Medical Advocates
Darunavir (Prezista/TMC-114)
  Journal Citations

General Reports
Pharmacokinetics
 Viral Dynamics
 Drug/Drug Interactions
Resistance
Efficacy
Diagnostics/Monitoring
Therapeutic Strategies
Economics


 		  
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Last Update:  October 07, 2008 
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General Reports
 
 
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
 
New therapeutic agents in the management of HIV: an overview of darunavir for clinicians
Rotty J, Hoy J.
Sex Health. 2008 Sep;5(3):235-41.
 Abstract
 
A potent HIV protease inhibitor, darunavir, does not inhibit ZMPSTE24 or lead to
an accumulation of farnesyl-prelamin A in cells.
Coffinier C, Hudon SE, Lee R, et al  
J Biol Chem. 2008 Jan 28
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Conformational Analysis of TMC114, a Novel HIV-1 Protease Inhibitor.
Nivesanond K, Peeters A, Lamoen D, Alsenoy CV. 
J Chem Inf Model. 2008 Jan 4
Abstract
 
Binding kinetics of darunavir to HIV-1 protease explain the potent antiviral activity and
high genetic barrier.
Dierynck I, De Wit M, Gustin E, et al 
J Virol. 2007 Oct 10;
Abstract
 
Darunavir: A Nonpeptidic Antiretroviral Protease Inhibitor.
McCoy C.
Clin Ther. 2007 Aug;29(8):1559-1576.
 Abstract
 
The validation of plasma darunavir concentrations determined by the HPLC method for protease
inhibitors.
Takahashi M, Kudaka Y, Okumura N, et al
Biol Pharm Bull. 2007 Oct;30(10):1947-9.
 Abstract
 
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.
Ghosh AK, Dawson ZL, Mitsuya H. 
Bioorg Med Chem. 2007 Sep 14;
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Darunavir: a second-generation protease inhibitor.
Busse KH, Penzak SR.
Am J Health Syst Pharm. 2007 Aug 1;64(15):1593-602
 Abstract
 
Darunavir (TMC114): a new HIV-1 protease inhibitor.
Molina JM, Hill A.
Expert Opin Pharmacother. 2007 Aug;8(12):1951-1964.
 Abstract
 
Analysis of Treatment Costs for HIV RNA Reductions and CD4 Increases for Darunavir
Versus Other Antiretrovirals in Treatment-Experienced, HIV-Infected Patients.
Hill AM, Smith C.  
HIV Clin Trials. 2007 May-Jun;8(3):121-31.
 Abstract
 
Darunavir: an overview of an HIV protease inhibitor developed to overcome drug resistance.
Taiwo BO, Hicks CB. 
AIDS Read. 2007 Mar;17(3):151-6, 159-61.
 Abstract
 
Darunavir (Prezista) for HIV infection.
[No authors listed]
Med Lett Drugs Ther. 2006 Sep 11;48(1243):74-5
Abstract
 
Ultra-high Resolution Crystal Structure of HIV-1 Protease Mutant Reveals Two Binding Sites for
Clinical Inhibitor TMC114
Kovalevsky AY, Liu F, Leshchenko S   
J Mol Biol. 2006 Aug 4;
Abstract

TMC114, a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor Active
against Protease Inhibitor-Resistant Viruses, Including a Broad Range of Clinical Isolates.
De Meyer S, Azijn H, Surleraux D, et al 
Antimicrob Agents Chemother. 2005 Jun;49(6):2314-21.
 Abstract

Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor.
Surleraux DL, Tahri A, Verschueren WG, et al
J Med Chem. 2005 Mar 24;48(6):1813-22.
Abstract
 
Stereoselective photochemical 1,3-dioxolane addition to 5-alkoxymethyl-2(5H)-furanone:
synthesis of bis-tetrahydrofuranyl ligand for HIV protease inhibitor UIC-94017 (TMC-114).
Ghosh AK, Leshchenko S, Noetzel M.
J Org Chem. 2004 Nov 12;69(23):7822-9.
 Abstract
 
FULL-TEXT ARTICLE
Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017
(TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.
Koh Y, Nakata H, Maeda K, et al
Antimicrob Agents Chemother. 2003 Oct;47(10):3123-9
 Abstract
Pharmacokinetics
     
 
Darunavir: pharmacokinetics and drug interactions.
Back D, Sekar V, Hoetelmans RM.  
Antivir Ther. 2008;13(1):1-13.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
The Effect of Different Meal Types on the Pharmacokinetics of Darunavir (TMC114)/Ritonavir
in HIV-Negative Healthy Volunteers.
Sekar V, Kestens D, Spinosa-Guzman S, et al 
J Clin Pharmacol. 2007 Apr;47(4):479-84.
 Abstract

FULL-TEXT ARTICLE
Structural and thermodynamic basis for the binding of TMC114, a next-generation human
immunodeficiency virus type 1 protease inhibitor.
King NM, Prabu-Jeyabalan M, Nalivaika EA, et al
 J Virol. 2004 Nov;78(21):12012-21.
Paper
Viral Dynamics
       
