Albaconazole -: Antifungal

The search for novel, potent broad-spectrum oral antifungal agents continues to be a research priority due to the increase in incidence of opportunistic fungal infections over the past 15 years. Azoles are attractive antimycotics with agents such as fluconazole and itraconazole exhibiting broad-spectrum activity and improved safety profiles over other antifungal compounds. One such novel azole to emerge which shows considerable clinical promise is albaconazole (UR-9825). The orally active azole has shown excellent activity in vitro, with MIC values lower than or comparable to those obtained for fluconazole, itraconazole, voriconazole, posaconazole and ravuconazole. The agent was also active against fluconazole-resistant Candida spp., non-albicans Candida strains, Cryptococcus neoformans, filamentous fungi (e.g., Aspergillus spp., Trichophyton spp., Microsporum spp.), Scedosporium, other life-threatening molds including amphotericin B-resistant strains and the parasite Trypanosoma cruzi. Moreover, the agent was markedly active in vivo in animal models of candidiasis, aspergillosis, cryptococcosis, scedosporiosis and trypanosomiasis. Albaconazole has been shown to be rapidly absorbed in humans with excellent cardiovascular safety and tolerability profiles obtained. The agent is scheduled to begin phase 11 clinical trials in vulvovaginal candidiasis later this year.