Medical Advocates

Rilpivirine (Edurant)
 
Journal Abstracts, Papers, and Commentaries

General Reports
Pharmacokinetics

Diagnostics/Monitoring
Viral Dynamics
Resistance
Efficacy

Adverse Events
Drug/Drug Interactions
Therapeutic Strategies

 


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Last Update:  April 16, 2014
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General Reports
 

 
Rilpivirine: drug profile of a second-generation non-nucleoside reverse transcriptase HIV-inhibitor.
Ripamonti D, Bombana E, Rizzi M.
 
Expert Rev Anti Infect Ther. 2013 Nov 28
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Effect of food on rilpivirine/emtricitabine/tenofovir disoproxil fumarate, an antiretroviral single-tablet regimen for the treatment of HIV infection.
Custodio JM, Yin X, Hepner M,  et al
J Clin Pharmacol
. 2013 Oct 19

Abstract

A WEEK-IN-REVIEW FEATURED REPORT
An update on clinical utility of rilpivirine in the management of HIV infection in treatment-naďve patients.
Putcharoen O, Kerr SJ, Ruxrungtham K.
HIV AIDS
(Auckl)
. 2013 Sep 16;5:231-241.
Abstract

Rilpivirine inhibits drug transporters ABCB1, SLC22A1 and SLC22A2 in vitro.
Moss DM, Liptrott NJ, Curley P, et al 
Antimicrob Agents Chemother
. 2013 Sep 3

Abstract

Safety profile of rilpivirine: general and neuropsychiatric tolerability, safety in patients with hepatitis B or C viruses, and lipid profile.
López Cortés LF, Martínez E, von Wichmann MA.
Enferm Infecc Microbiol Clin
. 2013 Jun;31S2:6-11
Abstract

Rilpivirine - a novel HIV-1 non-nucleoside reverse transcriptase inhibitor
Snopková S, Havlíčková K, Polák P, Slesinger P, Husa P.
Klin Mikrobiol Infekc Lek. 2013 Mar;19(1):19-22.
Abstract

The Role of Rilpivirine in Clinical Practice: Strengths and Weaknesses of the New Nonnucleoside Reverse Transcriptase Inhibitor for HIV Therapy.
Imaz A, Podzamczer D.
AIDS Rev. 2012 Oct;14(4):268-78.
Abstract

Absence of a pharmacokinetic interaction of rilpivirine with the P-glycoprotein substrate digoxin in healthy volunteers.
Crauwels H, Deckx H, Enweonye I,  et al
J Int AIDS Soc
. 2012 Nov 11;15(6):18337.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT 
Update on rilpivirine: A new potent non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV replication.
Zaharatos GJ, Wainberg MA.
Ann Med
. 2012 Nov 17.
Abstract

Rilpivirine. First-line treatment of HIV infection: efavirenz is better documented.

[No authors listed]
Prescrire Int. 2012 Nov;21(132):262-5

Abstract

A WEEK-IN-REVIEW FEATURED REPORT 
Rilpivirine: a new non-nucleoside reverse transcriptase inhibitor.
Sharma M, Saravolatz LD.
J Antimicrob Chemother
. 2012 Oct 25
Abstract

Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection: a systematic review.
Schafer JJ, Short WR.
Antivir Ther. 2012 Jul 25.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
FULL-TEXT ARTICLE

Rilpivirine: A second-generation nonnucleoside reverse transcriptase inhibitor.
James C, Preininger L, Sweet M.
Am J Health Syst Pharm. 2012 May 15;69(10):857-61.
Paper

Rilpivirine and complera: new first-line treatment options.
O'Neal R.
BETA
. 2011 Fall-Winter;23(4):14-8.
Abstract

Rilpivirine: A second-generation nonnucleoside reverse transcriptase inhibitor.
James C, Preininger L, Sweet M.
Am J Health Syst Pharm
. 2012 May 15;69(10):857-61.
Abstract

Rilpivirine : a next-generation non-nucleoside analogue for the treatment of HIV infection.
Fernández-Montero JV, Vispo E,  et al
Expert Opin Pharmacother. 2012 May;13(7):1007-14
Abstract

