Butenafine

Butenafine (KP363) is a potent and broad spectrum benzylamine antifungal agent^[1]. Butenafine inhibits fungal ergosterol biosynthesis at the point of squalene epoxidation, leading to a deficiency of the fungal cell membranes. Butenafine is effective against dermatophytes infections, such as tinea pedis, tinea cruris, tinea versicolor^[1][2]. IC50 & Target: IC50: antifungal^[1] In Vitro: 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^[1].
Butenafine (25; 50 or 100 μM) eliminates the promastigote forms of L. amazonensis and L. braziliensis in a dose-dependent manner, and shows EC₅₀ 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 CC₅₀ of 97.88 μM^[1].
In Vivo: 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^[1].
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^[1].
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^[1].