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Amprenavir (Agenerase)
 
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Last Update:  February 16, 2017
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General Reports
       
 
Repositioning of amprenavir as a novel extracellular signal-regulated kinase-2 inhibitor and apoptosis inducer in MCF-7 human breast cancer.
 Jiang W, Li X, Li T, Wang H,  et al
Int J Oncol. 2017 Jan 24.
Abstract

Joint X-ray/neutron crystallographic study of HIV-1 protease with clinical inhibitor amprenavir - insights for drug design.
 Weber IT, Waltman MJ, Mustyakimov M,  et al
J Med Chem. 2013 Jun 17.
 Abstract

FULL-TEXT ARTICLE
Pregnane X Receptor Mediates Dyslipidemia Induced by the HIV Protease Inhibitor Amprenavir in Mice.
 Helsley RN, Sui Y, Ai N,  et al
Mol Pharmacol. 2013 Mar 21.
 Paper
 

Structural and Thermodynamic Basis of Amprenavir/Darunavir and Atazanavir Resistance in HIV-1 Protease with Mutations at Residue 50.
Mittal S, Bandaranayake RM, King NM, et al
J Virol. 2013 Jan 30.
 Abstract

Amprenavir inhibits the migration in human hepatocarcinoma cell in vitro and the growth of xenografts in vivo.
Esposito V, Verdina A, Manente L, et aL
J Cell Physiol. 2012 Aug 9.
 Abstract

Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.
 Yan J, Huang N, Li S, Yang LM,  et al
Bioorg Med Chem Lett. 2012 Mar 1;22(5):
 Abstract

Solution Kinetics Measurements Suggest HIV-1 Protease Has Two Binding Sites for Darunavir and Amprenavir.
Kovalevsky AY, Ghosh AK, Weber IT. 
J Med Chem. 2008 Sep 20.
 Abstract
 
Effects of ritonavir and amprenavir on insulin sensitivity in healthy volunteers.
 Lee GA, Rao M, Mulligan K, et al
 AIDS. 2007 Oct;21(16):2183-2190.
 Abstract
 
Intraluminal drug and formulation behavior and integration in in vitro permeability estimation:
A case study with amprenavir.
Brouwers J, Tack J, Lammert F, Augustijns P. et al 
J Pharm Sci. 2006 Feb;95(2):372-83.
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Intraluminal drug and formulation behavior and integration in in vitro permeability estimation:
A case study with amprenavir.
 Brouwers J, Tack J, Lammert F, Augustijns P.
J Pharm Sci. 2005 Dec 22;95(2):372-383
 Abstract

FULL-TEXT ARTICLE
 HIV-1 genotype and phenotype correlate with virological response to abacavir, amprenavir and
efavirenz in treatment- experienced patients.
Falloon J, Ait-Khaled M, Thomas DA, et al.
AIDS 2002 Feb 15;16(3):387-396
 Paper

  
Pharmacokinetics
         
 
Population pharmacokinetic modeling and simulation of amprenavir following fosamprenavir/ritonavir administration for dose optimization in HIV infected pediatric patients.
Barbour AM, Gibiansky L, Wire MB.
 J Clin Pharmacol. 2014 Feb;54(2):206-214
 Abstract

Pharmacokinetics of amprenavir in HIV-1 patients with renal insufficiency.
Janus N, Launay-Vacher V, Izzedine H,et al  
Med Mal Infect. 2007 Nov 6;
 Abstract
 
Compartmental Pharmacokinetic Analysis of Oral Amprenavir with Secondary Peaks.
Okusanya O, Forrest A, Difrancesco R, et al 
Antimicrob Agents Chemother. 2007 Feb 5;
Abstract
 
Pharmacokinetic and safety evaluation of high-dose combinations of fosamprenavir and
ritonavir.
Shelton MJ, Wire MB, Lou Y, Adamkiewicz B, Min SS. 
Antimicrob Agents Chemother. 2006 Mar;50(3):928-34.
Abstract
 