Rilpivirine.
Sanford M.
Drugs
. 2012 Mar 5;72(4):525-41
Abstract

Rilpivirine: a new addition to the anti-HIV-1 armamentarium.
Miller CD, Crain J, Tran B, Patel N.
Drugs Today (Barc). 2011 Jan;47(1):5-15
Abstract

Crystal Structures of HIV-1 Reverse Transcriptase with Etravirine (TMC125) and Rilpivirine (TMC278): Implications for Drug Design.
Lansdon EB, Brendza KM, Hung M, et al  
J Med Chem
. 2010 May 3
Abstract

Short-term randomized proof-of-principle trial of TMC278 in patients with HIV type-1 who have previously failed antiretroviral therapy.
Arastéh K, Rieger A, Yeni P, et al 
Antivir Ther
. 2009;14(5):713-22
Abstract

Rilpivirine: a novel non-nucleoside reverse transcriptase inhibitor.
Garvey L, Winston A.
Expert Opin Investig Drugs. 2009 Jul;18(7):1035-4
Abstract
 
Development of a long-acting injectable formulation with nanoparticles of rilpivirine (TMC278) for HIV treatment.
Baert L, van 't Klooster G, Dries W, et al
Eur J Pharm Biopharm
. 2009 Mar 27
Abstract

Etravirine and rilpivirine: nonnucleoside reverse transcriptase inhibitors with activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agents.
Fulco PP, McNicholl IR.
Pharmacotherapy
2009 Mar;29(3):281-94
Abstract


Rilpivirine, a non-nucleoside reverse transcriptase inhibitor for the treatment of HIV infection.
Ripamonti D, Maggiolo F.
Curr Opin Investig Drugs. 2008 Aug;9(8):899-912.
Abstract
 
Powder for reconstitution of the anti-HIV-1 drug TMC278 - Formulation development, stability and animal studies.
Van Gyseghem E, Pendela M, Baert L, et al
Eur J Pharm Biopharm. 2008 Jul 9.
Abstract
 
High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations.
Das K, Bauman JD, Clark AD Jr,
Proc Natl Acad Sci U S A. 2008 Feb 5;105(5):1466-71.
Paper
 
FULL-TEXT PDF ARTICLE
Two-dimensional infrared spectra reveal relaxation of the nonnucleoside inhibitor TMC278 complexed with HIV-1 reverse transcriptase.
Fang C, Bauman JD, Das K, et al
Proc Natl Acad Sci U S A. 2008 Feb 5;105(5):1472-7.
Paper
 
Short-term antiviral activity of TMC278--a novel NNRTI--in treatment-naive HIV-1-infected subjects.
Goebel F, Yakovlev A, Pozniak AL, et al
AIDS. 2006 Aug 22;20(13):1721-6.
Abstract

 
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile  (R278474, rilpivirine).
Janssen PA, Lewi PJ, Arnold E, et al
J Med Chem. 2005 Mar 24;48(6):1901-9.
Abstract


Pharmacokinetics
 

  Mechanism of action and pharmacokinetics of rilpivirine.
Portilla J, Estrada V.
Enferm Infecc Microbiol Clin. 2013 Jun;31S2:2-5.
Abstract

Effect of food on the pharmacokinetics of emtricitabine/rilpivirine/tenofovir disoproxil fumarate single-tablet regimen.
Ramanathan S, Custodio J, Yin X, Hepner M,  et al  
J Int AIDS Soc
. 2012 Nov 11;15(6):18333.
Abstract

FULL-TEXT ARTICLE
Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
van 't Klooster G, Hoeben E, Borghys H,
Antimicrob Agents Chemother
. 2010 May;54(5):2042-50.
Paper


Diagnostics/Monitoring
 

 
A validated assay by liquid chromatography-tandem mass spectrometry for the simultaneous quantification of elvitegravir and rilpivirine in HIV positive patients.
Aouri M, Calmy A, Hirschel B,  et al 
J Mass Spectrom
. 2013 May;48(5):616-625.
Abstract

A validated assay by liquid chromatography-tandem mass spectrometry for the simultaneous quantification of elvitegravir and rilpivirine in HIV positive patients.
Aouri M, Calmy A, Hirschel B,  et al 
J Mass Spectrom. 2013 May;48(5):616-625.

