|Trade names||Noxafil, Posanol|
|By mouth (oral suspension, delayed-release tablets), IV|
|Bioavailability||Low (8 to 47% Oral)|
|Protein binding||98 to 99%|
|Elimination half-life||16 to 31 hours|
|Excretion||Fecal (71–77%) and renal (13–14%)|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||700.778 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Posaconazole is used to treat invasive Aspergillus and Candida infections. It is also used for the treatment of oropharyngeal candidiasis (OPC), including OPC refractory to itraconazole and/or fluconazole therapy.
Posaconazole works by disrupting the close packing of acyl chains of phospholipids, impairing the functions of certain membrane-bound enzyme systems such as ATPase and enzymes of the electron transport system, thus inhibiting growth of the fungi. It does this by blocking the synthesis of ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of methylated sterol precursors. Posaconazole is significantly more potent at inhibiting 14-alpha demethylase than itraconazole.
Posaconazole is absorbed within three to five hours. It is predominantly eliminated through the liver, and has a half-life of about 35 hours. Oral administration of posaconazole taken with a high-fat meal exceeds 90% bioavailability and increases the concentration by four times compared to fasting state.