In Vitro and In Vivo Antidermatophyte Activities of NND-502, a Novel Optically Active Imidazole Antimycotic Agent

ABSTRACT In vitro and in vivo antidermatophyte activities of NND-502, a new imidazole antimycotic agent, were compared with those of two existing antifungal agents, lanoconazole and terbinafine. NND-502 exhibited strong in vitro antifungal activity against Trichophytonspp.; its MIC was 1 to 4 times lower than that of lanoconazole or terbinafine. In an in vivo study with a guinea pig model of tinea pedis, 7-day topical treatment with a 0.5% solution of NND-502 (dissolved in polyethylene glycol 400) was more effective than that with a 0.5% solution of either lanoconazole or terbinafine for eradicating fungi from the infected feet. When the duration of treatment was shortened to 3 days, a topical 1% solution of NND-502 achieved a complete mycological cure, while topical 1% solutions of lanoconazole and terbinafine did not.

[1]  H. Yamaguchi,et al.  Short-term topical therapy of experimental tinea pedis in guinea pigs with lanoconazole, a new imidazole antimycotic agent , 1995, Antimicrobial agents and chemotherapy.

[2]  H. Yamaguchi,et al.  [A study on effectiveness of treatment and prevention of relapse using topical administration of terbinafine in a guinea pig model for tinea pedis]. , 1994, The Japanese journal of antibiotics.

[3]  I. James,et al.  Short‐duration therapy with terbinafine 1% cream in dermatophyte skin infections , 1994, The British journal of dermatology.

[4]  E. Evans,et al.  Comparison of terbinafine and clotrimazole in treating tinea pedis. , 1993, BMJ.

[5]  H. Yamaguchi,et al.  Butenafine, a New Benzylamine Derivative: In vitro Effect on Arthrospores of T. mentagrophytes and Therapeutic Efficacy on Experimental Tinea Pedis in Guinea pigs , 1992 .

[6]  H. Yamaguchi,et al.  Therapeutic efficacy of latoconazole in formulations of clinical use on experimental dermatophytosis in guinea pigs. , 1992, Arzneimittel-Forschung.

[7]  N. Zaias,et al.  Short-term therapy of tinea cruris/corporis with topical terbinafine , 1992 .

[8]  H. Yamaguchi,et al.  Antifungal activity of the new agent latoconazole in two tinea models. , 1991, Arzneimittel-Forschung.

[9]  H. Yamaguchi,et al.  Effects of butenafine hydrochloride, a new benzylamine derivative, on experimental dermatophytosis in guinea pigs , 1990, Antimicrobial Agents and Chemotherapy.

[10]  H. Yamaguchi,et al.  Effects of butenafine hydrochloride, a new benzylamine derivative, on experimental tinea pedis in guinea pigs , 1990, Antimicrobial Agents and Chemotherapy.

[11]  H. Ha.  Clinical evaluation of terconazole. European experience. , 1989 .

[12]  H. A. Hirsch.  Clinical evaluation of terconazole. European experience. , 1989, The Journal of reproductive medicine.

[13]  T. Matsuyama,et al.  Experimental Tinea Pedis in Guinea Pig Feet Scanning Electron Microscopic and Histological Study of the Infection , 1988 .

[14]  W. Wagner,et al.  Oxiconazol bei Dermatomykosen — ein doppelblinder, randomisierter Therapievergleich mit Bifonazol/Oxiconazol in Dermatomycosis — a Double‐blind, Randomized Comparison with Bifonazol , 1987 .

[15]  W. Wagner,et al.  [Oxiconazole in dermatomycosis--a double-blind, randomized therapy compared with bifonazole]. , 1987, Mykosen.

[16]  T. Matsuyama,et al.  Experimental tinea pedis induced by non-abrasive inoculation of Trichophyton mentagrophytes arthrospores on the plantar part of a guinea pig foot. , 1987, Journal of medical and veterinary mycology : bi-monthly publication of the International Society for Human and Animal Mycology.

[17]  B. Allen,et al.  Sulconazole versus clotrimazole in the treatment of dermatophytosis , 1986, Clinical and experimental dermatology.

[18]  E. Kokoschka,et al.  Treatment of Dermatomycoses with Topical Fenticonazole and Econazole/Lokalbehandlung von Dermatomykosen mit Fenticonazol und Econazol , 1986, Mykosen.

[19]  G. Petrányi,et al.  SYNTHESIS AND ANTIFUNGAL ACTIVITY OF (E)-N-(6,6-DIMETHYL-2-HEPTEN-4-YNYL)-N-METHYL-1-NAPHTHALENEMETHANAMINE (SF 86-327) AND RELATED ALLYLAMINE DERIVATIVES WITH ENHANCED ORAL ACTIVITY , 1985 .

[20]  N S Ryder,et al.  Allylamine derivatives: new class of synthetic antifungal agents inhibiting fungal squalene epoxidase. , 1984, Science.

[21]  S. Stettendorf.  Tolerability and efficacy of bifonazole in dermatomycoses. , 1983, Arzneimittel-Forschung.

[22]  T. Fredriksson.  Treatment of dermatomycoses with topical tioconazole and miconazole. , 1983, Dermatologica.

[23]  K. Kuokkanen.  Topical Tioconazole in Deimatomycosis: Lokalbehandlung mit Tioconazol bei Dermatomykosen , 1982 .

[24]  K. Kuokkanen.  Topical tioconazole in dermatomycosis. , 1982, Mykosen.

[25]  J. Ulrich,et al.  Topical clotrimazole in tinea pedis. , 1977, Southern medical journal.