Amprenavir and Efavirenz Pharmacokinetics before and after the Addition of Nelfinavir,
Indinavir, Ritonavir, or Saquinavir in Seronegative Individuals.
Morse GD, Rosenkranz S, Para MF 
Antimicrob Agents Chemother. 2005 Aug;49(8):3373-81.
 Abstract
 
Potent antiviral activity of amprenavir in primary macrophages infected by human
immunodeficiency virus.
Aquaro S, Guenci T, Santo FD 
|Antiviral Res. 2004 Feb; 61(2): 133-7
 Abstract

Oxidative Metabolism of Amprenavir in the Human Liver.  Effect of the CYP3A Maturation.
 Treluyer JM, Bowers G, Cazali N, et al.
 Drug Metab Dispos 2003 Mar 1;31(3):275-281
 Abstract

Steady-State Pharmacokinetics of Amprenavir Coadministered with Ritonavir in Human
Immunodeficiency Virus Type 1-Infected Patients.
Goujard C, Vincent I, Meynard JL  
 Antimicrob Agents Chemother 2003 Jan;47(1):118-123
 Abstract

FULL-TEXT ARTICLE
Pharmacokinetic study of human immunodeficiency virus protease inhibitors used in
combination with amprenavir.
Sadler BM, Gillotin C, Lou Y, et al.
Antimicrob Agents Chemother 2001 Dec;45(12):3663-8
Abstract

FULL-TEXT ARTICLE
Pharmacokinetics and safety of amprenavir and ritonavir following multiple-dose, co-administration
to healthy volunteers.
Sadler BM, Piliero PJ, Preston SL, et al. 
AIDS 2001 May 25;15(8):1009-18
 Abstract

FULL-TEXT ARTICLE
Safety and Pharmacokinetics of Amprenavir (141W94), a Human Immunodeficiency Virus (HIV)
Type 1  Protease Inhibitor,  following Oral Administration of Single Doses to HIV-Infected Adults .
Sadler BM, Gillotin C,  Lou Y, Stein DS.
Antimicro Agents Chemother. 2001 Jan;45(1):30-7.
Paper

FULL-TEXT ARTICLE
 Pharmacokinetic and Pharmacodynamic Study of the Human Immunodeficiency Virus Protease
Inhibitor  Amprenavir after  Multiple Oral Dosing.
Sadler BM, Gillotin C, Lou Y, Stein DS.
 Antimicrob Agents Chemother  2001 Jan;45(1):30-37
Paper

 		 
Drug/Srug Interactions
 
 
FULL-TEXT PDF ARTICLE(Link to article on publication site)
 Effect of Fosamprenavir/Ritonavir on the Pharmacokinetics of Dolutegravir in Healthy Subjects.
 Song I, Borland J, Chen S,  et al
Antimicrob Agents Chemother. 2014 Aug 25.
Abstract

 Steady-state amprenavir and tenofovir pharmacokinetics after coadministration of unboosted or
ritonavir-boosted fosamprenavir with tenofovir disoproxil fumarate in healthy volunteers.
Luber A, Condoluci D, Slowinski P, et al  
HIV Med. 2009 Oct 23.
 Abstract

Amprenavir and lopinavir pharmacokinetics following coadministration of amprenavir or
fosamprenavir with lopinavir/ritonavir, with or without efavirenz.
Pham PA, Hendrix CW, Barditch-Crovo P, et al 
Antivir Ther. 2007;12(6):963-9.
Abstract
 
Ritonavir Increases Plasma Amprenavir (APV) Exposure to a Similar Extent when Coadministered with
either Fosamprenavir or APV.
 Wire MB, Baker KL, Jones LS, et al  
 Antimicrob Agents Chemother. 2006 Apr;50(4):1578-80.
 Abstract
 
Pharmacokinetics and pharmacodynamics of methadone enantiomers after coadministration with
amprenavir in opioid-dependent subjects.
Hendrix CW, Wakeford J, Wire MB, et al  
Pharmacotherapy. 2004 Sep;24(9):1110-21.
 Abstract
 