  Darunavir Inhibitory Quotient Predicts the   48-Week Virological Response to Darunavir -Based
Salvage Therapy in HIV-infected Protease Inhibitor- Experienced Adults
Moltó J, Santos JR, Pérez-Álvarez N, Cedeño S, et al
Antimicrob Agents Chemother. 2008 Aug 25
 bstract
Drug/Drug Interactions
     
 
Pharmacokinetic interaction between ethinyl estradiol, norethindrone and darunavir with low-dose ritonavir in
healthy women.
Sekar VJ, Lefebvre E, Guzman SS, et al  
Antivir Ther. 2008;13(4):563-9.Li
 abstract
 
A WEEK IN REVIEW FEATURED REPORT
Effect of Repeated Doses of Darunavir plus Low-Dose Ritonavir on the Pharmacokinetics of Sildenafil
in Healthy Male Subjects:Phase I Randomized, Open-Label, Two-Way Crossover Study.
Sekar V, Lefebvre E, De Marez T, et al 
Clin Drug Investig. 2008;28(8):479-485.
 Abstract
 
Darunavir: pharmacokinetics and drug interactions.
 Back D, Sekar V, Hoetelmans RM.  
 Antivir Ther. 2008;13(1):1-13.
 Abstract
 
Pharmacokinetic Interaction Between Darunavir and Saquinavir in HIV-negative Volunteers.
Sekar VJ, Lefebvre E, Mariën K, et al 
Ther Drug Monit. 2007 Dec;29(6):795-801.
 Abstract
 
Pharmacokinetic interaction between TMC114/r and efavirenz in healthy volunteers.
Sekar VJ, De Pauw M, Mariën K,  et al
Antivir Ther. 2007;12(4):509-14
 Abstract
 
Pharmacokinetic interaction between TMC114/ritonavir and tenofovir disoproxil fumarate in
healthy volunteers.
Hoetelmans RM, Mariën K, De Pauw M, et al 
Br J Clin Pharmacol. 2007 Jul 4;
Abstract

Pharmacokinetic interaction between TMC114/r and omeprazole or ranitidine in HIV-negative
healthy volunteers.
Sekar VJ, Lefebvre E, De Paepe E, et al
Antimicrob Agents Chemother. 2007 Jan 8;
 Abstract

Resistance
     
 
A WEEK IN REVIEW FEATURED REPORT
Resilience to Resistance of HIV-1 Protease Inhibitors: Profile of Darunavir.
Lefebvre E, Schiffer CA. 
AIDS Rev. 2008 Jul-Sep;10(3):131-42.
 Abstract
 
Pattern and impact of emerging resistance mutations in treatment experienced patients failing
darunavir-containing regimen.
Delaugerre C, Pavie J, Palmer P, et al
AIDS. 2008 Aug 7.
 Abstract
 
Resistance Profile of Darunavir: Combined 24-Week Results from the POWER Trials.
De Meyer S, Vangeneugden T, Van Baelen B, et al 
AIDS Res Hum Retroviruses. 2008 Mar 7
 Abstract
 
A WEEK IN REVIEW FEATURED REPORT
 Evidence for different susceptibility to tipranavir and darunavir in patients infected with
distinct HIV-1 subtypes.
Poveda E, de Mendoza C, Parkin N, et al 
AIDS. 2008 Mar 12;22(5):611-6.
 Abstract
 
Factors associated with the selection of mutations conferring resistance to protease inhibitors in
PI-experienced patients displaying treatment failure on darunavir.
Lambert-Niclot S, Flandre P, et al
Antimicrob Agents Chemother. 2007 Nov 26;
 Abstract
 
Prevalence of darunavir resistance-associated mutations: patterns of occurrence and
association with past treatment.
Mitsuya Y, Liu TF, Rhee SY, et al 
J Infect Dis. 2007 Oct 15;196(8):1177-9
 Abstract
 
A WEEK IN REVIEW FEATURED PROFILE
Screening and selecting for optimized antiretroviral drugs: rising to the challenge of
drug resistance.[TMC-114]
de Bethune MP, Hertogs K.
Curr Med Res Opin. 2006 Dec;22(12):2603-12.
 Abstract

Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug
resistant mutations D30N, I50V, and L90M.
Kovalevsky AY, Tie Y, Liu F, et al
J Med Chem. 2006 Feb 23;49(4):1379-87.
 Abstract
Efficacy
     
 
Structural Evidence for Effectiveness of Darunavir and Two Related Antiviral Inhibitors against HIV-2 Protease.
Kovalevsky AY, Louis JM, Aniana A, et al
J Mol Biol. 2008 Sep 20.
Abstract
 
A WEEK IN REVIEW FEATURED REPORT
Efficacy of Once-Daily Darunavir/Ritonavir 800/100 mg in HIV-Infected, Treatment-Experienced Patients
With No Baseline Resistance-Associated Mutations to Darunavir.
De Meyer SM, Spinosa-Guzman S, Vangeneugden TJ, et al 
 J Acquir Immune Defic Syndr. 2008 Sep 2.
Abstract
 
