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Last Update:  February 05, 2018
 
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New and Noteworthy
 

February 2018

 


General/Miscellaneous Reports
 

     Journal Papers, Abstracts, and Commentaries
 
 
Ligand Binding Pathways and Conformational Transitions of the HIV Protease.
Miao Y, Huang YM, Walker RC, et al

Biochemistry
. 2018 Feb 2
Abstract

Long-term effectiveness of recommended boosted protease inhibitor-based antiretroviral therapy in Europe.
Santos JR, Cozzi-Lepri A, Phillips A,  et al

HIV
Med
. 2018 Feb 1.
Abstract

HHV8 and Kaposi's sarcoma: should we really give up protease inhibitors in all HIV-infected patients?
Philibert P, Chiche L, Caillères S, et al

AIDS
. 2017 Jul 7.
Abstract

Insight into Binding Mechanisms of Inhibitors MKP56, MKP73, MKP86 and MKP97 to HIV-1 Protease by Using Molecular Dynamics Simulation
Shi S, Zhang S, Zhang Q.
J Biomol Struct Dyn. 2017 Mar 9:1-43
Abstract

Strategic use of dual regimens of boosted protease inhibitors plus maraviroc in poorly adherent subjects in view of long-acting drugs: A retrospective study.
Capetti AF, Micale M, Carenzi L,  et al
 
Medicine (Baltimore)
. 2017 Feb;96(7):e5728.
Abstract

The choice between a ritonavir-boosted protease inhibitor- and a non-nucleoside reverse transcriptase inhibitor-based regimen for initiation of antiretroviral treatment - results from an observational study in Germany.
Mahlich J, Groß M, Kuhlmann A, Bogner J, et al
J Pharm Policy Pract. 2016 Dec 30;9:39.
Abstract

Human CaaX Protease ZMPSTE24 Expressed in Yeast: Structure and Inhibition by HIV Protease Inhibitors.
Clark KM, Jenkins JL, Fedoriw N, Dumont ME.

 
Protein Sci
. 2016 Oct 24. doi: 10.1002/pro.3074.
Paper

FULL-TEXT ARTICLE
HIV Protease Inhibitors Apoptotic Effect in SH-SY5Y Neuronal Cell Line.
Tricarico PM, de Oliveira Franca RF,  et al

Cell Physiol Biochem
. 2016;39(4):1463-70
Paper

Protease inhibitor monotherapy was non-inferior and cost-effective as maintenance therapy compared to triple therapy in viral load suppressed patients with HIV-1 infection.
Ripamonti D.

Evid Based Med
. 2016 Aug 26.
Abstract

FULL-TEXT ARTICLE
Long-term effectiveness of initiating non-nucleoside reverse transcriptase inhibitor- versus ritonavir-boosted protease inhibitor-based antiretroviral therapy: implications for first-line therapy choice in resource-limited settings.
Lima VD, Hull M, McVea D, et al
J Int AIDS Soc
. 2016 Aug 5;19(1):20978.
Paper

FULL-TEXT ARTICLE
Improved adipose tissue function with initiation of protease inhibitor-only ART.
Maughan RT, Feeney ER, Capel E, etr al
J Antimicrob Chemother. 2016 Aug 11
Paper

Impact of protease inhibitors on the evolution of urinary markers: Subanalyses from an observational cross-sectional study.
Bonjoch A, Puig J, Pérez-Alvarez N, et al

Medicine (
Baltimore)
. 2016 Aug;95(32):e4507
Abstract

Investigational protease inhibitors as antiretroviral therapies.
Midde NM, Patters BJ, Rao P,  et al

Expert Opin Investig Drugs
. 2016 Jul 14
Abstract

Sociodemographic and clinical factors associated with the preference between NNRTIs and PIs for the initial treatment of HIV infection: Perfil-es study.
Viciana P, Ocampo A, Hevia H, et al
AIDS Care
. 2016 May 3:1-6.
Abstract

FULL-TEXT LETTER
Protease inhibitors and azolic antifungals in HIV patients with histoplasmosis: a clinical pharmacokinetics perspective
Okumura IM
Braz Jl  Infec DApr 16, 2016
Commentary

A cross-sectional study to evaluate the association of hyperbilirubinaemia on markers of cardiovascular disease, neurocognitive function, bone mineral density and renal markers in HIV-1 infected subjects on protease inhibitors
Barber TJ, Moyle G, Hill A, et al

HIV Clin Trials. 2016 May;17(3):123-30.
Abstract

Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS.
Ghosh AK, Osswald HL, Prato G.

J Med Chem
. 2016 Jan 22.
Abstract

Late treatment failures in cerebrospinal fluid in patients on long-term maintenance ART with ritonavir-boosted protease PI monotherapy.
Kahlert C, Bregenzer A, Gutmann C, et al 
Infection
. 2015 Dec 11
Abstract

Differences in the Prediction of Area Under the Curve for a Protease Inhibitor Using Trough Versus Peak Concentration: Assessment Using Published Pharmacokinetic Data for Indinavir.
Srinivas NR.
Am J Ther. 2015 Aug 18.
Abstract

FULL-TEXT ARTICLE
Systemic inflammation and residual viraemia in HIV-positive adults on protease inhibitor monotherapy: a cross-sectional study.
Arenas-Pinto A, Milinkovic A,  Peppa D, et al
BMC Infect Dis. 2015 Mar 21;15(1):138.
Paper

