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In vitro and in vivo antidermatophytic activity of saperconazole, a new fluorinated triazole
K P Fu1, D M Isaacson, J Lococo
1Department of Microbiology Research, R.W. Johnson Research Institute, Raritan, New Jersey 08869.
Abstract:
The in vitro activity of saperconazole against selected isolates of dermatophytes and its in vivo efficacy in a guinea pig dermatophytic infection model using Trichophyton mentagrophytes were evaluated. Susceptibility testing was determined with an agar dilution method in three media: yeast nitrogen base agar (YNBA), brain heart infusion agar (BHIA) and Sabouraud dextrose agar (SDA). An inoculum of 1 x 10(5) CFU of T. mentagrophytes spores was placed onto the surface of these agars. Incubation was at 32 degrees C for 72 h. The MIC of saperconazole against all isolates was less than 1 microgram/ml, whereas the MIC ranged from 0.1 to > 128 micrograms/ml for fluconazole. The MIC range of saperconazole against Trichophyton species was < or = 0.002 to 0.25 micrograms/ml; against Microsporum species it was < 0.001 to 0.1 microgram/ml; and against Epidemophyton species was < or = 0.002 to 0.25 micrograms/ml. These data showed that saperconazole was the most active compound tested against these selected dermatophytes. The activities of saperconazole against T. mentagrophytes, T. rubrum and M. canis were not affected by the medium. The MICs against these organisms were < or = 0.008 micrograms/ml in SDA, YNBA or BHIA. There were 2- to 4-fold decreases in activity for fluconazole at the same conditions. In vivo, topical treatment with saperconazole at concentrations of 0.125% and 0.25% resulted in 50% and 75% microbiological cure rates, respectively, in the guinea pig topically infected with T. mentagrophytes.
Insights
Saperconazole demonstrates potent in vitro antifungal activity against dermatophytes, significantly outperforming fluconazole. Topical saperconazole achieved high cure rates in a guinea pig model of fungal infection.
Area of Science:
- Mycology
- Antimicrobial Agents
- Dermatology
Background:
- Dermatophytosis is a common fungal infection.
- Existing treatments have limitations.
- Novel antifungal agents are needed.
Purpose of the Study:
- To evaluate the in vitro activity of saperconazole against dermatophytes.
- To assess the in vivo efficacy of saperconazole in a guinea pig model of dermatophytosis.
Main Methods:
- Agar dilution method used for in vitro susceptibility testing.
- Three media (YNBA, BHIA, SDA) evaluated.
- Guinea pig model with Trichophyton mentagrophytes infection used for in vivo testing.
Main Results:
- Saperconazole exhibited low minimum inhibitory concentrations (MICs) (<1 µg/mL) against all dermatophyte isolates.
- Saperconazole was significantly more potent than fluconazole, with MICs <0.008 µg/mL in various media.
- Topical saperconazole at 0.125% and 0.25% achieved 50% and 75% microbiological cure rates, respectively.
Conclusions:
- Saperconazole is a highly potent antifungal agent against dermatophytes in vitro.
- Saperconazole demonstrates promising in vivo efficacy for treating dermatophytosis.
- Saperconazole represents a potential new therapeutic option for fungal skin infections.