Abstract

Determination of rilpivirine (TMC-278) plasma concentrations by the conventional LC-MS method.
Shibata M, Takahashi M, Kuwahara T, et al
J Int AIDS Soc
. 2012 Nov 11;15(6):18361
Abstract

Liquid chromatography-tandem mass spectrometric assay for the non-nucleoside reverse transcriptase inhibitor rilpivirine in human plasma.
Burugula L, Pilli NR, Makula A,  et al
Biomed Chromatogr
. 2012 Jun 22.
.
Abstract


Viral Dynamics
 

  Genotypic and phenotypic characterization of HIV-1 isolates obtained from patients on rilpivirine therapy experiencing virologic failure in the phase 3 ECHO and THRIVE studies: 48-week analysis.
Rimsky L, Vingerhoets J, Van Eygen V, et al
J Acquir Immune Defic Syndr
. 2011 Nov 7.
Abstract

Resistance
 

 

Prevalence in the USA of rilpivirine resistance-associated mutations in clinical samples and effects on phenotypic susceptibility to rilpivirine and etravirine.
Picchio GR, Rimsky LT, Van Eygen V,
Antivir Ther. 2014 Apr 4
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Rilpivirine, emtricitabine and tenofovir resistance in HIV-1-infected rilpivirine-naive patients failing antiretroviral therapy.
Lambert-Niclot S, Charpentier C, Storto A, et al
J Antimicrob Chemother
. 2013 Dec 2
Abstract

The Connection Domain Mutation N348I in HIV-1 Reverse Transcriptase Enhances Resistance to Etravirine and Rilpivirine but Restricts the Emergence of the E138K Resistance Mutation by Diminishing Viral Replication Capacity.
Xu HT, Colby-Germinario SP, Oliveira M,  et al
J Virol
. 2013 Nov 13.
Abstract

Genetic barrier to the development of resistance to rilpivirine and etravirine between HIV-1 subtypes CRF02_AG and B.
Fofana DB, Soulie C, Maiga AI, et al
J Antimicrob Chemother. 2013 Jul 5.
Abstract

Resistance profile of rilpivirine.
Imaz A, García F, di Yacovo S, Llibre JM.
Enferm Infecc Microbiol Clin. 2013 Jun;31S2:36-43
Abstract

The Effect of Mutations at Position E138 in HIV-1 Reverse Transcriptase and their Interactions with the M184I Mutation in Defining Patterns of Resistance to the Non-Nucleoside Reverse Transcriptase Inhibitors Rilpivirine and Etravirine.
Xu HT, Colby-Germinario SP, Asahchop EL, et al 
Antimicrob Agents Chemother
. 2013 Apr 22.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Prevalence of pre-existing resistance-associated mutations to rilpivirine, emtricitabine and tenofovir in antiretroviral-naive patients infected with B and non-B subtype HIV-1 viruses.
Lambert-Niclot S, Charpentier C, Storto A,  et al
J Antimicrob Chemother
. 2013 Jan 29.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Distinct resistance patterns to etravirine and rilpivirine in viruses containing nnrti mutations at baseline.
Asahchop EL, Wainberg MA, Oliveira M, et al
AIDS. 2012 Dec 19.
Abstract

A WEEK-IN-REVIEW FEATURED ARTICLE

Preexisting mutations in the rilpivirine Phase III trials ECHO and THRIVE: prevalence and impact on virologic response.
Vingerhoets J, Rimsky L, Van Eygen V,  et al
Antivir Ther
. 2012 Sep 6.
Abstract

FULL-TEXT PDF ARTICLE
Biochemical Mechanism of HIV-1 Resistance to Rilpivirine.
Singh K, Marchand B, Rai DK,  et al
J Biol Chem. 2012 Sep 6
Paper

Rilpivirine Resistance Mutations in HIV Patients Failing Non-Nucleoside Reverse Transcriptase Inhibitor-Based Therapies.
Anta L, Llibre JM, Poveda E,  et al
AIDS
. 2012 Aug 7.
Abstract

FULL-TEXT ARTICLE
Panel of prototypical recombinant infectious molecular clones resistant to nevirapine, efavirenz, etravirine, and rilpivirine.
Balamane M, Varghese V, Melikian GL, et al
Antimicrob Agents Chemother. 2012 Aug;56(8):4522-4
Paper
 