Sildenafil and bosentan plasma concentrations in a human immunodeficiency virus- infected patient with pulmonary arterial hypertension treated with ritonavir-boosted protease inhibitor.
Chinello P, Cicalini S, Pichini S,  et al
Infect Dis Rep. 2015 Mar 16;7(1):5822.
Abstract

Low level HIV viremia is more frequent under protease-inhibitor containing firstline therapy than under NNRTI-regimens
Wiesmann F, Braun P, Knickmann M, Knechten H.
J Int AIDS Soc. 2014 Nov 2;17(4(Suppl 3)):19828.
Abstract

FULL-TEXT PDF ARTICLE
Inflammatory, procoagulant markers and HIV residual viremia in patients receiving protease inhibitor monotherapy or triple drug therapy: a cross-sectional study.
Estébanez M, Stella-Ascariz N, Mingorance J,
BMC Infect Dis
. 2014 Jul 10;14(1):379
Paper

Protease inhibitor monotherapy is not associated with increased viral replication in lymph nodes.
Vinuesa D, Parra-Ruiz J, Chueca N,  et al
 
AIDS
. 2014 May 16.
Abstract

Sequence-Specific Alterations of Epitope Production by HIV Protease Inhibitors.
Kourjian G, Xu Y, Mondesire-Crump I,  et al 

J Immunol
. 2014 Mar 10.
Abstract

Multi-Step Inhibition against HIV Lifecycle-Underlying the "Magic" of Protease Inhibitors.
Poveda E.

AIDS Rev
. 2014 Jan-Mar;16(1):52.
Abstract

Binary and ternary combinations of anti-HIV protease inhibitors: effect on gene expression and functional activity of CYP3A4 and efflux transporters.
Kwatra D, Vadlapudi AD, Vadlapatla RK,  et al

Drug Metabol Drug Interact
. 2014 Jan 8:1-1

Abstract

Lack of Effect of Doxycycline on Trough Concentrations of Protease Inhibitors or Non-Nucleoside Reverse Transcriptase Inhibitors in HIV-Infected Patients.
Abgrall S, Le Bel J, Lele N,  et al

HIV Clin Trials
. 2013 Nov-Dec;14(6):313-8
Abstract

Time to HIV-1 RNA Suppression Below 5 copies/ml During First-Line Protease Inhibitor-Based Antiretroviral Treatment - Any Impact of Residual Viremia on Treatment Success?
Ripamonti D, Hill A, Lauthouwers E, van Delft Y, Moecklinghoff C.
AIDS Rev. 2013 Oct-Dec;15(4):230-6.

Abstract

Contribution of Gag and protease to variation in susceptibility to protease inhibitors between different strains of subtype B HIV-1.
Sutherland KA, Mbisa JL, Cane PA,  et al
J Gen Virol. 2013 Oct 30.
Abstract

Solubility Profiling of HIV Protease Inhibitors in Human Intestinal Fluids.
Wuyts B, Brouwers J, Mols R, Tack J, et al

J Pharm Sci
. 2013 Aug 12.
Abstract

Nucleoside Reverse Transcriptase Inhibitors, Nonnucleoside Reverse Transcriptase Inhibitors, and Protease Inhibitors in the Treatment of HIV Infections (AIDS).
De Clercq E.
Adv Pharmacol. 2013;67:317-58.
Abstract

Higher vitamin D levels in HIV-infected out-patients on treatment with boosted protease inhibitor monotherapy.
Cervero M, Agud J, Torres R, et al
 
HIV Med
. 2013 Jun 5.
Abstract

Positioning of HIV-protease inhibitors in clinical practice.
Andreoni M, Perno CF.
Eur Rev Med Pharmacol Sci. 2012 Jan;16(1):10-8.
Abstract

Complex Drug Interactions of the HIV Protease Inhibitors 3: Effect of Simultaneous or Staggered Dosing of Digoxin and Ritonavir, Nelfinavir, Rifampin or Bupropion.
Kirby BJ, Collier AC, Kharasch ED,  et al
Drug Metab Dispos. 2011 Dec 21
.
Abstract

Influence of drug transport proteins on the pharmacokinetics and drug interactions of HIV protease inhibitors.
Griffin L, Annaert P, Brouwer KL.

J Pharm Sci
. 2011 Jun 22. .
Abstract

HIV Protease Inhibitors: Effect on the Opportunistic Protozoan Parasites.
Alfonso Y, Monzote L.

Open Med Chem J
. 2011;5:40-50
Abstract

Characterization of HIV-1 from patients with virological failure to a boosted protease inhibitor regimen.
Lillemark MR, Gerstoft J, Obel N,
et al
J Med Virol
. 2011 Mar;83(3):377-383

Abstract

Comparative Molecular Field Analysis of a Series of Inhibitors of HIV-1 Protease.
Ferreira LG, Leitão A, Montanari CA, Andricopulo AD.