Interactions between amprenavir and the lopinavir-ritonavir combination in heavily pretreated
patients infected with human immunodeficiency virus.
Taburet AM, Raguin G, Le Tiec C, et al 
Clin Pharmacol Ther. 2004 Apr;75(4):310-23
 Abstract

Effects of didanosine formulations on the pharmacokinetics of amprenavir.
Shelton MJ, Giovanniello AA, Cloen D ,et al.
Pharmacotherapy. 2003 Jul;23(7):835-42.
 Abstract

Steady-State Pharmacokinetics of Amprenavir Coadministered with Ritonavir in Human
Immunodeficiency Virus Type 1-Infected Patients.
Goujard C, Vincent I, Meynard JL  
 Antimicrob Agents Chemother 2003 Jan;47(1):118-123
 Abstract

Pharmacokinetic interaction between amprenavir and delavirdine: Evidence of induced clearance
by amprenavir.
Tran JQ, Petersen C, Garrett M, et al.
Clin Pharmacol Ther 2002 Dec;72(6):615-626
 Abstract

FULL-TEXT ARTICLE
Pharmacokinetic modeling and simulations of interaction of amprenavir and ritonavir.
Sale M, Sadler BM, Stein DS.
Antimicrob Agents Chemother 2002 Mar;46(3):746-54
 Abstract

Methadone blood concentrations are decreased by the administration of abacavir plus amprenavir.
Bart PA,  Rizzardi PG, Gallant S et al .
Ther Drug Monit 2001 Oct;23(5):553-5            
Abstract

FULL-TEXT ARTICLE
 Pharmacokinetic Interaction between Amprenavir and Rifabutin or Rifampin in Healthy Males.
Polk RE, Brophy DF, Israel DS, Patron R, et al.
Antimicrob Agents Chemother. 2001 Feb;45(2):502-8.
 Paper

FULL-TEXT ARTICLE
 Pharmacokinetic Interaction between Amprenavir and Clarithromycin in Healthy Male Volunteers.
Brophy DF, Israel DS, Pastor A, et al.
Antimicrob Agents Chemother. 2000 Apr;44(4):978-84.
 Paper

FULL-TEXT ARTICLE
 Use of Drug Effect Interaction Modeling with Monte Carlo Simulation To Examine the Impact of
Dosing Interval on the Projected Antiviral Activity of the Combination of Abacavir and Amprenavir.
Drusano GL, D'Argenio DZ, Preston SL, et al.
Antimicrob Agents Chemother 2000 Jun;44(6):1655-1659
Paper

  
Safety
 
  Safety profile and tolerability of amprenavir in the treatment of adult and pediatric patients  with HIV
infection.
Pedneault L, Brothers C, Pagano G, et al.
Clin Ther 2000 Dec;22(12):1378-94; discussion 1377
Abstract
Viral Dynamics
 
  FULL-TEXT ARTICLE
 Pharmacokinetic and Pharmacodynamic Study of the Human Immunodeficiency Virus Protease |
Inhibitor Amprenavir after Multiple Oral Dosing.
Sadler BM, Gillotin C, Lou Y, Stein DS.
Antimicrob Agents Chemother 2001 Jan;45(1):30-37
 Paper
Resistance
 
 
A Contribution to the Drug Resistance Mechanism of Darunavir, Amprenavir, Indinavir, and Saquinavir Complexes with HIV-1 Protease Due to Flap Mutation I50V: A Systematic MM-PBSA and Thermodynamic Integration Study.
 Leonis G, Steinbrecher TB, Papadopoulos MG.
 J Chem Inf Model. 2013 Jul 8
 Abstract

Energetic basis for drug resistance of HIV-1 protease mutants against amprenavir.
 Kar P, Knecht V.
J Comput Aided Mol Des. 2012 Feb 14
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
 Insights into amprenavir resistance in E35D HIV-1 protease mutation from molecular dynamics and
binding free-energy calculations.
Meiselbach H, Horn AH, Harrer T, Sticht H.
J Mol Model (Online). 2006 Jun 23;
 Abstract
 
