Update on Posaconazole Pharmacokinetics: Comparison of Old and New Formulations

Posaconazole is an extended-spectrum triazole antifungal that until recently was only available as an oral suspension. The absorption of this suspension is limited and is greatly affected by food, gastric pH, and intestinal motility. The systemic availability can be enhanced by administration with a high-fat meal, nutritional supplement, or acidic beverage, and by dividing into multiple daily doses. A new delayed-released tablet dosed once-daily has been developed and was recently approved by the U.S. Food and Drug Administration. This provides an attractive option for healthcare providers and patients because it has more predictable systemic availability and higher serum concentrations. However, the inability to crush or chew this tablet still leaves the need for another form of posaconazole, especially for critically ill patients. Such an option may soon become available, as a new drug application has been submitted to the FDA for a once-daily intravenous formulation of posaconazole.