In vitro and in vivo activities of HQQ-3, a new triazole antifungal agent

Abstract

The activity of HQQ-3, a new triazole antifungal agent, was evaluated and compared with those of fluconazole, ketoconazole and terbinafine in vitro and with fluconazole in vivo. HQQ-3 exhibited potent in vitro activity against clinically important fungi. The activity of HQQ-3 against Candida spp. was superior to those of fluconazole and terbinafine and comparable or superior to that of ketoconazole. HQQ-3 retained potent activity against Candida albicans strains with low levels of susceptibility to fluconazole (fluconazole MIC 80s range, 4 to >64 μg/ml). Against Cryptococcus neoformans and filamentous fungi, the activity of HQQ-3 was superior to that of fluconazole. HQQ-3 also exhibited potent in vivo activity against murine systemic infections caused by C. albicns and C. krusei. The 50% effective doses against these infections were 0.12 to 1.9 mg/kg of body weight. These result suggest that HQQ-3 may be useful in the treatment of candidiasis. © 2006 Pharmaceutical Society of Japan.