Second-generation azole antifungal agents

Abstract

The development of the triazole antifungal agents in the 1980s and 1990s greatly enhanced physicians' ability to treat fungal infections due to the lower toxicity of these agents compared with previous antifungal therapies. Despite the addition of these agents, there continues to be limited therapeutic choices for a number of mycoses that cause significant disease in humans. Three new agents (voriconazole, posaconazole and ravuconazole) have been developed which appear to have expanded antifungal activity compared with prior azoles. This review discusses the pharmacology, in vitro and in vivo activity, clinical studies and toxicities of these second-generation azoles. Presently, only voriconazole is available clinically and is indicated for the treatment of esophageal candidiasis, invasive aspergillosis, and refractory infections with Scedosporium apiospermum and Fusarium spp. Posaconazole and ravuconazole are still in development for human use.