101828-21-1

IC50: antifungal

Butenafine demonstrates comparable activity against the dermatophytes with a MIC range of 0.03-0.25 μg/ml. It displays limited activity against the yeast Candida albicans and no activity against Malassezia furfur .Butenafine (25; 50 or 100 μM) eliminates the promastigote forms of L. amazonensis and L. braziliensis in a dose-dependent manner, and shows EC ₅₀ values of 34.10±3.76 μM and 81.25±10.24 μM, respectively, in peritoneal macrophages from BALB/c mice. Butenafine induces mild cytotoxicity in peritoneal macrophages from BALB/c mice with a CC ₅₀ of 97.88 μM.

Butenafine (subcutaneous administration; 1-100 mg/kg) to mice has no effect on the central and autonomic nervous systems. Topical administration of 0.3-3.0% butenafine solutions to guinea pigs also has no effect on the somatic nervous system.In primary therapeutic studies on guinea pigs, Butenafine (1% topical application; 4-10 days; day 3 and 4 post-infection) exhibits a complete cure after 10 days in vivo-effect on dermatophytosis, T. mentagrophytes .Butenafine (0.125, 0.25, 0.5 and 1.0% topical application; q.d. or b.i.d. for 10 days; day 4 post-infection) exhibits a 100% cure after 0.5% or 1% application and has no difference in efficacy between 1% q.d. and b.i.d. in vivo-effect on dermatophytosis, T. mentagrophytes.