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Darunavir (Prezista/TMC-114)
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Last Update:  April 02, 2015 
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Animal Studies
 

  Hepatobiliary and intestinal elimination of darunavir in an integrated preclinical rat model.
Stappaerts J, Fattah S, Annaert P, Augustijns P.
Xenobiotica. 2013 Nov 26
Abstract

Dosage
 

  Monotherapy with boosted PIs as an ART simplification strategy in clinical practice.
Santos JR, Llibre JM, Berrio-Galan D, et al
J Antimicrob Chemother. 2014 Dec 18
Abstract

Efficacy of a reduced dose of Darunavir/RTV in a cohort of antiretroviral-naïve and experienced HIV-infected patients: a medium-term follow-up.
Lanzafame M, Lattuada E, Rigo F, Hill A, Vento S
J Int AIDS Soc
. 2014 Nov 2;17(4(Suppl 3)):
Abstract

Bioavailability and bioequivalence of a darunavir 800-mg tablet formulation compared with the 400-mg tablet formulation.
Kakuda TN, Leopold L, Timmers M, et al
Int J Clin Pharmacol Ther
.
2014 Sep;52(9):805-16.

Abstract


General Reports
 

 

Antiviral activity and CSF concentrations of 600/100 mg of darunavir/ritonavir once daily in HIV-1 patients with plasma viral suppression.
Di Yacovo MS, Moltó J, Ferrer E,  et al

J Antimicrob Chemother
. 2015 Jan 20.
Abstract

Randomized trial of DRV/r or LPV/r QD monotherapy vs maintaining a PI/r-based antiretroviral regimen in persons with suppressed HIV replication.
Pinnetti C, Lorenzini P, Cozzi-Lepri A, et al

J Int AIDS Soc
. 2014 Nov 2;17(4(Suppl 3)):19809
Abstract

Dimerization of HIV-1 protease occurs through two steps relating to the mechanism of protease dimerization inhibition by darunavir.
Hayashi H, Takamune N, Nirasawa T, et al

Proc Natl Acad Sci U S A
. 2014 Aug 4.

Abstract

Lack of mitochondrial toxicity of darunavir, raltegravir and rilpivirine in neurons and hepatocytes: a comparison with efavirenz.
Blas-García A, Polo M, Alegre F, et al
 J
Antimicrob Chemother
. 2014 Jul 9
Abstract

Evaluation of Atazanavir and Darunavir Interactions with Lipids for Developing pH-Responsive Anti-HIV Drug Combination Nanoparticles.
Duan J, Freeling JP, Koehn J,  et al 

J Pharm Sci
. 2014 Jun 19.
Abstract

Structures of Darunavir-Resistant HIV-1 Protease Mutant Reveal Atypical Binding of Darunavir to Wide Open Flaps.
Zhang Y, Chang YC, Louis JM, et al
 
ACS Chem Biol
. 2014 Apr 16.
Abstract

Investigation on the mechanism for the binding and drug resistance of wild type and mutations of G86 residue in HIV-1
protease complexed with Darunavir by molecular dynamic simulation and free energy calculation.

Li D, Zhang Y, Zhao RN,  et al

J Mol Model
. 2014 Feb;20(2):2122.
Abstract

Cellular HIV reservoir replenishment is not affected by blip or intermittent viremia episodes during darunavir/ritonavir
monotherapy.

Torres-Cornejo A, Benmarzouk-Hidalgo OJ, Gutiérrez-Valencia A, et al
AIDS
. 2013 Dec 19
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Interindividual and Intraindividual Variability’s of Darunavir and Ritonavir Plasma Trough Concentrations in Multidrug Experienced HIV Patients Receiving Salvage Regimens.
Baroncelli S, Villani P, Galluzzo CM,, et al 
Ther Drug Monit
. 2013 Sep 20.
Abstract

Determination of P-glycoprotein surface expression and functional ability after in vitro treatment with darunavir or raltegravir in lymphocytes of healthy donors.
Tempestilli M, Gentilotti E, Tommasi C,  et al

Int Immunopharmacol
. 2013 May 23
Abstract

GAM analysis of the relationship between DRV PK and pharmacodynamics following DRV/r 800/100 mg qd in the phase III trials ARTEMIS and ODIN.
Kakuda T, Tomaka F, Van De Casteele T, Vangeneugden T. 

J Int AIDS Soc
. 2012 Nov 11;15(6):18338.
Abstract

No change of plasma darunavir concentrations by switching from ritonavir soft capsule to tablet.
Shibata M, Takahashi M, Fukushima N, et al
J Int AIDS Soc. 2012 Nov 11;15(6):18360.
Abstract

Darunavir plasma level in HIV overweight patients.
Poupard M, Boussairi A, Krause J, Khuong-Josses M.
J Int AIDS Soc
. 2012 Nov 11;15(6):18359.