Med Chem
. 2011 Jan 11.
Abstract

HIV protease inhibitors: garlic supplements and first-pass intestinal metabolism impact on the therapeutic efficacy.
Berginc K, Trdan T, Trontelj J, Kristl A.
Biopharm Drug Dispos. 2010 Oct 26.
Abstract

Boosted Protease Inhibitor Monotherapy. What Have We Learnt after Seven Years of Research?
Pulido F, Matarranz M, Rodríguez-Rivera V,  et al

AIDS Rev
. 2010 Jul-Sep;12(3):127-134
Abstract

Human immunodeficiency virus protease inhibitors reduce the growth of human tumors via a proteasome-independent block of angiogenesis and matrix metalloproteinases.
Toschi E, Sgadari C, Malavasi L, et al
I
nt
J Cancer
. 2010 Jul 8
Abstract

Gag Mutations Can Impact Virological Response to Dual Boosted Protease Inhibitor Combinations in Antiretroviral Naive HIV Infected Patients (2 IP - ANRS 127 trial).|
Larrouy L, Chazallon C, Landman R, et al

Antimicrob Agents Chemother
. 2010 May 3
Abstract

Protease inhibitor-based antiretroviral therapy in treatment-naive HIV-1-infected patients: the evidence behind the options.
Naggie S, Hicks C.

J Antimicrob Chemother
. 2010 Apr 23.
Abstract

HIV-protease inhibitors suppress skeletal muscle fatty acid oxidation by reducing CD36 and CPT-I fatty acid transporters.
Richmond SR, Carper MJ, Lei X, et al
 
Biochim Biophys Acta
. 2010 Jan 28.
Abstract

HIV protease inhibitors inhibit FACE1/ZMPSTE24: a mechanism for acquired lipodystrophy in patients on highly active antiretroviral therapy?|
Goulbourne CN, Vaux DJ.
 
J Biochem Soc Trans
. 2010 Feb;38(Pt 1):292-6.
Abstract

HIV-1 protease inhibitors. A review for clinicians.
Deeks SG, Smith M, Holodniy M, Kahn JO.
JAMA. 1997 Jan 8;277(2):145-53.
Abstract

HIV Protease Inhibitors Induce ER Stress and Disrupt Barrier Integrity in Intestinal Epithelial Cells.
Wu X, Sun L, Zha W, Studer E, et al

Gastroenterology
. 2009 Sep 1.
Abstract

HIV protease inhibitors: recent clinical trials and recommendations on use.
Fernández-Montero JV, Barreiro P, Soriano V.

Expert Opin Pharmacother
. 2009 Jul;10(10):1615-29.
Abstract

Regulatory issues in developing new HIV protease inhibitors: risks and benefits.
Struble KA, Chan-Tack KM, Soon GG.
Curr Opin HIV AIDS. 2008 Nov;3(6):676-80.
Abstract

Tolerability and Efficacy of PI Versus NNRTI-Based Regimens in Subjects Receiving HAART During Acute or Early HIV Infection.
Ernstrom KB, Little SJ, Routy JP, et al
J Acquir Immune Defic Syndr. 2009 Feb 3.
Abstract

Protease inhibitor therapy in resource-limited settings.
Elliott JH, Pujari S.
Curr Opin HIV AIDS. 2008 Nov;3(6):612-619
Abstract
 

HIV monotherapy with ritonavir-boosted protease inhibitors: a systematic review.
Bierman WF, van Agtmael MA, Nijhuis M, et al
AIDS. 2008 Dec 24.

Abstract
 

Boosted Protease Inhibitor-Based or Nonnucleoside Reverse Transcriptase-Based HAART:
Is There a Best Choice for Antiretroviral-Naive HIV-1 Infected Patients?
Cuzin L, Allavena C, Morlat P, Dellamonica P.
AIDS Rev. 2008 Oct-Dec;10(4):205-11.
Abstract
 
Nucleoside-Free Boosted Double PI Regimen: Significant CD4(+) T-Cell Recovery in Patients with Poor Immunologic Response Despite Virologic Suppression.
Lehmann C, Jung N, Hofmann A, et al
Curr HIV Re
s
. 2008 Nov;6(6):555-9
Abstract
 
Perceived stress and norepinephrine predict the effectiveness of response to protease inhibitors in HIV.
Ironson G, Balbin E, Stieren E, et al
Int J Behav Med. 2008;15(3):221-6.
Abstract
 
Second-line antiretroviral therapy in resource-limited settings: the experience of Médecins Sans Frontières.
Pujades-Rodríguez M, O'Brien D, 

AIDS
. 2008 Jul 11;22(11):1305-12.
Abstract
 
Design of HIV Protease Inhibitors Targeting Protein Backbone: An Effective Strategy for Combating Drug Resistance.
Ghosh AK, Chapsal BD, Weber IT, Mitsuya H.

Acc Chem Res
. 2007 Aug 28;
Abstract
 
Efficacy of boosted protease inhibitor monotherapy in patients with complex medical problems.
Garrett NJ, Matin N, Edwards SG, Miller RF.

