title: Comparison of in vitro antifungal activities of efinaconazole and currently available antifungal agents against a variety of pathogenic fungi associated with onychomycosis.
abstract: 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.
authors: Dow Pharmaceutical Sciences, a Division of Valeant Pharmaceuticals North America LLC, Petaluma, California, USA. wjo@dowpharmsci.com
authors: William J
authors: WJ
authors: Jo Siu
authors: Yoshiyuki
authors: Y
authors: Tatsumi
authors: Hisato
authors: H
authors: Senda
authors: Radhakrishnan
authors: R
authors: Pillai
authors: Takashi
authors: T
authors: Nakamura
authors: Daisuke
authors: D
authors: Sone
authors: Annette
authors: A
authors: Fothergill
mesh_terms: D000935:Antifungal Agents / Q000494:pharmacology*; D001230:Aspergillus / Q000187:drug effects / Q000472:pathogenicity; D002175:Candida / Q000187:drug effects / Q000472:pathogenicity; D003454:Cryptococcus / Q000187:drug effects / Q000472:pathogenicity; D017964:Itraconazole / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009025:Morpholines / Q000494:pharmacology; D009281:Naphthalenes / Q000494:pharmacology; D014009:Onychomycosis / Q000382:microbiology*; D011541:Pseudallescheria / Q000187:drug effects / Q000472:pathogenicity; D060645:Scopulariopsis / Q000187:drug effects / Q000472:pathogenicity; D000077291:Terbinafine; D014230:Triazoles / Q000494:pharmacology*; D014249:Trichophyton / Q000187:drug effects / Q000472:pathogenicity; D014250:Trichosporon / Q000187:drug effects / Q000472:pathogenicity
chemical_list: D000935:Antifungal Agents; D009025:Morpholines; D009281:Naphthalenes; D014230:Triazoles; D017964:Itraconazole; C038974:amorolfine; D000077291:Terbinafine; C431707:efinaconazole