Posaconazole
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| Trade names | Noxafil, Posanol |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607036 |
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| Routes of administration |
By mouth (oral suspension, delayed-release tablets), IV |
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| Pharmacokinetic data | |
| Bioavailability | High |
| Protein binding | 98 to 99% |
| Metabolism | Liver (glucuronidation) |
| Biological half-life | 16 to 31 hours |
| Excretion | Fecal (71–77%) and renal (13–14%) |
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| Synonyms | 4-{4-[4-(4-{[(5R)-5-(2,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-1-[(2S,3S)-2-hydroxypentan-3-yl]-4,5-dihydro-1H-1,2,4-triazol-5-one |
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| ECHA InfoCard | 100.208.201 |
| Chemical and physical data | |
| Formula | C37H42F2N8O4 |
| Molar mass | 700.778 g/mol |
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Posaconazole is a triazole antifungal drug. It is marketed in the United States, the European Union, and in other countries by Schering-Plough under the trade name Noxafil. In Canada, posaconazole is marketed by Schering-Plough under the trade name Posanol.
It is FDA-approved for the prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as HSCT recipients with GVHD or those with hematologic malignancies with prolonged neutropenia from chemotherapy. It is also used for the treatment of oropharyngeal candidiasis (OPC), including OPC refractory to itraconazole and/or fluconazole therapy.
It is also used to treat invasive infections by Candida, Mucor, and Aspergillus species in severely immunocompromised patients.
Clinical evidence for its utility in treatment of invasive disease caused by Fusarium species (fusariosis) is limited.
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.
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Wikipedia