We evaluated the registered antifungal medications and outlined their methods of action, pharmacological characteristics, and susceptibility to certain fungus. Approved antimycotics can inhibit 1,3-β-d-glucan synthase, lanosterol 14-αdemethylase, protein and deoxyribonucleic acid production, or sequester ergosterol. Their most serious side effects are hepatotoxicity, nephrotoxicity, and myelotoxicity. Echinocandins have essentially no drug-drug interactions, while triazoles have the most. Antifungal resistance can be established in most infections by drug target overexpression, efflux pump activation, and amino acid substitution. Additionally reviewed are the investigational antifungal medications undergoing clinical studies. The most promising new antifungal treatments are siderophores used in the Trojan horse technique or siderophore production enzyme inhibitors.