Minority variants associated with resistance to HIV-1 nonnucleoside reverse transcriptase inhibitors during primary infection.
Nicot F, Saliou A, Raymond S, et al  J
Clin Virol
. 2012 Jul 19.
Abstract

E138K and M184I mutations in HIV-1 reverse transcriptase co-emerge as a result of APOBEC3 editing in the absence of drug exposure.
Fourati S, Malet I, Lambert S,  et al
AIDS. 2012 Jun 12
Abstract

A WEEK-IN REVIEW FEATURED REPORT
Panel of Prototypical Recombinant Infectious Molecular Clones Resistant to Nevirapine, Efavirenz, Etravirine, and Rilpivirine.
Balamane M, Varghese V, Melikian GL,  et al
Antimicrob Agents Chemother
. 2012 Jun 4.
Abstract

A WEEK-IN REVIEW FEATURED REPORT
Prevalence of TMC278 (rilpivirine) associated mutations in the Frankfurt Resistance Database.
Reinheimer C, Doerr HW, Stürmer M. et al
J Clin Virol
. 2011 Dec 30.
Abstract

   
  Etravirine and rilpivirine resistance in HIV-1 subtype CRF01_AE-infected adults failing non-nucleoside reverse transcriptase inhibitor-based regimens.
Bunupuradah T, Ananworanich J, Chetchotisakd P,  et al
Antivir Ther. 2011;16(7):1113-21
Abstract

Efficacy
 

 
Rilpivirine Versus Efavirenz with Emtricitabine/Tenofovir Disoproxil Fumarate in Treatment-Naďve HIV-1-Infected Patients with HIV-1 RNA ≤100,000 Copies/mL: Week 96 Pooled ECHO/THRIVE Subanalysis.
Behrens G, Rijnders B, Nelson M,  et al  
AIDS Patient Care STDS
. 2014 Mar 24.
Abstract

Outcomes In Older Versus Younger Patients Over 96 Weeks In Hiv-1-Infected Patients Treated With Rilpivirine Or Efavirenz In Echo And Thrive
Ryan R, Dayaram YK, Schaible D,  et al
Curr HIV Res
. 2014 Jan 28
Abstract

Data on rilpivirine in treatment-naďve patients. Lessons from ECHO, THRIVE and STaR.
Domingo P, Ribera E.
Enferm Infecc Microbiol Clin. 2013 Jun;31S2:20-29.
Abstract

Rilpivirine Versus Efavirenz in HIV-1-Infected Subjects Receiving Emtricitabine/Tenofovir DF: Pooled 96-Week Data from ECHO and THRIVE Studies.
Nelson MR, Elion RA, Cohen CJm et al
HIV Clin Trials. 2013 May-Jun;14(3):81-91.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
96-week resistance analyses of rilpivirine in treatment-naive, HIV-1-infected adults from the ECHO and THRIVE Phase III trials.
Rimsky L, Van Eygen V, Hoogstoel A,  et al
Antivir Ther. 2013 May 28
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Rilpivirine : a next-generation non-nucleoside analogue for the treatment of HIV infection.
Fernández-Montero JV, Vispo E,  et al
Expert Opin Pharmacother
. 2012 May;13(7):1007-14
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Combination therapies, effectiveness, and adherence in patients with HIV infection: clinical utility of a single tablet of emtricitabine, rilpivirine, and tenofovir.
Wainberg MA.HIV AIDS (Auckl). 2013;5:41-9.
Abstract

Rilpivirine versus efavirenz in HIV-1 patients with baseline viral load ≤100 000 copies/ml: week 48 Phase III analysis.
Molina JM, Clumeck N, Redant K,  et al
AIDS
. 2012 Dec 31.
Abstract

A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants.
Johnson BC, Pauly GT, Rai G, et al
Retrovirology
. 2012 Dec 5;9(1):99.
Abstract

Week 96 efficacy and safety of rilpivirine in treatment-naďve, HIV-1 patients in two Phase III randomised trials.
Cohen CJ, Molina JM, Cassetti I, et al
AIDS
. 2012 Dec 3.
Abstract

Rilpivirine. First-line treatment of HIV infection: efavirenz is better documented.
[No authors listed]
Prescrire Int. 2012 Nov;21(132):262-5
Abstract

