Butenafine is a new antifungal agent with primary fungicidal activity
against dermatophytes such as Trichophyton mentagrophytes, Microsporum
canis and Trichophyton rubrum which cause tinea infections. C-14-labe
lled butenafine (=30 mu g/g tissue) was found within guinea-pig dorsal
skin 24 hours after topical application. Most of the drug was distrib
uted into the epidermis including the horny layer. Small amounts were
found in the dermis, probably transported via sebaceous glands and hai
r follicles. In vitro, the minimum concentration that completely inhib
ited growth of dermatophytes (MIG) and the minimum fungicidal concentr
ations (MFC) for butenafine against T. mentagrophytes and M. canis wer
e similar(0.012 to 0.05 mg/L) and were 4 to 130 times lower than those
for naftifine, tolnaftate, clotrimazole and bifonazole. It also has g
reater activity against I: rubrum, M. gypseum and Epidermophyton flocc
osum when compared with naftifine tolnaftate and clotrimazole; compari
sons with bifonazole against these strains were not available. Assessm
ent after 1 week's treatment in patients with tinea pedis revealed tha
t mycological cure rates were greater in those who received twice-dail
y butenafine for 1 week or once-daily butenafine for 4 weeks than in p
lacebo recipients. Mycological and overall cure rates were either furt
her increased or maintained up to 5 weeks after treatment cessation co
mpared with end-of-treatment values. In patients with tinea cruris or
tinea corporis who received once-daily butenafine 1% for 2 weeks, the
mycological and overall cure rates continued to increase for up to 1 w
eeks after treatment cessation.