Antifungal activity of saperconazole (R 66 905) in vitro

Abstract

Saperconazole, a novel orally active triazole antifungal, inhibited Candida spp., Aspergillus spp. and dermatophyte fungi in vitro. Its minimal inhibitory concentrations for Candida spp. and dermatophytes were relatively high, like those of comparable triazole antifungals, but all of the Aspergillus isolates tested were inhibited by less than 0.1 mg/l. Relative inhibition factors of saperconazole were in the range 31-76% for Candida isolates, 6-18% for Aspergillus isolates and 5-10% for dermatophytes. These figures predict a good inhibitory activity of saperconazole for all the fungi tested, with particularly strong activity against Aspergillus spp. and dermatophytes. Saperconazole inhibited hyphal branch formation in C. albicans at concentrations as low as 10(8) M.