AIDS.
2007 Aug 20;21(13):1821-3
Abstract
 
HIV Protease Inhibitors Enhance the Efficacy of Irradiation.
Cuneo KC, Tu T, Geng L, et al 
Cancer Res. 2007 May 15;67(10):4886-93.
Abstract
 
HIV-1 protease inhibitors do not interfere with provirus transcription and host cell apoptosis nduced by combined treatment TNF-alpha+TSA.
Vandergeeten C, Quivy V, Moutschen M, et al 
Biochem Pharmacol. 2007 Feb 24;
Abstract
 
Maintaining reduced viral fitness and CD4 response in HIV-infected patients with viremia receiving a
boosted protease inhibitor.
Grant P, Taylor J, Cain P, Short W, et al
Clin Infect Dis. 2009 Mar 1;48(5):680-2.
Abstract
 
Flying in the Face of Resistance: Antiviral-independent Benefit of HIV Protease Inhibitors on T-cell Survival.
Vlahakis SR, Bren GD, Algeciras-Schimnich A, et al 
Clin Pharmacol Ther. 2007 Mar 14;
Abstract
 
Variability in non-nucleoside reverse transcriptase and protease inhibitors concentrations among HIV-infected adults in routine clinical practice.
Molto J, Blanco A, Miranda C, Miranda J, et al

Br J Clin Pharmacol. 2007 Jan 12;
Abstract
 
Acid suppressive therapy and the effects on protease inhibitors.
Fulco PP, Vora UB, Bearman GM. 

Ann Pharmacother
. 2006 Nov;40(11):1974-83.
Abstract
 
Initial highly-active antiretroviral therapy with a protease inhibitor versus a non-nucleoside reverse transcriptase inhibitor: discrepancies between direct and indirect meta-analyses.
Chou R, Fu R, Huffman LH, Korthuis PT.
Lancet. 2006 Oct 28;368(9546):1503-15.
74 Abstract
 
Susceptibility to protease inhibitors in HIV-2 primary isolates from patients failing antiretroviral therapy.
Rodes B, Sheldon J, Toro C,  et al
J Antimicrob Chemother. 2006 Feb
Abstract
 
Postprandial response to a physiologic caloric load in HIV-positive patients receiving protease inhibitor-based or nonnucleoside reverse transcriptase inhibitor-based antiretroviral
therapy.
Thomas-Geevarghese A, Raghavan S, Minolfo R, et al 
 
Am J Clin Nutr.
2005 Jul;82(1):146-54.
Abstract
 
Prescribing of Contraindicated Protease Inhibitor and Statin Combinations Among HIV-Infected Persons.
Hulgan T, Sterling TR, Daugherty J, et al 
J Acquir Immune Defic Syndr. 2005 Mar 1;38(3):277-282.
Abstract
 
FULL-TEXT PDF ARTICLE
The two-year impact of first generation protease inhibitor based antiretroviral therapy (PI-ART) on health-related quality of life.
Eriksson LE, Bratt GA, Sandstrom E, Nordstrom G.
Health Qual Life Outcomes. 2005 May 4;3(1):32
Paper
 
The impact of HIV-protease inhibitors on opportunistic parasites.
Pozio E, Morales MA. et al  
 
Trends Parasitol.
2005 Feb;21(2):58-63.

Abstract

Tolerability and Safety of HIV Protease Inhibitors in Adults.
Sax PE, Kumar P.  

J Acquir Immune Defic Syndr.
2004 Sep 1;37(1):1111-1124
Abstract
 
Dynamics of HIV replication in lymphocytes and the efficacy of protease inhibitors.
Bermejo M, Sanchez-Palomino S, Usan L, Alcami J. 

J Med Virol.
2004 Aug;73(4):502-7.
Abstract
 
Protease inhibitor-sparing simplified maintenance therapy: a need for perspective.
Bucher HC, Young J, Battegay M.
  
J Antimicrob Chemother.
2004 Jul 21
Abstract
 
Transport of HIV Protease Inhibitors Through the Blood-Brain Barrier and Interactions With the Efflux Proteins, P-Glycoprotein and Multidrug Resistance Proteins.
Gimenez F, Fernandez C, Mabondzo A.
J Acquir Immune Defic Syndr. 2004 Jun 1;36(2):649-658
Abstract
 
Effectiveness of antiretroviral therapy after protease inhibitor failure: an analytic overview.
Losina E, Islam R, Pollock AC, et a
l
 
Clin Infect Dis. 2004 Jun 1;38(11):1613-22.
Abstract
 
Attitudes toward HIV protease inhibitors and medication adherence in an inner city HIV population.
Demmer C.
AIDS Patient Care STDS. 2003 Nov;17(11):575-80.
Abstract
 
FULL-TEXT PDF PUBLICATION
The HIV Protease Inhibitors

The Drug Advisor Volume 2. No 8 August 2003
Paper

Simplification of antiretroviral treatment--how to sustain success, reduce toxicity and ensure adherence avoiding PI use.
Barreiro P, Garcia-Benayas T, Soriano V, Gallant
J
.
AIDS Rev 2002 Oct-Dec;4(4):233-41
Abstract

Therapeutic drug monitoring of HIV-protease inhibitors to assess noncompliance.
Hugen PW, Burger DM, Aarnoutse RE,et al|
Ther Drug Monit 2002 Oct;24(5):579-87
Abstract

Factors associated with mortality in human immunodeficiency virus type  1-infected adults initiating protease inhibitor-containing therapy: role of education level and of early transaminase level elevation (APROCO-ANRS EP11 study).
The Antiproteases Cohorte Agence Nationale de Recherches sur
le SIDA EP 11 study.Lewden C, Raffi F, Cuzin L, et al

J Infect Dis 2002 Sep 1;186(5):710-4
Abstract
 
HIV-1 Protease Inhibitors- A Review for Clinicians.
Deeks, SG, Smith M, Holodniy M et al.
JAMA 1997; 277(2): 145-53.
Abstract
 