Resistance profiles observed in virological failures after 24 weeks of amprenavir/ritonavir containing
regimen in protease inhibitor experienced patients.
Marcelin AG, Affolabi D, Lamotte C, et al  
J Med Virol. 2004 Sep;74(1):16-20.
 Abstract
 
Resistance profiles observed in virological failures after 24 weeks of amprenavir/ritonavir containing
regimen in protease inhibitor experienced patients.
Marcelin AG, Affolabi D, Lamotte C, et al
J Med Virol. 2004 Sep;74(1):16-20.
 Abstract
 
HIV protease mutations associated with amprenavir resistance during salvage therapy: importance
of I54M.
Murphy MD, Marousek GI, Chou S. et al.
J Clin Virol. 2004 May;30(1):62-7
 Abstract
 
HIV susceptibility to amprenavir: phenotype-based versus rules-based interpretations.
Scudeller L, Torti C, Quiros-Roldan E, et al 
J Antimicrob Chemother. 2003 Oct 16
Abstract
 
Non-parametric methods to predict HIV drug susceptibility phenotype from genotype.
Gregory DiRienzo A, DeGruttola V, Larder B, Hertogs K.
 Stat Med. 2003 Sep 15;22(17):2785-98.
 Abstract

Links Improving lopinavir genotype algorithm through phenotype correlations:novel mutation
patterns and amprenavir cross-resistance.
Parkin NT, Chappey C, Petropoulos CJ  
AIDS 2003 May 2;17(7):955-61
 Abstract

Amprenavir-resistant HIV-1 exhibits lopinavir cross-resistance and reduced replication capacity.
Prado JG, Wrin T, Beauchaine J, et al.
AIDS 2002 May 3;16(7):1009-17
 Abstract

FULL-TEXT ARTICLE
 Low Level of Cross-Resistance to Amprenavir (141W94) in Samples from Patients Pretreated
with Other Protease Inhibitors.
Schmidt B, Korn K, Moschik B, et al.
Antimicrob Agents Chemother.  2000 Nov;44(11):3213-6
 Paper

FULL-TEXT ARTICLE
 A Mutation in Human Immunodeficiency Virus Type 1 Protease, N88S, That Causes In Vitro
Hypersensitivity to Amprenavir.
Ziermann R, Limoli K, Das K, Arnold E,
J Virol 2000 May;74(9):4414 - 4419
 Paper

FULL-TEXT ARTICLE
 Structural and Kinetic Analyses of the Protease from an Amprenavir-Resistant Human
Immunodeficiency Virus Type 1 Mutant Rendered Resistant to Saquinavir and Resensitized
to Amprenavir  
Markland W, Rao BG, Parsons JD,  et al
J Virol 2000 Aug;74(16):7636-7641
Paper
Efficacy
 
 
FULL-TEXT ARTICLE
Revealing Origin of Decrease in Potency of Darunavir and Amprenavir against HIV-2 relative to HIV-1 Protease by Molecular Dynamics Simulations.
 Chen J, Liang Z, Wang W,  et al
Sci Rep. 2014 Nov 3;4:6872.
 Paper

Effectiveness and tolerability of a once-daily amprenavir/ritonavir-containing highly active
antiretroviral therapy regimen in antiretroviral-naive patients at risk for nonadherence: 48-week
results after 24 weeks of directly observed therapy.
Jayaweera D, Kolber M, Brill M,et al
HIV Med. 2004 Sep;5(5):364-370.
 Abstract
 
A 42-Week Open-Label Study to Assess the Pharmacokinetics, Antiretroviral Activity,
and Safety of Amprenavir or Amprenavir plus Ritonavir in Combination with Abacavir and
Lamivudine for Treatment of HIV-Infected Patients.
Wood R, Eron J, Arasteh K, Teofilo E, et al  
Clin Infect Dis. 2004 Aug 15;39(4):591-4.
Abstract
 
