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Fosamprenavir
From Wikipedia, the free encyclopedia
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Fosamprenavir
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| Systematic (IUPAC) name | |
| [(2R,3S)-1-[(4-aminophenyl)sulfonyl-(2-methyl propyl)amino]-3-{[(3S)-oxolan-3-yl]oxycarbonylamino}- 4-phenyl-butan-2-yl]oxyphosphonic acid |
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| Identifiers | |
| CAS number | |
| ATC code | J05 |
| PubChem | |
| Chemical data | |
| Formula | C25H36N3O9PS |
| Mol. mass | 585.608 g/mol 623.700 g/mol (calcium salt) |
| Pharmacokinetic data | |
| Bioavailability | Unknown |
| Protein binding | 90% |
| Metabolism | Hydrolysed to amprenavir and phosphate in GI tract epithelium |
| Half life | 7.7 hours |
| Excretion | Fecal (as metabolites of amprenavir) |
| Therapeutic considerations | |
| Pregnancy cat. |
C (U.S.) |
| Legal status | |
| Routes | Oral |
Fosamprenavir (marketed by GlaxoSmithKline as fosamprenavir calcium, under the trade name Lexiva®) is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. The FDA approved it October 20, 2003. The human body metabolizes fosamprenavir in order to form amprenavir, which is the active ingredient. That metabolization increases the duration that amprenavir is available, making fosamprenavir a slow-release version of amprenavir and thus reducing the number of pills required versus standard amprenavir.
A head-to-head study with lopinavir[1] showed the two drugs to have comparable potency, but patients on fosamprenavir tended to have a higher serum cholesterol. Fosamprenavir's main advantage over lopinavir is that it is cheaper. Although fosamprenavir does not itself require refrigeration, it is usually given with ritonavir which does.
- ^ Eron J Jr, Yeni P, Gathe J Jr, et al. (2006). "The KLEAN study of fosamprenavir-ritonavir versus lopinavir-ritonavir, each in combination with abacavir-lamivudine, for initial treatment of HIV infection over 48 weeks: a randomised non-inferiority trial". Lancet 368: 476–82. doi:10.1016/S0140-6736(06)69155-1.
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