226700-81-8
226700-81-8 structure
- Name: Fosamprenavir (Calcium Salt)
- Chemical Name: Fosamprenavir calcium
- CAS Number: 226700-81-8
- Molecular Formula: C25H34CaN3O9PS
- Molecular Weight: 623.669
- Catalog: Signaling Pathways Anti-infection HIV
- Create Date: 2018-07-04 15:44:41
- Modify Date: 2024-01-09 22:10:28
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GW433908 is a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, with improved solubility over the parent molecule and a potential for reduced pill burden on current dosing regimens; GW433908G is the calcium salt of the prodrug.IC50 Value:Target: HIV Proteasein vitro: There were no significant changes in buprenorphine or PI plasma levels and no significant changes in medication adverse effects or opioid withdrawal. Increased concentrations of the inactive metabolite buprenorphine-3-glucuronide suggested that darunavir-ritonavir and fosamprenavir-ritonavir induced glucuronidation of buprenorphine[1].in vivo: Fosamprenavir-ritonavir administered with methadone did not alter plasma amprenavir pharmacokinetics compared with historical control data; nor did it alter the unbound R-methadone at 2 and 6 hours after methadone dosing. Pharmacodynamic indexes remained essentially unchanged after adding fosamprenavir-ritonavir to methadone [2]. After a high-fat meal compared with fasting, (1) the bioavailability of GW433908G suspension was decreased by 20% and Cmax by 41%, and (2) for GW433908G tablets, there was no influence on AUC(12% lower Cmax). After a low-fat meal compared with fasting, (1) there was bioequivalence for GW433908G tablets, but (2) bioavailability was decreased by 23% for amprenavir capsules (Cmax was also lower, by 46%) [3].Clinical trial: Study of an Investigational Regimen Including FDA Approved HIV Drugs In HIV-Infected Pediatric Subjects. Phase 2
| Name | Fosamprenavir calcium |
|---|---|
| Synonyms |
Telzir
Lexiva calcium (1R,2S)-1-({[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}methyl)-3-phenyl-2-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)propyl phosphate Carbamic acid, N-[(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-1-(phenylmethyl)-2-(phosphonooxy)propyl]-, (3S)-tetrahydro-3-furanyl ester, calcium salt (1:1) calcium [(3s)-oxolan-3-yl] n-[(2s,3r)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-1-phenyl-3-phosphonatooxy-butan-2-yl]carbamate carbamic acid, [(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-1-(phenylmethyl)-2-(phosphonooxy)propyl]-, (3S)-tetrahydro-3-furanyl ester, calcium salt (1:1) Calcium-(1R,2S)-1-({[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}methyl)-3-phenyl-2-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)propylphosphat Calcium (2R,3S)-1-{[(4-aminophenyl)sulfonyl](isobutyl)amino}-4-phenyl-3-({[(3S)-tetrahydro-3-furanyloxy]carbonyl}amino)-2-butanyl phosphate [(2R,3S)-1-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-[[(3S)-oxolan-3-yl]oxycarbonylamino]-4-phenyl-butan-2-yl]oxyphosphonic acid Fosamprenavir Calcium Salt phosphate de (1R,2S)-1-({[(4-aminophényl)sulfonyl](2-méthylpropyl)amino}méthyl)-3-phényl-2-({[(3S)-tétrahydrofuran-3-yloxy]carbonyl}amino)propyle de calcium Fosamprenavir (Calcium Salt) |
| Description | GW433908 is a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, with improved solubility over the parent molecule and a potential for reduced pill burden on current dosing regimens; GW433908G is the calcium salt of the prodrug.IC50 Value:Target: HIV Proteasein vitro: There were no significant changes in buprenorphine or PI plasma levels and no significant changes in medication adverse effects or opioid withdrawal. Increased concentrations of the inactive metabolite buprenorphine-3-glucuronide suggested that darunavir-ritonavir and fosamprenavir-ritonavir induced glucuronidation of buprenorphine[1].in vivo: Fosamprenavir-ritonavir administered with methadone did not alter plasma amprenavir pharmacokinetics compared with historical control data; nor did it alter the unbound R-methadone at 2 and 6 hours after methadone dosing. Pharmacodynamic indexes remained essentially unchanged after adding fosamprenavir-ritonavir to methadone [2]. After a high-fat meal compared with fasting, (1) the bioavailability of GW433908G suspension was decreased by 20% and Cmax by 41%, and (2) for GW433908G tablets, there was no influence on AUC(12% lower Cmax). After a low-fat meal compared with fasting, (1) there was bioequivalence for GW433908G tablets, but (2) bioavailability was decreased by 23% for amprenavir capsules (Cmax was also lower, by 46%) [3].Clinical trial: Study of an Investigational Regimen Including FDA Approved HIV Drugs In HIV-Infected Pediatric Subjects. Phase 2 |
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| Related Catalog | |
| References |
| Melting Point | 282-284ºC |
|---|---|
| Molecular Formula | C25H34CaN3O9PS |
| Molecular Weight | 623.669 |
| Exact Mass | 623.137939 |
| PSA | 201.57000 |
| LogP | 5.44910 |
| Storage condition | 2-8℃ |