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| Clinical data | |
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| Trade names | Lexiva, Telzir |
| Other names | Fosamprenavir calcium (USANUS) |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a604012 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | Unknown |
| Protein binding | 90% |
| Metabolism | Hydrolysed toamprenavir andphosphate inGI tractepithelium |
| Eliminationhalf-life | 7.7 hours |
| Excretion | Fecal (as metabolites of amprenavir) |
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| Chemical and physical data | |
| Formula | C25H36N3O9PS |
| Molar mass | 585.61 g·mol−1 |
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Fosamprenavir (FPV), sold under the brand namesLexiva andTelzir, is amedication used to treatHIV/AIDS.[3][4] It is aprodrug of theprotease inhibitor andantiretroviral drugamprenavir.[5] It is marketed byViiV Healthcare as thecalcium salt.[3][4]
Fosamprenavir was approved for medical use in the United States in October 2003,[6] and in the European Union in July 2004.[4] The human body metabolizes fosamprenavir in order to form amprenavir, which is the active ingredient.[3]
A head-to-head study withlopinavir showed the two drugs to have comparable potency, but patients on fosamprenavir tended to have a higher serum cholesterol.[7]
Fosamprenavir is used for the treatment ofHIV-1 infections, typically but not necessarily in combination with low-doseritonavir or other antiviral drugs.[8][9]
The most common adverse effect is diarrhea. Other common side effects includeheadache, dizziness and exanthema, which is usually transient. Severe allergic reactions (Stevens–Johnson syndrome) are rare.[8]
Amprenavir (the active metabolite of fosamrenavir, which is found in blood plasma, liver and other organs) is metabolized via the liver enzymeCYP3A4 and also weakly inhibits this enzyme. This means that combination with drugs that are also metabolized by CYP3A4 can increase their plasma concentrations and thus side effects; and combination with drugs that inhibit CYP3A4 can increase amprenavir concentrations.[8]
When combining fosamprenavir with low doses of the CYP3A4 inhibitor ritonavir, this interaction is intended as it allows for application of lower fosamprenavir doses.[8]
Fosamprenavir is quickly activated to amprenavir, even before it reaches the circulation. Amprenavir is a HIVprotease inhibitor.[8]
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