 
     Conference Reports, Abstracts, and Posters
 
 
Price-demand relationship in publicly financed ART market and its application to identify opportunities for cost reduction in WHO recommended protease inhibitors (PIs)
S. Juneja, S.S. Mishra, P. Prakash, A. Gupta
(XX International AIDS Conference)
Abstract

HIV-1 seminal shedding among patients undergoing protease inhibitor monotherapy vs. patients on triple therapy
A. Torres-Cornejo, M.Á. López-Ruz, O.J. Benmarzouk-Hidalgo, et al
(XX International AIDS Conference)
Abstract

 

Pharmacokinetics
 

     Journal Papers, Abstracts, and Commentaries

 
The Cellular Pharmacokinetics of HIV Protease Inhibitors: Current Knowledge and Future Perspectives.
Zha W, Zha BS, Zhou F,  et al

Curr Drug Metab
. 2012 Jun 29.
Abstract

HIV Protease Inhibitors Activate the Unfolded Protein Response and Disrupt Lipid Metabolism in Primary Hepatocytes.
Zhou H, Gurley EC, Jarujaron S ,et al

Am J Physiol Gastrointest Liver Physiol.
2006
Jul 20;
Abstract
 

The management of HIV-1 protease inhibitor pharmacokinetic interactions.
Winston A, Boffito M.

J Antimicrob Chemother. 2005 Jun 7;
Abstract
 
The pharmacokinetics of HIV protease inhibitor combinations.
Boffito M, Maitland D, Samarasinghe Y, Pozniak A. 

Curr Opin Infect Dis
. 2005 Feb;18(1):1-7.
Abstract

HIV protease inhibitors protect apolipoprotein B from degradation by the proteasome:A potential mechanism for protease inhibitor-induced hyperlipidemia.
Liang JS, Distler O, Cooper DA, et al.
Nat Med 2001 Dec;7(12):1327-31
Abstract

 

Drug/Drug Interactions Data
 

     Journal Papers, Abstracts, and Commentaries
 
 

 

Lack of effects of statins on high-density lipoprotein subfractions in HIV-1-infected patients receiving protease inhibitors.
Bittar R, Aslangul É, Giral P, Assoumou L, et al

C R Biol
. 2016 Dec 20.
Abstract  

Effect of protease inhibitors on steady state pharmacokinetics of oral norethindrone contraception in HIV infected women.
Atrio J, Stanczyk FZ, Neely M,  et al
J Acquir Immune Defic Syndr. 2013 Sep 13
Abstract  

Drug-Drug Interactions Between HMG-CoA Reductase Inhibitors (Statins) and Antiviral Protease Inhibitors.
Chauvin B, Drouot S, Barrail-Tran A, Taburet AM.

Clin Pharmacokinet
. 2013 May 24
Abstract  

Prediction of drug-drug Interactions Between Various Antidepressants and Efavirenz or Boosted Protease Inhibitors Using a Physiologically Based Pharmacokinetic Modelling Approach.
Siccardi M, Marzolini C, Seden K et al
Clin Pharmacokinet. 2013 Mar 12

Abstract
  

Predictors of Clinically Significant Drug-Drug Interactions Among Patients Treated with Nonnucleoside Reverse Transcriptase Inhibitor-, Protease Inhibitor-, and Raltegravir-Based Antiretroviral Regimens (March).
Patel N, Abdelsayed S, Veve M, Miller CD.
Ann Pharmacother. 2011 Mar 8.
Abstract  

Daily dosing of tacrolimus in patients treated with HIV-1 therapy containing a ritonavir-boosted protease inhibitor or raltegravir.
Bickel M, Anadol E, Vogel M, et al
 
J Antimicrob Chemother
. 2010 Mar
Abstract  

Interaction of HIV protease inhibitors with OATP1B1, 1B3, and 2B1.
Annaert P, Ye ZW, Stieger B, Augustijns P.
Xenobiotica
. 2010 Jan 27.
Abstract  

Pharmacokinetics and Pharmacodynamics of Sildenafil in a Patient Treated With Human Immunodeficiency Virus Protease Inhibitors.
Aschmann YZ, Kummer O, Linka A, et al
 
Ther Drug Monit.
2008 Feb;30(1):130-134.
Abstract  
 

Drug Interactions between HIV Protease Inhibitors and Acid-Reducing Agents.
Falcon RW, Kakuda TN.
Clin Pharmacokinet. 2008;47(2):75-89.
Abstract  
 
Quantitative Assessment of HIV-1 Protease Inhibitor Interactions with Drug Efflux Transporters in the Blood-Brain Barrier.
Bachmeier CJ, Spitzenberger TJ, Elmquist WF, Miller DW. 

