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Rilpivirine(TMC278)
 
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Last Update:  April 18, 2012
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New and Noteworthy
 
April 2012
 
Journal Abstracts, Papers, and Commentaries
 
 
Where rilpivirine meets with tenofovir, the start of a new anti-HIV drug combination era.
 De Clercq E.
Biochem Pharmacol. 2012 Apr 5.
 Abstract

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

A WEEK-IN-REVIEW FEATURED REPORT
Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naïve, 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

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

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

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

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

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

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

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

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

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) f
or 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
Conference Reports, Abstracts, and Posters
 
19 CROI
 
  Relationship between Combination of Baseline Viral Load and CD4 Cell Count, and Week 48 or 96 Responses to Rilpivirine or Efavirenz in Treatment-naïve HIV-1+ Adults: Pooled Analysis from the Phase 3 ECHO and THRIVE Trials
 C Cohen , J-M Molina, D Jayaweera,  et al
 Abstract
 
Week-96 Resistance Analysis of the Rilpivirine Phase 3 Trials in Treatment-naïve HIV+ Adults
 L Rimsky, V Van Eygen, J Vingerhoets, et al
 Abstract
 
Resistance-associated Mutations to Efaviranez, Etravirine, Nevirapine, and Rilpivirine among ARV-naïve HIV-1+ Patients: Thailand
 S Sungkanuparph, S Kiertiburanakul, E Pasomsub, W Chantratita
 Abstract
 
Rilpivirine Resistance Mutations in HIV-1+ Patients Failing NNRTI Therapy: Drug-resistance Database, the Spanish AIDS Research Network
 L Anta, J Llibre, E Poveda, et al
 Abstract
 
The Interactions of Rilpivirine with Drug Transporters in vitro
 D Moss, M Siccardi, S Khoo,  et al
 Abstract
 
Mutation Y188L of HIV-1 Reverse Transcriptase Is Strongly Associated with Reduced Susceptibility to Rilpivirine
 M Haddad, L Napolitano, A Paquet,  et al
 Abstract
 
Absence of Pharmacokinetic Interaction between the NNRTI Rilpivirine (TMC278) and the Integrase Inhibitor Raltegravir
 H Crauwels, M Steven, Guy De La Rosa, K Boven
 Abstract

6th IAS Conference
 
  Pooled week 96 efficacy, resistance and safety results from the double-blind, randomised, phase III trials comparing rilpivirine (RPV) versus efavirenz (EFV) in treatment-naïve, HIV-1-infected adults
 C. Cohen, J.-M. Molina, I. Cassetti, et al
Abstract

Ninth International Congress on Drug Therapy in HIV Infection
 

  POSTER
 Efficacy and safety of TMC278 in treatment-naïve, HIV-infected patients: Week 96 data from
TMC278-C204
 J-M Molina, C Cordes, P Ive, et al
 PDF Poster
 
  POSTER
 Efficacy and safety of TMC278 in treatment-naïve, HIV-infected patients: Week 96 data from
TMC278-C204
 J-M Molina, C Cordes, P Ive, et al 
PDF Poster
 
XVII International AIDS Conference
 
  A WEEK IN REVIEW FEATURED REPORT
 POWERPOINT PRESENTATION
 TMC278 (rilpivirine), an investigational next-generation NNRTI, demonstrates long-term efficacy
and tolerability in ARV-naïve patients: 96-week results of study C204
M Santoscoy, P Cahn,C Gonsalez, et al
Presentation
 
  POSTER
TMC278 long acting – a parenteral nanosuspension formulation that provides sustained clinically
relevant plasma concentrations in HIV-negative volunteers
 R Verloes, G van‘t Klooster, L Baert, et al
PDF Poster
 
POSTER
The pharmacokinetic interaction between rifabutin and TMC278, an investigational NNRTI
 HM Crauwels, RPG van Heeswijk, D Kestens,  et al 
PDF Poster

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