SCH 39304, A NEW ANTIFUNGAL AGENT - ORAL AND TOPICAL TREATMENT OF VAGINAL AND SUPERFICIAL INFECTIONS

Sch 39304 is a new broad spectrum triazole antifungal agent that is ac tive, orally and topically, against superficial Trichophyton mentagrop hytes and vaginal Candida albicans infections. Sch 39304 was compared to fluconazole (FLZ) in a T mentagrophytes infection model in guinea p igs. 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 sc ores 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 w ith both drugs. Sch 39304 was also compared with FLZ in a vaginal C al bicans 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) a lso cured all hamsters. When treatment was intravaginal (8 days), Sch 39304 was again more active than FLZ (2-fold), and also miconazole (8- fold), with 100% of the hamsters cured at concentrations as low at 0.0 25%.