A WEEK-IN-REVIEW FEATURED ARTICLE
Where rilpivirine meets with tenofovir, the start of a new anti-HIV drug combination era.
De Clercq E.
Biochem Pharmacol
. 2012 Apr 5.
Abstract

Efficacy and safety of rilpivirine in treatment-naive, HIV-1-infected patients with hepatitis B virus/hepatitis C virus coinfection enrolled in the Phase III randomized, double-blind ECHO and THRIVE trials.
Nelson M, Amaya G, Clumeck N, et al
J Antimicrob Chemother
. 2012 Apr 24.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naďve, HIV-1-infected patients: Pooled results from the phase 3 double-blind, randomized ECHO and THRIVE trials.
Cohen C, Molina J, Cahn P, et al
J Acquir Immune Defic Syndr
. 2012 Feb 16
Abstract

   
  Rilpivirine versus efavirenz with tenofovir and emtricitabine in treatment-naive adults infected with HIV-1 (ECHO): a phase 3 randomised double-blind active-controlled trial.
Molina JM, Cahn P, Grinsztejn B. et al
Lancet. 2011 Jul 16;378(9787):238-46.
Abstract
   
  Rilpivirine versus efavirenz with two background nucleoside or nucleotide reverse transcriptase inhibitors in treatment-naive adults infected with HIV-1 (THRIVE): a phase 3, randomised, non-inferiority trial.
Cohen CJ, Andrade-Villanueva J, Clotet B, et al 
Lancet
. 2011 Jul 16;378(9787):229-37.
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

Adverse Events
 

  Analysis of Lipid Levels and Changes in Body Fat Distribution in Treatment-Naive, HIV-1-Infected Adults Treated with Rilpivirine or Efavirenz Over 96 Weeks in the ECHO and THRIVE Trials.
Tebas P, Sension M, Arribas J,  et al
Clin Infect Dis
. 2014 Apr 11.
Abstract

Change in vitamin D levels and risk of severe vitamin D deficiency over 48 weeks among HIV-1-infected, treatment-naive adults receiving rilpivirine or efavirenz in a Phase III trial (ECHO).
Wohl DA, Orkin C, Doroana M,  et al
Antivir Ther. 2014 Jan 16.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Liver Toxicity in HIV-Infected Patients Receiving Novel Second-Generation Nonnucleoside Reverse Transcriptase Inhibitors Etravirine and Rilpivirine.
Casado JL. 
AIDS Rev. 2013 Jul-Sep;15(3):139-45.
Abstract


Drug/Drug Interactions
 

  The effect of rilpivirine on the pharmacokinetics of methadone in HIV-negative volunteers.
Crauwels HM, van Heeswijk RP, Vandevoorde A,  
J Clin Pharmaco
l
. 2013 Nov 6.
Abstract

Lack of an effect of rilpivirine on the pharmacokinetics of ethinylestradiol and norethindrone in healthy volunteers.
Crauwels HM, van Heeswijk RP, Buelens A,  et al
Int J Clin Pharmacol Ther
. 2013 Oct 28.
Abstract

Lack of Pharmacokinetic Interaction Between Rilpivirine and Integrase Inhibitors Dolutegravir and GSK1265744.
Ford SL, Gould E, Chen S, et al 
Antimicrob Agents Chemother
. 2013 Aug 26.

Abstract

Pharmacokinetic interactions
Arazo Garcés P, Los Santos Gil ID.
Enferm Infecc Microbiol Clin. 2013 Jun;31S2:12-19
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Clinical Perspective on Drug‑Drug Interactions with the Non-nucleoside Reverse Transcriptase Inhibitor Rilpivirine.
Crauwels H, van Heeswijk RP, Stevens M,  et al 
AIDS Rev
. 2013 May 17;15(2):87-101.

Abstract


Therapeutic Strategies
 

  Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens.
Mills AM, Cohen C, Dejesus E ,et al
HIV Clin Trials. 2013 Sep-Oct;14(5):216-33.
Abstract

Potential role of rilpivirine in simplification regimens.
Casado JL, Moreno S.
Enferm Infecc Microbiol Clin. 2013 Jun;31S2:30-35.
Abstract

 


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