Abstract

Darunavir is predominantly unbound to protein in cerebrospinal fluid and concentrations exceed the wild-type HIV-1 median 90% inhibitory concentration.
Croteau D, Rossi SS, Best BM,  et al 

J Antimicrob Chemother
. 2012 Nov 9
Abstract

Darunavir: A Critical Review of Its Properties, Use and Drug Interactions.
Ruela Corrêa JC, D’Arcy DM, Dos Reis Serra CH,  et al

Pharmacology
. 2012 Jul 12;90(1-2):102
Abstract

Single and Multiple Dose Pharmacokinetics of Darunavir plus Ritonavir and Etravirine
in Semen and Rectal Tissue of HIV-Negative Men.
Brown KC, Patterson KB, Jennings SH,

J Acquir Immune Defic Syndr
. 2012 May 18.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Determinants of darunavir cerebrospinal fluid concentrations: impact of once-daily dosing and
pharmacogenetics.
Calcagno A, Yilmaz A, Cusato J, et al
AIDS. 2012 May 2.
Abstract

Origin of Decrease in Potency of Darunavir and Two Related Antiviral Inhibitors Against HIV2
Compared to HIV1 Protease.
Kar P, Knecht V

J Phys Chem B
. 2012 Jan 26.
Abstract

Effects of darunavir/ritonavir-based therapy on metabolic and anthropometric parameters in women and
men over 48 weeks.
Currier JS, Martorell C, Osiyemi O, et al
AIDS Patient Care STDS. 2011 Jun;25(6):333-40.
Abstract

Positive Impact of HIV-1 Gag Cleavage Site Mutations on Virological Response to Darunavir
Boosted with Ritonavir.
Larrouy L, Lambert-Niclot S, Charpentier C, Fourati S,  t al
Antimicrob Agents Chemother. 2011 Jan 31
Abstract

Darunavir concentrations exceed the protein-corrected EC50 for wild-type HIV in the semen of
HIV-1-infected men.
Taylor S, Jayasuriya AN, Berry A, Gilleran G,
et al
AIDS
. 2010 Aug 25
Abstract

800 mg Darunavir tablets prepared by hot melt extrusion.
Thommes M, Baert L, Rosier J.
Pharm Dev Technol. 2010 Aug 23.
Abstract

Low frequency of intermittent HIV-1 semen excretion in patients treated by darunavir/ritonavir (
600/100 mg BID) + 2 nucleoside reverse transcriptase inhibitors or monotherapy.
Lambert-Niclot S, Peytavin G, Duvivier C, et al
Antimicrob Agents Chemother. 2010 Aug 16
Abstract

Trends in uptake of recently approved antiretrovirals within a national healthcare system.
Belperio P, Mole L, Boothroyd D, Backus L.
HIV Med
. 2009 Oct 23.
Abstract

Intracellular ‘boosting’ of darunavir using known transport inhibitors in primary PBMC.
Kwan WS, Janneh O, Hartkoorn R,  et al 
Br J Clin Pharmacol. 2009 Sep;68(3):375-80
Abstract

New antiretroviral drugs: a review of the efficacy, safety, pharmacokinetics, and resistance profile
of tipranavir, darunavir, etravirine, rilpivirine, maraviroc, and raltegravir.
Hughes CA, Robinson L, Tseng A, Macarthur RD.
Expert Opin Pharmacother. 2009 Aug 13.
Abstract

Identification of new genotypic cut-off levels to predict the efficacy of lopinavir/ritonavir and
darunavir/ritonavir in the TITAN trial.
Hill A, Marcelin AG, Calvez V. 
HIV Med
. 2009 Jul 6.
Abstract

 

Darunavir Concentrations in Cerebrospinal Fluid and Blood in HIV-1-Infected Individuals.
Yilmaz A, Izadkhashti A, Price RW, et al  
AIDS Res Hum Retroviruses. 2009 Mar 26.
Abstract
 
Improved bioavailability of darunavir by use of kappa-carrageenan versus microcrystalline cellulose
as pelletisation aid.

Thommes M, Baert L, Van’t Klooster G, et al
Eur J Pharm Biopharm. 2009 Mar 19.
Abstract
 
Role of tenofovir in HIV and hepatitis C virus coinfection.
Tuma P, Vispo E, Barreiro P, Soriano V.
Enferm Infecc Microbiol Clin. 2008 Jun;26(Supl.8):31-37
Abstract

 
Chemical characteristics, mechanism of action and antiviral activity of darunavir.
Pasquau Liaño J, Hidalgo Tenorio C.
Enferm Infecc Microbiol Clin. 2008 Oct;26(Supl.10):3-9
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
 
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

Safety