title: Sch 39304, a new antifungal agent: oral and topical treatment of vaginal and superficial infections.
abstract: Sch 39304 is a new broad spectrum triazole antifungal agent that is active, orally and topically, against superficial Trichophyton mentagrophytes and vaginal Candida albicans infections. Sch 39304 was compared to fluconazole (FLZ) in a T. mentagrophytes infection model in guinea pigs. Following topical administration, Sch 39304 (0.125%, twice daily, 10 days), was 5-8-fold more effective than FLZ, based on culture and lesion score results. Following oral administration, Sch 39304 (2.5 mg kg-1, once daily, 10 days) produced a dramatic reduction in lesion scores and was 20-fold more active than FLZ; however, due to the length of time it takes for the drugs to reach the infected area of the skin and eradicate the infections, most animals remained culture positive with both drugs. Sch 39304 was also compared with FLZ in a vaginal C. albicans infection in hamsters. Following oral administration (4 days), Sch 39304 (1.6 mg kg-1), cured all hamsters and was 4-fold more active than FLZ. In addition, Sch 39304 as a single oral dose (10 mg kg-1) also cured all hamsters. When treatment was intravaginal (8 days), Sch 39304 was again more active than FLZ (2-fold), and also micronazole (8-fold), with 100% of the hamsters cured at concentrations as low at 0.025%.
authors.affiliation: Schering-Plough Research Inst., Kenilworth, New Jersey 07033.
authors.forename: R M
authors.initials: RM
authors.lastname: Parmegiani
authors.forename: D
authors.initials: D
authors.lastname: Loebenberg
authors.forename: A
authors.initials: A
authors.lastname: Cacciapuoti
authors.forename: B
authors.initials: B
authors.lastname: Antonacci
authors.forename: C
authors.initials: C
authors.lastname: Norris
authors.forename: F
authors.initials: F
authors.lastname: Menzel
authors.forename: L
authors.initials: L
authors.lastname: Moss
authors.forename: T
authors.initials: T
authors.lastname: Yarosh-Tomaine
authors.forename: R S
authors.initials: RS
authors.lastname: Hare
authors.forename: G H
authors.initials: GH
authors.lastname: Miller
mesh_terms: D000284:Administration, Oral; D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D002181:Candidiasis, Vulvovaginal / Q000188:drug therapy*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005260:Female; D015725:Fluconazole / Q000627:therapeutic use; D006168:Guinea Pigs; D008825:Miconazole / Q000627:therapeutic use; D014005:Tinea / Q000188:drug therapy*; D014230:Triazoles / Q000008:administration & dosage / Q000627:therapeutic use*
chemical_list: D000935:Antifungal Agents; D014230:Triazoles; C056513:Sch 39304; D008825:Miconazole; D015725:Fluconazole