Medical Advocates
Aplaviroc(GSK 873140)
  Journal Papers, Abstracts and Commentaries

 General Reports
 Safety
 Pharmacokinetics
Drug/Drug Interactions
 Efficacy
 Adverse Events



 		  
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Last Update:  December 08, 2014 
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General Reports
     
  FULL-TEXT ARTICLE
 Identification and Characterization of INCB9471, an Allosteric Non-Competitive Small Molecule Antagonist of
CCR5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection.
Shin N, Solomon K, Zhou N, Wang KH,  et al
J Pharmacol Exp Ther. 2011 Apr 1
 Paper

The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor.
Watson C, Jenkinson S, Kazmierski W, Kenakin T.
 Mol Pharmacol. 2005 Apr;67(4):1268-82
Abstract
Safety
     
  Antiviral activity and safety of aplaviroc with lamivudine/zidovudine in HIV-infected, therapy-naive patients:
the ASCENT (CCR102881) study.
Currier J, Lazzarin A, Sloan L,  et al  
Antivir Ther. 2008;13(2):297-306
Abstract
 
Antiviral activity and safety of 873140, a novel CCR5 antagonist, during short-term monotherapy in
HIV-infected adults.
Lalezari J, Thompson M, Kumar P,  et al
 AIDS. 2005 Sep 23;19(14):1443-8.
 Abstract
Pharmacokinetics
     
 

FULL-TEXT ARTICLE
 Pharmacokinetics and short-term safety of 873140, a novel CCR5 antagonist, in healthy adult subjects.
Adkison KK, Shachoy-Clark A, Fang L,
Antimicrob Agents Chemother. 2005 Jul;49(7):2802-6.
Paper
Drug/Drug Interactions
     
 
Antiviral activity and safety of aplaviroc, a CCR5 antagonist, in combination with lopinavir/ritonavir in HIV-infected,
therapy-naïve patients: results of the EPIC study (CCR100136).
Yeni P, Lamarca A, Berger D, et al
HIV Med. 2009 Feb;10(2):116-124
 Abstract
 
FULL-TEXT ARTICLE
The effects of ritonavir and lopinavir/ritonavir on the pharmacokinetics of a novel CCR5 antagonist, aplaviroc, i
n healthy subjects.
Adkison KK, Shachoy-Clark A, Fang L, et al
 Br J Clin Pharmacol. 2006 Sep;62(3):336-44
 Paper
 
Evaluation of the drug interaction potential of aplaviroc, a novel human immunodeficiency virus entry inhibitor,
using a modified cooperstown 5 + 1 cocktail.
Johnson BM, Song IH, Adkison KK, et al
 J Clin Pharmacol. 2006 May;46(5):577-87
 Abstract
   
Efficacy
     
 
A WEEK IN REVIEW FEATURED REPORT
Virologic Failure in Therapy Naive Subjects on Aplaviroc+Lopinavir/Ritonavir (CCR100136):
Detection of Aplaviroc Resistance Requires Clonal Analysis of Envelope.
Kitrinos KM, Amrine-Madsen H, Irlbeck DM, et al
 Antimicrob Agents Chemother. 2008 Dec 15.
 Abstract
 
Virologic Failure in First Line HIV Therapy with a CCR5 Entry Inhibitor (Aplaviroc/Combivir, CCR102881):
NRTI Resistance Regardless of Envelope Tropism.
Demarest JF, Amrine-Madsen H, Irlbeck DM, Kitrinos KM; on behalf of the CCR102881 Clinical Study Team.
 Antimicrob Agents Chemother. 2008 Dec 15.
Abstract
   
Adverse Events
     
 
FULL-TEXT ARTICLE
Hepatotoxicity Observed in Clinical Trials of Aplaviroc (GW873140)
Nichols WG, . Steel HM,. BonnyT, et al
 Antimicrob Agents Chemother. 2008 Mar;52(3):858-65.
 Paper

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