Pharm Res.
2005 Aug;22(8):1259-68
Abstract  

Drug interactions between HIV protease inhibitors based on physiologically-based pharmacokinetic model.
Shibata N, Gao W, Okamoto H, et al.
J Pharm Sci 2002 Mar;91(3):680-9

Abstract  

 

Viral Dynamics
 

     Journal Papers, Abstracts, and Commentaries
 
  Review: Immunologic Response to Protease Inhibitor-Based Highly Active Antiretroviral Therapy: A Review.
Wainberg MA, Clotet B.
AIDS Patient Care STDS.
2007 Sep;21(9):609-620.
Abstract
 
  Virological and immunological outcomes at 3 years after starting antiretroviral therapy with regimens containing non-nucleoside reverse transcriptase inhibitor, protease inhibitor, or
both in NITIO: open-label randomised trial.INITIO Trial
International Co-ordinating Committee; Yeni P, Cooper DA, Aboulker JP, et al 
Lancet. 2006 Jul 22;368(9532):287-98
Abstract
 
  Mechanisms of early virologic failure in antiretroviral-naive patients starting protease inhibitor-containing regimens: the APROVIR Study
Masquelier B, Peytavin G, Leport C, et al
J Infect Dis 2002 Nov 15;186(10):1503-7
Abstract
 
  Predictors of virological rebound in HIV-1-infected patients initiating a protease inhibitor-containing regimen.
Le Moing V, Chene G, Carrieri MP , et al.
AIDS
2002 Jan 4;16(1):21-29
 
Abstract
   
  Impact of discontinuation of initial protease inhibitor therapy on further virological response in a cohort of human immunodeficiency virus-infected patients.
Le Moing V, Chene G, Leport C, et al.
Clin Infect Dis 2002 Jan 15;34(2):239-47

Abstract 

Adherence
 

     Journal Papers, Abstracts, and Commentaries

 
Variable adherence to prescribed dosing regimens for protease inhibitors: scope and outcomes.
Blaschke TF.
Curr Opin HIV AIDS. 2008 Nov;3(6):603-7
Abstract

Effect of Adherence to HAART on Virologic Outcome and on the Selection of Resistance-Conferring Mutations in NNRTI- or PI-Treated Patients.
Maggiolo F, Airoldi M, Kleinloog HD, et al
HIV Clin Trials. 2007 Sep-Oct;8(5):282-92
Abstract
 

Regimen-dependent variations in adherence to therapy and virological suppression in patients initiating protease inhibitor-based highly active antiretroviral therapy.
Moore DM, Hogg RS, Yip B, et al
HIV Med. 2006 Jul;7(5):311-6.
Abstract
 
The social realities of adherence to protease inhibitor regimens: substance use, health care and psychological States.
Halkitis PN, Kutnick AH, Slater S. et al
J Health Psychol. 2005 Jul;10(4):545-58.

Abstract  
 

     Conference Reports, Abstracts, and Posters

  Suboptimal self-reported antiretroviral therapy (ART) adherence associated with certain protease inhibitors and virologic rebound in the SMART study
S. Mannheimer, J.L. O'Connor, E.M. Gardner, et al.
(XIX International AIDS Conference)
Abstract

Treatment Strategies
 

     Journal Papers, Abstracts, and Commentaries

 
Factors associated with virological rebound in HIV-infected patients receiving protease inhibitor monotherapy.
Stöhr W, Dunn DT, Arenas-Pinto A, et al  

AIDS
. 2016 Nov 13;30(17):2617-2624.
bstract

FULL-TEXT ARTICLE
Switching to boosted protease inhibitor plus a second antiretroviral drug (dual therapy) for treatment simplification: a multicenter observational study.
Latini A, Fabbiani M, Borghi V, et al  

BMC Infect Dis
. 2016 Aug 11;16(1):401.
Paper

FULL-TEXT ARTICLE
Response to First-Line Ritonavir-Boosted Protease Inhibitors (PI/r)-Based Regimens in HIV Positive Patients Presenting to Care with Low CD4 Counts: Data from the Icona Foundation Cohort.
d'Arminio Monforte A, Cozzi-Lepri A, Maggiolo F,  et al
PLoS One. 2016 Jun 27;11(6):e0156360.
Paper

Estimated Glomerular Filtration Rate Trajectories in HIV-Infected Subjects Treated With Different Ritonavir-Boosted Protease Inhibitors and Tenofovir Disoproxil Fumarate or Abacavir.
Gianotti N, Galli L, Poli A, Salpietro S, et al
Medicine (Baltimore). 2016 May;95(22):e3780.
Abstract

FULL-TEXT ARTICLE
Effectiveness of Ritonavir-Boosted Protease Inhibitor Monotherapy in Clinical Practice Even with Previous Virological Failures to Protease Inhibitor-Based Regimens.
López-Cortés LF, Castaño MA, López-Ruz MA, et al
PLoS One. 2016 Feb 12;11(2):e0148924.
Paper

Efficacy of protease inhibitor monotherapy vs. triple therapy: meta-analysis of data from 2303 patients in 13 randomized trials.
Arribas JR, Girard PM, Paton N, et al

HIV Med
. 2015 Dec 28.

Abstract

Protease inhibitor monotherapy is effective in controlling HIV-1 shedding in the male genital tract.
Torres-Cornejo A, BenMarzouk-Hidalgo OJ, Viciana P,  et al
Clin Microbiol Infect. 2015 Oct 7.
Abstract

FULL-TEXT ARTICLE
HIV Protease Inhibitors Sensitize Human Head and Neck Squamous Carcinoma Cells to Radiation by Activating Endoplasmic Reticulum Stress.
Liu R, Zhang L, Yang J,  et al 

PLoS One
. 2015 May 1;10(5):e0125928
Paper

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 PI monotherapy versus triple therapy for 1964 patients in 10 randomised trials.
Arribas J, Girard PM, Paton N,  et al
J Int AIDS Soc. 2014 Nov 2;17(4(Suppl 3)):19788
Abstract

Antiretroviral Therapy and Efficacy after Virologic Failure on First-line Boosted Protease Inhibitor Regimens.
Zheng Y, Hughes MD, Lockman S, et al

