Azole Antimycotics - A Highway to New Drugs or a Dead End?

R.      Musiol; W.      Kowalczyk

Abstract

Azole antimycotics are a well-known and important class of agents that are used in hospital practice, everyday health care, veterinary medicine and for crop protection. The era of azole fungicides began with the breakthrough of chlormidazole roughly 50 years ago. Since then, more than 20 drugs of this group, including triazoles, have been brought to the market. The specific chemical structure and mechanism of the action of azoles along with the eukaryotic character of fungal pathogens raise several serious issues. Resistance to drugs and disturbance to metabolic pathways are among the most important. On the other hand, these same features are responsible for unique and novel applications of these drugs. As a result, old and ineffective antifungal drugs can be successfully used in the treatment of parasitic diseases, bacterial infections or cancers. Are azoles getting their second wind?

Keywords: Antifungals, azoles, cytochrome P450 fluconazole, off-label use, polypharmacology, resistance, triazoles, drugs, modern medicine