A randomized study investigating the efficacy and safety of amprenavir in combination with
low-dose ritonavir in protease inhibitor-experienced HIV-infected adults.
Pulido F, Katlama C, Marquez M, et al
HIV Med. 2004 Jul;5(4):296-3
 Abstract
 
A prospective, controlled study assessing the effect of lopinavir on amprenavir concentrations
boosted by ritonavir.
Mauss S, Scholten S, Wolf E, et al 
HIV Med. 2004 Jan; 5(1): 15-7.
Abstract
 
Six-week randomized controlled trial to compare the tolerabilities, pharmacokinetics, and antiviral
activities of GW433908 and amprenavir in human immunodeficiency virus type 1-infected patients.
Wood R, Arasteh K, Stellbrink HJ, et al 
Antimicrob Agents Chemother. 2004 Jan;48(1):116-23.
 Abstract
 
Potent antiviral activity of amprenavir in primary macrophages infected by human
immunodeficiency virus.
Aquaro S, Guenci T, Santo FD, et al.
 Antiviral Res. 2004 Feb;61(2):133-7.
 Abstract
 
In vitro-in vivo model for evaluating the antiviral activity of amprenavir in combination with
ritonavir administered at 600 and 100 milligrams, respectively, every 12 hours.
Preston SL, Piliero PJ, Bilello JA, et al   
 Antimicrob Agents Chemother. 2003 Nov;47(11):3393-9
 Abstract
 
FULL-TEXT PDF ARTICLE
 Twice-daily Amprenavir 1200mg versus Amprenavir 600mg/Ritonavir 100mg, in combination
with at least 2 other antiretroviral drugs in HIV-1 infected patients.
Nadler JP, Gathe JC Jr, Pollard RB Jr, et al.
BMC Infect Dis. 2003 Jun 10
PDF Paper

The pharmacokinetics of Amprenavir, Zidovudine, and Lamivudine in the genital tracts of men infected
with human immunodeficiency virus type 1 (AIDS clinical trials group study 850).
Pereira AS, Smeaton LM, Gerber JG, et al.
J Infect Dis 2002 Jul 15;186(2):198-204
 Abstract

FULL-TEXT ARTICLE
HIV-1 genotype and phenotype correlate with virological response to abacavir, amprenavir and
efavirenz in treatment- experienced patients.
Falloon J, Ait-Khaled M, Thomas DA, et al.
AIDS 2002 Feb 15;16(3):387-396
 Paper

Human immunodeficiency virus type 1 hypersusceptibility to amprenavir in vitro can be
associated  with virus load response to treatment in vivo.
Zachary KC, Hanna GJ, D'Aquila RT.
Clin Infect Dis 2001 Dec 15;33(12):2075-7
 Abstract

FULL-TEXT ARTICLE
 Single-Dose Pharmacokinetics of Amprenavir, a Human Immunodeficiency Virus Type 1 
Protease Inhibitor, in Subjects with Normal or Impaired Hepatic Function.
Veronese L, Rautaureau J, Sadler BM, et al.
Antimicrob Agents Chemother 2000 Apr;44(4):821-826
 Paper

  
Adverse Events
 
 
Effect of the HIV protease inhibitor amprenavir on the growth and differentiation of
primary gingival epithelium.
Israr M, Mitchell D, Alam S,  et al
Antivir Ther. 2010;15(2):253-65.
 Abstract

Same patient, new stone composition: amprenavir urinary stone.
Feicke A, Rentsch KM, Oertle D, Strebel RT.
Antivir Ther. 2008;13(5):733-4.
 Abstract
 
Amprenavir-induced maculopapular exanthem followed by desensitization in a patient with late-stage
human immunodeficiency virus.
Kohli-Pamnani A, Huynh P, Lobo F.  
Ann Allergy Asthma Immunol. 2006 Apr;96(4):620-3.
 Abstract

