Invasive fungal infections are seen with growing frequency, likely due to increases in numbers of patients at risk of infection. Optimal selection and dosing of antifungal agents are important, as these infections are often refractory to available therapy. In contrast to antibacterials, studies examining the pharmacodynamic properties of antifungals and their application in treating invasive disease often are lacking. Agents administered for invasive infections are amphotericin B, flucytosine, and azole antifungals. Several drugs are under investigation, such as posiconazole, voriconazole, and the echinocandins, and preliminary pharmacodynamic data likely will help shape dosing regimens. Clinical trials that investigated dosage and administration, as well as the potential benefits of combination and sequential therapy, are addressed. In addition, antifungal susceptibility and animal models of infection are discussed.