Clin Infect Dis
. 2014 May 19. .
Abstract

Second-line protease inhibitor-based antiretroviral therapy after non-nucleoside reverse transcriptase inhibitor failure: the effect of a nucleoside backbone.
Waters L, Bansi L, Asboe D, Pozniak A,  et al

Antivir Ther
. 2013;18(2):213-.
Abstract

FULL-TEXT PDF ARTICLE
Boosted protease inhibitor monotherapy in HIV-infected adults: outputs from a pan-European expert panel meeting
Arribas JR, Doroana M, Turner D,
et al
AIDS Research and Therapy
2013, 10:3
Paper

Protease Inhibitor Monotherapy As Maintenance Regimen In Patients With HIV Infection.
Calza L, Manfredi R.
Curr HIV Res. 2012 Sep 26.
Abstract

Second line protease inhibitor (PI/r) based antiretroviral therapy (ART) after non-nucleoside reverse transcriptase inhibitor (NNRTI) failure: impact of nucleoside (NRTI) backbone.
Waters L, Bansi L, Asboe D, et al

Antivir Ther
. 2012 Aug 22. .
Abstract

Boosted protease inhibitor monotherapy as a maintenance strategy: an observational study in the FHDH-ANRS CO4 cohort.
Guiguet M, Ghosn J, Duvivier C, Meynard JL,  et al
AIDS. 2012 Jun 12.
Abstract

Protease inhibitor treatment effect on aortic stiffness in normotensive patients with human immunodeficiency virus infection.
Lopez-Sublet M, Honoré P, Bentata M, et al
J
 Mal Vasc
. 2012 Jun 12..
Abstract

Statin Therapy Decreases Serum Levels of High-Sensitivity C-Reactive Protein and Tumor Necrosis Factor-α in HIV-Infected Patients Treated With Ritonavir-Boosted Protease Inhibitors.
Calza L, Trapani F, Bartoletti M, et al

HIV Clin Trials
. 2012 May-Jun;13(3):153-61.|
Abstract

FULL-TEXT ARTICLE
Virologic Failures on Initial Boosted-PI Regimen Infrequently Possess Low-Level Variants with Major PI Resistance Mutations by Ultra-Deep Sequencing
Lataillade M, Chiarella J, Yang R, et al

PLoS One
. 2012;7(2):e30118I

Paper

Protease Inhibitors as Preferred Initial Regimen for Antiretroviral-Naive HIV Patients.
Tejerina F, López Bernaldo de Quirós JC.

AIDS R
ev
. 2011 Oct;13(4):227-33.
Abstract

FULL-TEXT ARTICLE

Effectiveness of Protease Inhibitor Monotherapy versus Combination Antiretroviral Maintenance Therapy:A Meta-Analysis
Mathis S, Khanlari B, Pulido F,  et al

PLoS ONE
6(7):
e22003
Paper

FULL-TEXT ARTICLE
Randomized Trial of Time-Limited Interruptions of Protease Inhibitor-Based Antiretroviral Therapy (ART) vs. Continuous Therapy for HIV-1 Infection
Firnhaber C, Azzoni L, Foulkes AS, et al  

PLoS One
.
2011;6(6):e21450.
Paper

Comparative effectiveness of continuing a virologically effective first-line boosted protease inhibitor combination or of switching to a three-drug regimen containing either efavirenz, nevirapine or abacavir.
Bommenel T, Launay O, Meynard JL, et al
J Antimicrob Chemother
. 2011 Jun 1
Abstract

Immunovirological Response to Triple Nucleotide Reverse-Transcriptase Inhibitors and Ritonavir-Boosted Protease Inhibitors in Treatment-Naive HIV-2-Infected Patients: The ACHIEV2E
Collaboration Study Group.
Benard A, van Sighem A, Taieb A,  et al
Clin Infect Dis
. 2011 May;52(10):1257-1266

Abstract

Protease inhibitor monotherapy.
Pérez-Valero I, Arribas JR.

Curr Opin Infect Dis
. 2010 Dec 9.
Abstract

How much ritonavir is needed to boost protease inhibitors? Systematic review of 17
dose-ranging pharmacokinetic trials.
Hill A, van der Lugt J, Sawyer W, Boffito M.
AIDS
. 2009 Oct 3.
Abstract

Clinical application of the inhibitory quotient: is there a role in HIV protease inhibitor therapy?
Winston A, Khoo S.
Curr Opin HIV AIDS. 2008 Nov;3(6):608-11.
Abstract

Double-boosted protease inhibitor antiretroviral regimens: what role?
Ribera E, Curran A.

Drugs
. 2008;68(16):2257-67.
Abstract
 

Second-line antiretroviral therapy in resource-limited settings: the experience of Médecins Sans Frontières.
Pujades-Rodríguez M, O'Brien D, Humblet P, Calmy A.
AIDS. 2008 Jul 11;22(11):1305-12.
Abstract
 
Ezetimibe Combined with Low-Dose Statin Effectively Lowers LDL in Protease Inhibitor Treated Patients.
Berg-Wolf MV, Klibanov OM, Gaughan JP, Tedaldi EM.

