In patients with severe underlying illnesses, invasive fungal infections have developed into significant sources of morbidity and mortality. Treatment options have been restricted to amphotericin B deoxycholate (AmB-D) with or without flucytosine for more than three decades. Only after the clinical advancement of itraconazole (ITC) and fluconazole (FLC) in the late 1980s did therapeutic options become available. The arsenal of antifungal agents, however, has significantly increased over the past ten years as a result of the introduction of less toxic AmB formulations, the improvement of antifungal triazoles, and the appearance of echinocandin lipopeptides, a new class of antifungal agents that target the fungal cell wall. In order to treat invasive fungal infections, this article discusses the clinical pharmacology of both licenced and investigational antifungal medications.