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[Therapeutic effect of amorolfine on experimental dermatophytosis]
K Uchida1, A Matsuzaka, H Yamaguchi
1Teikyo University Research Center for Medical Mycology.
Abstract:
Therapeutic effects of cream and solution of amorolfine (MT-861), a new morpholine antifungal agent, were investigated using 1% cream and solution of bifonazole (BFZ) as the reference drug in Trichophyton mentagrophytes-infected guinea pig to evaluate the usefulness of MT-861. The results obtained are summarized as follows. 1. Once-a-day topical applications of 0.125, 0.5, and 1% MT-861 cream preparations starting day-5 postinfection were therapeutically effective. The effectiveness increased with increasing concentrations of active preparations, reaching nearly the maximum level at 0.5%. The treatment with 0.5% or 1% MT-861 cream preparation produced significantly greater improvement of clinical symptoms and culture results than did the treatment with the 1% BFZ cream preparation. 2. Treatment of 7 days or longer with 0.5 or 1% cream of MT-861 was required to produce therapeutic effect. Close relationships were observed between chitin contents of skin lesions and the presence of the pathogen in the lesions after 1, 2 and 3 weeks of treatment. 3. When MT-861 solutions were applied once daily for 2 weeks, the effectiveness increased as drug concentrations increased similarly to the cream treatment. A significant difference was observed (P less than 0.05 approximately 0.001) in degrees of lesions and culture results between the treatment with MT-861 and with BFZ control solutions. Thus, excellent therapeutic effectiveness in the Trichophyton infection model of guinea pigs was obtained by treatment with both the cream and the solution of MT-861. Once a day dosage of 0.5% drug concentration produced adequate effectiveness. A high clinical usefulness is expected in the treatment of fungal infections of the skin using MT-861.
Insights
Amorolfine (MT-861) cream and solution demonstrated significant therapeutic effects against Trichophyton mentagrophytes infections in guinea pigs. A 0.5% concentration applied once daily proved effective, outperforming bifonazole (BFZ).
Area of Science:
- Dermatology
- Mycology
- Pharmacology
Background:
- Superficial fungal infections pose a significant public health challenge.
- Novel antifungal agents are continuously sought for improved therapeutic outcomes.
- Amorolfine (MT-861) is a new morpholine antifungal agent with potential clinical applications.
Purpose of the Study:
- To evaluate the therapeutic efficacy of amorolfine (MT-861) cream and solution.
- To compare the effectiveness of MT-861 with bifonazole (BFZ) in a guinea pig model of Trichophyton mentagrophytes infection.
- To determine optimal concentrations and treatment durations for MT-861.
Main Methods:
- Guinea pigs infected with Trichophyton mentagrophytes were treated with varying concentrations of MT-861 cream (0.125%, 0.5%, 1%) and solution.
- Bifonazole (BFZ) 1% cream and solution served as reference treatments.
- Therapeutic effects were assessed by clinical symptom improvement, fungal culture results, and chitin content in skin lesions.
Main Results:
- Once-daily topical application of MT-861 cream (0.125%, 0.5%, 1%) showed dose-dependent therapeutic effectiveness, with 0.5% achieving near-maximal results.
- MT-861 cream (0.5%, 1%) demonstrated significantly superior clinical and mycological outcomes compared to 1% BFZ cream.
- MT-861 solutions also exhibited concentration-dependent efficacy, outperforming BFZ solutions.
- A treatment duration of 7 days or longer with 0.5% or 1% MT-861 cream was required for therapeutic effect.
Conclusions:
- Both amorolfine (MT-861) cream and solution exhibit excellent therapeutic effectiveness against Trichophyton infections in a guinea pig model.
- A once-daily dosage of 0.5% amorolfine provides adequate efficacy.
- MT-861 demonstrates high clinical potential for treating superficial fungal skin infections.