Possible linkage of amprenavir with intracranial bleeding in an HIV-infected hemophiliac.
 Kodoth S, Bakshi S, Scimeca P, Black K, Pahwa S.
 AIDS Patient Care STDS 2001 Jul;15(7):347-52
 Abstract
Diagnostics/Monitoring
 
 
A liquid chromatography-tandem mass spectrometry assay for quantification of nevirapine,
indinavir, atazanavir, amprenavir, saquinavir, ritonavir, lopinavir, efavirenz, tipranavir, darunavir
and maraviroc in the plasma of patients infected with HIV.
 Martin J, Deslandes G, Dailly E, et al 
J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Aug 3
 Abstract

Predictive value of the HIV phenotype and genotype and of amprenavir and lopinavir inhibitory
quotients in heavily pretreated patients on a ritonavir-boosted dual protease inhibitor regimen.
Barrail-Tran A, Morand-Joubert L, Poizat G, et al 
Antimicrob Agents Chemother. 2008 Feb 19
Abstract
 
Determination of abacavir, amprenavir, didanosine, efavirenz, nevirapine, and stavudine concentration
in human plasma by MALDI-TOF/TOF.
 Notari S, Mancone C, Alonzi T, et al  
J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jan 16
Abstract
 
Development and evaluation of an immunoassay for the monitoring of the anti-HIV drug amprenavir.
Bastiani E, Benedetti F, Berti F, et al
 J Immunol Methods. 2007 Jun 14;
Abstract

Determination of amprenavir total and unbound concentrations in plasma by high-performance
liquid chromatography and ultrafiltration.
Barrail A, Tiec CL, Paci-Bonaventure S, et al
Ther Drug Monit. 2006 Feb;28(1):89-94.
 Abstract
Therapeutic Strategies
 
Salvage Therapy
 
 
Salvage Therapy with Ritonavir-Boosted Amprenavir/Fosamprenavir: Virological and
Immunological Response in Two Years Follow-up.
 Quercia R, Garnier E, Ferre V, Morineau P, et al
 HIV Clin Trials. 2005 Mar-Apr;6(2):73-80.
Abstract
 
The Pharmacokinetics, Safety, and Initial Virologic Response of a Triple-Protease Inhibitor
Salvage Regimen Containing Amprenavir, Saquinavir, and Ritonavir.
Corbett AH, Eron JJ, Fiscus SA ,et al 
J Acquir Immune Defic Syndr. 2004 Aug 1;36(4):921-928
 Abstract
 
Efficacy, safety and predictive factors of virological success of a boosted amprenavir-based
salvage regimen in heavily antiretroviral-experienced HIV-1-infected patients.
Clevenbergh P, Boulme R, Kirstetter M, Dellamonica P.
HIV Med. 2004 Jul;5(4):284-8.
Abstract
 
Deep Salvage With Amprenavir and Lopinavir/Ritonavir: Correlation of Pharmacokinetics
and Drug Resistance With Pharmacodynamics.
De Luca A, Baldini F, Cingolani A 
J Acquir Immune Defic Syndr. 2004 Apr 20;35(4):359-366.
 Abstract

HIV protease mutations associated with amprenavir resistance during salvage therapy:
importance of I54M.
Murphy MD, Marousek GI, Chou S. et al.
J Clin Virol. 2004 May;30(1):62-7
 Abstract
 
  Salvage therapy with amprenavir and ritonavir: Prospective study in 17 heavily pretreated
patients.
 Arvieux C, Tattevin P, Souala FM, et al .
 HIV Clin Trials 2002 Mar-Apr;3(2):125-32
 Abstract 
 
  FULL-TEXT ARTICLE
 Amprenavir Inhibitory Quotient and Virological Response in Human Immuno- deficiency 
Virus-Infected Patients on an Amprenavir-Containing Salvage Regimen without or with
Ritonovir
 Duval X, Lamotte C, Race E, et al.
Antimicrob Agents Chemother 2002 Feb;46(2):570-4
 Abstract

 
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