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aplaviroc

Known as: 4-(4-{[(3R)-1-butyl-3-[(R)-cyclohexylhydroxymethyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undecan-9-yl]methyl}phenoxy)benzoic acid, benzoic acid, 4-(4-(((3R)-1-butyl-3-((R)-cyclohexylhydroxymethyl)-2,5-dioxo-1,4,9- triazaspiro(55)undec-9-yl)methyl)phenoxy)- 
A C-C Chemokine Receptor Type 5 (CCR5) antagonist with activity against HIV-1. Aplaviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.
National Institutes of Health

Related topics

Related topics

6 relations
AK602Aplaviroc Hydrochloride

Broader (3)

BenzoatesPiperazinesSpiro Compounds

Narrower (1)

GW873140

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
2014
2014
Gating function of isoleucine‐116 in TM‐3 (position III:16/3.40) for the activity state of the CC‐chemokine receptor 5 (CCR5)
A conserved amino acid within a protein family indicates a significance of the residue. In the centre of transmembrane helix (TM… 
2011
2011
Allosteric and Orthosteric Sites in CC Chemokine Receptor (CCR5), a Chimeric Receptor Approach*
Background: Characterization of 7TM biology and chemistry is needed generally and within chemokine receptors. Results: A CCR5… 
2010
2010
Potent Inhibition of HIV‐1 Entry with a Chemically Programmed Antibody Aided by an Efficient Organocatalytic Synthesis
Innovative new approaches to HIV-1 prophylaxis and therapy are desperately needed. Despite the successes of highly active… 
2009
2009
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) *
This phase IIb study explored the antiviral activity and safety of the investigational CC chemokine receptor 5 (CCR5) antagonist… 
2008
2008
Virologic Failure in First-Line Human Immunodeficiency Virus Therapy with a CCR5 Entry Inhibitor, Aplaviroc, plus a Fixed-Dose Combination of Lamivudine-Zidovudine: Nucleoside Reverse Transcriptase…
ABSTRACT The CCR102881 (ASCENT) study evaluated the antiviral activity of the novel CCR5 entry inhibitor aplaviroc plus a fixed… 
2008
2008
In Vitro and Clinical Investigation of the Relationship Between CCR5 Receptor Occupancy and Anti‐HIV Activity of Aplaviroc
Aplaviroc (GW873140) binds specifically to human cellular CC chemokine receptor 5 (CCR5) and demonstrates potent anti‐human… 
2008
2008
Formulation development and process scale up of a high shear wet granulation formulation containing a poorly wettable drug.
Aplaviroc 200 mg tablets were made by a high shear wet granulation process. A formulation and process DOE were carried out to… 
Review
2007
Review
2007
CCR5 antagonists: comparison of efficacy, side effects, pharmacokinetics and interactions--review of the literature.
In the context of emerging resistance to antiretroviral agents in HIV medicine, the development of new drugs classes with a novel… 
2006
2006
The effects of ritonavir and lopinavir/ritonavir on the pharmacokinetics of a novel CCR5 antagonist, aplaviroc, in healthy subjects.
AIMS This study assessed the effects of the CYP3A inhibitors lopinavir/ritonavir (LPV/r) on the steady-state pharmacokinetics (PK… 
2005
2005
Trials of aplaviroc halted in treatment-naive patients.
On September 15, 2005, GlaxoSmithKline (GSK) announced that it had halted clinical trials of the CCR5 entry inhibitor, aplaviroc… 
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