Medical Advocates
Etravirine (Intelence/TMC125)
  Journal Papers, Abstracts, and
Commentaries

In Vitro Data
General Reports
Pharmacokinetics
Resistance
Drug/Drug Interactions
Efficacy
 		  
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Last Update:  September 06, 2008 
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In Vitro Data
 
  TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro
selection experiments.
Vingerhoets J, Azijn H, Fransen E, et al
J Virol. 2005 Oct;79(20):12773-82.
Abstract
General Reports
 
 
Etravirine for the treatment of HIV infection.
Seminari E, Castagna A, Lazzarin A.  Expert Rev Anti Infect Ther. 2008 Aug;6(4):427-33.

Is there a role for etravirine in patients with Nonnucleoside reverse transcriptase inhibitor
resistance?
Scott C, Grover D, Nelson M.  
AIDS. 2008 May 11;22(8):989-90.
 Abstract
 
Etravirine Has No Effect on QT and Corrected QT Interval in HIV-Negative Volunteers (June).
Peeters M, Janssen K, Kakuda TN, et al
Ann Pharmacother. 2008 Apr 29
Abstract
 
A WEEK IN REVIEW FEATURED REPORT
Etravirine.
Knoll BM, Vento S, Temesgen Z. 
Drugs Today (Barc). 2008 Jan;44(1):23-33
 Abstract

FULL-TEXT ARTICLE
TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against
nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1.
Andries K, Azijn H, Thielemans T, et al
 Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6.
 Paper

Roles of conformational and positional adaptability in structure-based design of TMC125-R165335
(etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and
effective against wild-type and drug-resistant HIV-1 variants.
Das K, Clark AD Jr, Lewi PJ, et al
J Med Chem. 2004 May 6;47(10):2550-60.
Abstract
Pharmacokinetics
 
 
Single- and multiple-dose pharmacokinetics of etravirine administered as two different formulations in HIV-1-infected
patients.
Kakuda TN, Schöller-Gyüre M,  
Antivir Ther. 2008;13(5):655-61.
 Abstract

A pharmacokinetic study of etravirine (TMC125) co-administered with ranitidine and omeprazole in
HIV-volunteers.
Schöller-Gyüre M, Kakuda TN, De Smedt G, et al
Br J Clin Pharmacol. 2008 May 19
 Abstract

Pharmacokinetic and Pharmacodynamic Study of the Concomitant Administration of
Methadone and TMC125 in HIV-Negative Volunteers.
 Schöller-Gyüre M, van den Brink W, et al
J Clin Pharmacol. 2008 Jan 14
Abstract
Resistance
 
 
Prevalence and risk factors for etravirine resistance among patients failing on non-nucleoside reverse transcriptase
inhibitors.
Lapadula G, Calabresi A, Castelnuovo F, et al  
Antivir Ther. 2008;13(4):601-5.
 Abstract

Prevalence of etravirine-associated mutations in clinical samples with resistance to nevirapine and efavirenz.
Llibre JM, Santos JR, Puig T, et al
J Antimicrob Chemother. 2008 Jul 23.
Abstract
Drug/Drug Interactions
 
 
A pharmacokinetic study of etravirine (TMC125) co-administered with ranitidine and omeprazole in
HIV-volunteers.
Schöller-Gyüre M, Kakuda TN, De Smedt G, et al
Br J Clin Pharmacol. 2008 May 19
 Abstract

Pharmacokinetic and Pharmacodynamic Study of the Concomitant Administration of
Methadone and TMC125 in HIV-Negative Volunteers.
Schöller-Gyüre M, van den Brink W, et al
J Clin Pharmacol. 2008 Jan 14
Abstract
Efficacy
 
 
Safety, Tolerability, and Preliminary Efficacy of 48 Weeks of Etravirine Therapy in a Phase IIb
Dose-Ranging Study Involving Treatment-Experienced Patients with HIV-1 Infection.
Montaner J, Yeni P, Clumeck NN, et al
Clin Infect Dis. 2008 Sep 2.
Abstract
 
Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in
DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial.
Lazzarin A, Campbell T, Clotet B, et al 
Lancet. 2007 Jul 7;370(9581):39-48.
 Abstract
 
Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in
DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial.
Madruga JV, Cahn P, Grinsztejn B, et al
Lancet. 2007 Jul 7;370(9581):29-38.
 Abstract

Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1: primary
24-week analysis.
The TMC125-C223 Writing Group.
 AIDS. 2007 Mar 30;21(6):F1-F10.
 Abstract

TMC125 exerts similar initial antiviral potency as a five-drug, triple class antiretroviral regimen.
Sankatsing SU, Weverling GJ, Peeters M, et al
AIDS. 2003 Dec 5;17(18):2623-7
Abstract

A randomized, double-blind, placebo-controlled trial of TMC125 as 7-day monotherapy in
antiretroviral naive, HIV-1 infected subjects.
Gruzdev B, Rakhmanova A, Doubovskaya E, et al
AIDS. 2003 Nov 21;17(17):2487-94.
 Abstract

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