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Amprenavir
drug data and news
Amprenavir drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Amprenavir | ||
| Brand Names/Synonyms | 141w94, Kvx-478, Agenerase, Prozei,; Agenerase; Amprenavir; Lexiva; VX-478 | ||
| Indication | For the treatment of HIV-1 infection in combination with other antiretroviral agents | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Amprenavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Amprenavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs. | ||
| Mechanism Of Action | Amprenavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. | ||
| Amprenavir News (When available) |
Boehringer Ingelheim Announces 48-week Results from Aptivus ... Feb 10, 2006 CROI: Tenofovir and kidney toxicity - low rates seen, but some ... Feb 9, 2006 CROI: etravirine (TMC125) and darunavir (TMC114) in treatment ... Feb 13, 2006 Multi-component drug delivery system: An emerging trend Feb 8, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... 09 Feb 2006 CROI: Tenofovir and kidney toxicity - low rates seen, but some ... 09 Feb 2006 Multi-component drug delivery system: An emerging trend Feb 8, 2006 Lexiva for the treatment of HIV infection in adults in combination ... Jan 19, 2006 Tipranavir continues to show benefit in treatment-experienced ... Nov 30, 2005 FDA Approves Updated Labeling for LEXIVA Nov 18, 2005 Procyon reports new data for its lead HIV protease inhibitor, PPL ... Nov 16, 2005 APTIVUS(R) Sustains Convincing Anti-HIV Nov 21, 2005 Once-daily boosted saquinavir has low blood levels when used with ... Nov 11, 2005 Boehringer Ingelheim Announces 48-Week Results from Aptivus(R) ... Nov 21, 2005 Solubilising excipient gets green light in Japan Sep 26, 2005 Tipranavir, a powerful treatment option for HIV-positive treatment ... Jul 31, 2005 Study Results Presented on Pharmacokinetics of Once-Daily HIV ... Jul 26, 2005 IAS: Have we prematurely discarded triple NRTI regimens? Jul 27, 2005 FDA approves new anti-HIV drug Aptivus® for use in combination ... Jun 25, 2005 Lipid-lowering drugs more effective than switch to NNRTI in ... Jun 16, 2005 FDA approves new anti-HIV drug Aptivus® for use in combination ... Jun 25, 2005 Lipid-lowering drugs more effective than switch to NNRTI in ... Jun 16, 2005 Taking liver-taxing drugs calls for periodic testing Apr 5, 2005 Antiretroviral Drug Interactions: An Expert Interview With Corky ... Mar 7, 2005 COMUNICADO DE BOEHRINGER INGELHEIM GMBH (1) Feb 27, 2005 Tipranavir superior to other PIs in detailed resistance analysis Feb 28, 2005 | ||
| Dosage Forms | CAPSULE | ||
| Drug_Category | Anti-HIV Agents; Antibiotics; Anti-HIV Agents; ATC:J05AE05; ATC:J05AE07 | ||
| Absorption | Not Available | ||
| Interactions | Interactions for Amprenavir: Amprenavir is metabolized in the liver by the cytochrome P450 enzyme system. Amprenavir inhibits CYP3A4. Caution should be used when coadministering medications that are substrates, inhibitors, or inducers of CYP3A4, or potentially toxic medications that are metabolized by CYP3A4. Amprenavir does not inhibit CYP2D6, CYP1A2, CYP2C9, CYP2C19, CYP2E1, or uridine glucuronosyltransferase (UDPGT). HIV Protease Inhibitors: The effect of amprenavir on total drug concentrations of other HIV protease inhibitors in subjects receiving both agents was evaluated using comparisons to historical data. Indinavir steady-state Cmax, A.C. and Cmin were decreased by 22%, 38%, and 27%, respectively, by concomitant amprenavir. Similar decreases in Cmax and AUC were seen after the first dose. Saquinavir steady-state Cmax, A.C. and Cmin were increased 21%, decreased 19%, and decreased 48%, respectively, by concomitant amprenavir. Nelfinavir steady-state Cmax, A.C. and Cmin were increased by 12%, 15%, and 14%, respectively, by concomitant amprenavir. Methadone: Coadministration of amprenavir and methadone can decrease plasma levels ofmethadone. Coadministration of amprenavir and methadone as compared to a non-matched historicalcontrol group resulted in a 30%, 27%, and 25% decrease in serum amprenavir AUC, Cmax, andCmin, respectively. Amprenavir is an inhibitor of cytochrome P450 C.P.A. metabolism and therefore should not be administered concurrently with medications with narrow therapeutic windows that are substrates of CYP3A4. There are other agents that may result in serious and/or life-threatening drug interactions. Laboratory Tests: The combination of Amprenavir and low-dose ritonavir has been associated with elevations of cholesterol and triglycerides, SGOT (AST), and SGPT (ALT) in some patients. Appropriate laboratory testing should be considered prior to initiating combination therapy with Amprenavir and ritonavir and at periodic intervals or if any clinical signs or symptoms of hyperlipidemia or elevated liver function tests occur during therapy. For comprehensive information concerning laboratory test alterations associated with ritonavir, physicians should refer to the complete prescribing information for NORVIR (ritonavir). | ||
| Toxicity | Not Available | ||
| Organisms Affected | Human immunodeficiency virus | ||
| Chemical IUPAC Name | tetrahydrofuran-3-yl[3-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-1-benzyl-2-hydroxy-propyl]aminomethanoate | ||
| Chemical Formula | C25H35N3O6S | ||
| Molecular Weight | 505.628 g/mol | ||
| Smiles String | CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2CCOC2)O)S(=O)(=O)C3=CC=C(C=C3)N | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | 2.064 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Not Available | ||
| Half Life | 7.1-10.6 hours | ||
| Protein Binding [%] | 90%. | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Amprenavir.html http://www.rxlist.com/cgi/generic2/ampren.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00605 | ||
| CAS Registry Number | 161814-49-9 | ||
| KEGG Compound ID | C08086 | ||
| PubChem ID | SID:63287 | ||
| PharmGKB ID | PA448422 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2243542 |
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