Efficacy and safety of once-daily darunavir/ritonavir versus lopinavir/ritonavir in treatment-naive
HIV-1-infected patients at week 48.
Ortiz R, Dejesus E, Khanlou H, Voronin E, et al
AIDS. 2008 Jul 31;22(12):1389-1397.
 Abstract
 
Follow-up of a multi-drug resistant HIV-1 infected patient successfully treated with darunavir and etravirine.
Audelin AM, Lebech AM, Petersen AB, Jørgensen LB.  
J Med Virol. 2008 Aug;80(8):1319-21.
 Abstract
 
Follow-up of a multi-drug resistant HIV-1 infected patient successfully treated with darunavir and etravirine.
Audelin AM, Lebech AM, Petersen AB, Jørgensen LB.  
J Med Virol. 2008 Jun 12;80(8):1319-1321.
Abstract
 
Virological response to darunavir/ritonavir-based regimens in antiretroviral-experienced patients
(PREDIZISTA study).
Pellegrin I, Wittkop L, Joubert LM, et al
Antivir Ther. 2008;13(2):271-9.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Experience with darunavir in HIV-infected adults enrolled in a US expanded access program:
results from a single center.
Gathe J. 
Curr Med Res Opin. 2008 Jan 29
 Abstract
 
Safety, Tolerability, and Efficacy of Darunavir (TMC114) with Low-Dose Ritonavir in
Treatment-Experienced, Hepatitis B or C Co-infected Patients in POWER 1 and 3.
Rachlis A, Clotet B, Baxter J, et al 
HIV Clin Trials. 2007 Jul-Aug;8(4):213-20.
 Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Safety and Efficacy of Darunavir (TMC114) With Low-Dose Ritonavir in Treatment-Experienced
Patients: 24-Week Results of POWER 3.
 Molina JM, Cohen C, Katlama C, et al 
J Acquir Immune Defic Syndr. 2007 Jul 5;
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
 Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks
in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial.
 Madruga JV, Berger D, McMurchie M, et al 
Lancet. 2007 Jul 7;370(9581):49-58.
 Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Prediction of clinical benefits of ritonavir-boosted TMC114 from treatment effects on CD4 counts
and HIV RNA.
 Hill A, Montaner J, Smith C. HIV Med. 2007 May;8(4):234-40.
 Abstract
 
Week 24 efficacy and safety of TMC114/ritonavir in treatment-experienced HIV patients.
Haubrich R, Berger D, Chiliade P, et al  
AIDS. 2007 Mar 30;21(6):F11-F18.
 Abstract
 
Efficacy and safety of TMC114/ritonavir in treatment-experienced HIV patients:
24-week results of POWER 1
Katlama C, Esposito R, Gatell JM, et al
AIDS. 2007 Feb 19;21(4):395-402.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Successful rescue therapy with darunavir (TMC114) in HIV-infected patients who have failed several
ritonavir-boosted protease inhibitors.
Poveda E, Blanco F, Garcia-Gasco P, et al
 AIDS 2006 Jul 13;20(11):1558-60.
 Abstract

MC114/ritonavir substitution for protease inhibitor(s) in a non-suppressive antiretroviral
regimen: a 14-day proof-of-principle trial.
Arasteh K, Clumeck N, Pozniak A, et al   
AIDS. 2005 Jun 10;19(9):943-94
 Abstract
Diagnostics/Monitoring
     
 
HPLC-MS method for the simultaneous quantification of the new HIV protease inhibitor
darunavir, and 11 other antiretroviral agents in plasma of HIV-infected patients.
D'Avolio A, Siccardi M, Sciandra M, et al 
J Chromatogr B Analyt Technol Biomed Life Sci. 2007 Oct 7;
Abstract
 
FULL TEXT PDF ARTICLE
 The validation of plasma darunavir concentrations determined by the HPLC method for
protease inhibitors.
Takahashi M, Kudaka Y, Okumura N, et al  
Biol Pharm Bull. 2007 Oct;30(10):1947-9
 Paper
 
Quantification of darunavir (TMC114) in human plasma by high-performance liquid
chromatography with ultra-violet detection.
Goldwirt L, Chhun S, Rey E, et al
J Chromatogr B Analyt Technol Biomed Life Sci. 2007 Jul 22;
 Abstract
 
Fast and simultaneous determination of darunavir and eleven other antiretroviral drugs for
therapeutic drug monitoring: method development and validation for the determination of all
currently approved HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors
in human plasma by liquid chromatography coupled with electrospray ionization tandem mass
spectrometry.
Ter Heine R, Alderden-Los CG
Rapid Commun Mass Spectrom. 2007 Jul 3;21(15):2505-2514
Abstract
Therapeutic Strategies
     
  Darunavir: after multiple antiretroviral treatment failure: another option.
[No authors listed] 
Prescrire Int. 2008 Jun;15(33):109.
 Abstract
Economics
     
  Analysis of Costs by CD4 Count Category for the Darunavir/r 600/100 mg bid and Control
ProteaseInhibitor Arms of the POWER 1 and 2 Trials.
Hill A, Hemmett L, Wilson B.
HIV Clin Trials. 2007 Sep-Oct;8(5):303-10.
 Abstract

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Darunavir (Prezista/TMC114)  Journal Citations