title: In vitro and in vivo antidermatophytic activity of saperconazole, a new fluorinated triazole.
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.
authors.affiliation: Department of Microbiology Research, R.W. Johnson Research Institute, Raritan, New Jersey 08869.
authors.forename: K P
authors.initials: KP
authors.lastname: Fu
authors.forename: D M
authors.initials: DM
authors.lastname: Isaacson
authors.forename: J
authors.initials: J
authors.lastname: Lococo
authors.forename: B
authors.initials: B
authors.lastname: Foleno
authors.forename: J
authors.initials: J
authors.lastname: Hilliard
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000494:pharmacology*; D001393:Azoles / Q000494:pharmacology*; D005260:Female; D006168:Guinea Pigs; D008826:Microbial Sensitivity Tests; D014005:Tinea / Q000188:drug therapy; D014249:Trichophyton / Q000187:drug effects*
chemical_list: D000935:Antifungal Agents; D001393:Azoles; C060571:saperconazole