02056-12. Epub 2013 Jan 14.
Onychomycosis is a common fungal nail infection in adults that is difficult to treat. The in vitro antifungal activity of efinaconazole, a novel triazole antifungal, was evaluated in recent clinical isolates of Trichophyton rubrum, Trichophyton mentagrophytes, and Candida albicans, common causative onychomycosis pathogens. In a comprehensive survey of 1,493 isolates, efinaconazole MICs against T. rubrum and T. mentagrophytes ranged from ≤ 0.002 to 0.06 μg/ml, with 90% of isolates inhibited (MIC90) at 0.008 and 0.015 μg/ml, respectively. Efinaconazole MICs against 105 C. albicans isolates ranged from ≤ 0.0005 to >0.25 μg/ml, with 50% of isolates inhibited (MIC50) by 0.001 and 0.004 μg/ml at 24 and 48 h, respectively. Efinaconazole potency against these organisms was similar to or greater than those of antifungal drugs currently used in onychomycosis, including amorolfine, ciclopirox, itraconazole, and terbinafine. In 13 T. rubrum toenail isolates from onychomycosis patients who were treated daily with topical efinaconazole for 48 weeks, there were no apparent increases in susceptibility, suggesting low potential for dermatophytes to develop resistance to efinaconazole. The activity of efinaconazole was further evaluated in another 8 dermatophyte, 15 nondermatophyte, and 10 yeast species (a total of 109 isolates from research repositories). Efinaconazole was active against Trichophyton, Microsporum, Epidermophyton, Acremonium, Fusarium, Paecilomyces, Pseudallescheria, Scopulariopsis, Aspergillus, Cryptococcus, Trichosporon, and Candida and compared favorably to other antifungal drugs. In conclusion, efinaconazole is a potent antifungal with a broad spectrum of activity that may have clinical applications in onychomycosis and other mycoses.
甲真菌病是一种常见的成人真菌感染,难以治疗。新型三唑类抗真菌药依氟康唑的体外抗真菌活性已在最近分离的红色毛癣菌、须癣毛癣菌和白色念珠菌的临床分离株中进行了评估,这些是常见的甲真菌病病原体。在对 1493 株分离株的全面调查中,依氟康唑对红色毛癣菌和须癣毛癣菌的 MIC 值范围为≤0.002 至 0.06μg/ml,90%的分离株被抑制(MIC90)在 0.008 和 0.015μg/ml 分别。依氟康唑对 105 株白色念珠菌分离株的 MIC 值范围为≤0.0005 至>0.25μg/ml,其中 50%的分离株在 24 和 48 小时时被 0.001 和 0.004μg/ml 的浓度抑制(MIC50)。依氟康唑对这些生物体的效力与目前用于甲真菌病的抗真菌药物相似或更强,包括阿莫罗芬、环吡酮、伊曲康唑和特比萘芬。在 13 例接受依氟康唑局部治疗 48 周的甲真菌病患者的红色毛癣菌趾甲分离株中,未见敏感性明显增加,表明皮肤癣菌对依氟康唑产生耐药的潜力较低。依氟康唑的活性在另外 8 株皮肤癣菌、15 株非皮肤癣菌和 10 株酵母(来自研究库的总共 109 株分离株)中进行了进一步评估。依氟康唑对红色毛癣菌、须癣毛癣菌、表皮毛癣菌、枝孢菌、镰刀菌、拟青霉、假丝酵母、链格孢菌、曲霉属、隐球菌属、毛孢子菌属和念珠菌属均有活性,与其他抗真菌药物相比具有良好的效果。总之,依氟康唑是一种具有广谱活性的强效抗真菌药物,可能在甲真菌病和其他真菌感染中具有临床应用。