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| Clinical data | |
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| Trade names | Noxafil, Posanol, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607036 |
| License data | |
| Pregnancy category | |
| Routes of administration | By mouth,intravenous |
| ATC code | |
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| Pharmacokinetic data | |
| Bioavailability | Low (8 to 47% Oral) |
| Protein binding | 98 to 99% |
| Metabolism | Liver (glucuronidation) |
| Eliminationhalf-life | 16 to 31 hours |
| Excretion | Fecal (71–77%) andKidney (13–14%) |
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| DrugBank |
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| ChEBI | |
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.208.201 |
| Chemical and physical data | |
| Formula | C37H42F2N8O4 |
| Molar mass | 700.792 g·mol−1 |
| 3D model (JSmol) | |
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Posaconazole, sold under the brand nameNoxafil among others, is atriazoleantifungal medication.[7][8]
It was approved for medical use in the European Union in October 2005,[6] and in the United States in September 2006.[5][9] It is available as ageneric medication.[10][11]
Posaconazole is used to treat invasiveAspergillus andCandida infections.[5] It is also used for the treatment oforopharyngeal candidiasis (OPC), including OPC refractory to other drugs such asitraconazole andfluconazole.[5]
Clinical evidence of efficacy in treatment of invasive disease caused byFusarium species (fusariosis) is limited.[12]
Intravenous administration appears to be helpful in amouse model ofnaegleriasis[13] and the drug killsAcanthamoeba castellanii cystsin vitro.[14]
It has been used to treatmucormycosis (black fungus disease) caused byRhizopus mold.[15]
Posaconazole works by disrupting the functions of certainmembrane-bound enzyme systems, thus inhibiting growth of the fungi. It does this by blocking the synthesis and turnover of theeukaryoticcell membrane componentergosterol by inhibiting an enzyme in this pathway known asCYP51. Posaconazole is significantly more potent at binding to CYP51 thanitraconazole.[5][16][17]
Posaconazole is active against the following microorganisms:[16][18]
Posaconazole is absorbed within three to five hours. It is predominantly eliminated through the liver, and has ahalf-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.[5][18]
Media related toPosaconazole at Wikimedia Commons