AIDS Patient Care STDS
. 2008 Ma
Abstract
 
Overview of boosted protease inhibitors in treatment-experienced HIV-infected patients.
Youle M. 
J Antimicrob Chemother. 2007 Sep 25;
Abstract
 
Superior virological response to boosted protease inhibitor-based highly active antiretroviral therapy in an observational treatment programme.
Wood E, Hogg R, Yip B, Moore D, et al

HIV Med. 2007 Mar;8(2):80-5.
Abstract
 
Three-year follow-up of protease inhibitor-based regimen simplification in HIV-infected patients.
Martinez E, Arnaiz JA, Podzamczer D, et al 

AIDS.
2007 Jan 30;21(3):367-369.
Abstract
 
A comparison of three highly active antiretroviral treatment strategies consisting of non-nucleoside reverse transcriptase inhibitors, protease inhibitors, or both in the presence of nucleoside reverse transcriptase inhibitors as initial therapy (CPCRA 058
FIRST Study): a long-term randomised trial.
MacArthur RD, Novak RM, Peng G, et al 
Lancet
. 2006 Dec 16;368(9553):2107-9.
Abstract
 
Effects of discontinuing Stavudine or protease inhibitor therapy on human immunodeficiency virus-related fat redistribution evaluated by dual-energy x-ray absorptiometry.
Tavassoli N, Bagheri H, Sommet A, et al

Pharmacotherapy.
2006 Feb;26(2):154-61
Abstract
 
Quadruple-2 protease inhibitors (PI)-therapy does not accelerate viral decay and suppression in PI-naive HIV-1 infected patients with severe immunosuppression and high viral load as
compared with standard triple therapy.
Portilla J, Boix V, Garcia-Henarejos JA, et al;
Int J STD AIDS. 2005 Dec;16(12):807-810.
Abstract
 
Superiority of protease inhibitors over nonnucleoside reverse-transcriptase inhibitors when highly active antiretroviral therapy is resumed after treatment interruption.
Barreiro P, de Mendoza C, Gonzalez-Lahoz J, Soriano V.
Clin Infect Dis. 2005 Sep 15;41(6):897-900.
Abstract
 
FULL-TEXT ARTICLE
Clinical efficacy of antiretroviral combination therapy based on protease inhibitors or non-nucleoside analogue reverse transcriptase inhibitors: indirect comparison of
controlled trials.
Yazdanpanah Y, Sissoko D, Egger M, et al
BMJ  2004;328:249 
Paper
 
Meta-analysis of randomized controlled trials of simplified versus continued protease inhibitor-based antiretroviral therapy in HIV-1-infected patients.
Bucher HC, Kofler A, Nuesch R,et al

AIDS.
2003 Nov 21;17(17):2451-9.
Abstract
 
Increased use of lipid-lowering therapy in patients receiving human immunodeficiency  virus protease inhibitors.
Stein JH, Wu Y, Kawabata H, Iloeje UH.

Am J Cardiol. 2003 Aug 1;92(3):270-4.
Abstract

Effect of simultaneous versus staggered dosing on pharmacokinetic interactions of protease inhibitors.
Washington CB, Flexner C, Sheiner  LB, et al.
Clin Pharmacol Ther
2003 May;73(5):406-16
Abstract
 

 
The role of pharmacological enhancement in protease inhibitor-based highly active antiretroviral therapy.
Becker SL
Expert Opin Investig Drugs 2003 Mar;12(3):401-12
Abstract
 
Dual vs single protease inhibitor therapy following antiretroviral treatment failure: a randomized trial.
Hammer SM, Vaida F, Bennett KK , et al.
JAMA 2002 Jul 10;288(2):169-80
Abstract
 

 

 

 


Diagnostics/Monitoring
 

     Journal Papers, Abstracts, and Commentaries
 
 
A cell-free enzymatic activity assay for the evaluation of HIV-1 drug resistance to protease inhibitors.
Matsunaga S, Masaoka T, Sawasaki T, et al 

Front Microbiol
. 2015 Oct 31;6:1220.
Abstract

Boosted protease inhibitors and the electrocardiographic measures of QT and PR durations.
Soliman EZ, Lundgren JD, Roediger MP,  et al

AIDS
. 2010 Dec 9
Abstract

Benefit of therapeutic drug monitoring of protease inhibitors in HIV-infected patients depends on PI used in HAART regimen--ANRS 111 trial.
Duval X, Mentré F, Rey E, et al
Fundam Clin Pharmacol. 2009 Aug;23(4):491-500
Abstract

A randomized trial of therapeutic drug monitoring of protease inhibitors in antiretroviral-experienced, HIV-1-infected patients.
Demeter LM, Jiang H, Mukherjee AL, et al

AIDS
. 2008 Dec 24
Abstract

An isocratic liquid chromatography method for determining HIV non-nucleoside reverse transcriptase
inhibitor and protease inhibitor concentrations in human plasma.
Weller DR, Brundage RC, Balfour HH Jr, Vezina HE. et al
J Chromatogr B Analyt Technol Biomed Life Sci.
2006 Oct 31;
Abstract


Non-HIV Indications
 

     Journal Papers, Abstracts, and Commentaries
 
 
Repositioning HIV protease inhibitors as cancer therapeutics.
Bernstein WB, Dennis PA.
Curr Opin HIV AIDS. 2008 Nov;3(6):666-75.
Abstract

Antileishmanial activity of HIV protease inhibitors.
Savoia D, Allice T, Tovo PA.
Int J Antimicrob Agents. 2005 Jun 12;
Abstract


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