Abstract
Aplaviroc (873140) is a novel spirodiketopiperazine CCR5 antagonist that binds specifically to human CCR5 and allosterically inhibits HIV entry. Aplaviroc has exhibited potent in vivo antiviral activity (1.66 log decrease in viral load at nadir) following 10 days of monotherapy. In vitro studies of antiviral activity demonstrate that aplaviroc is active against HIV isolates from a variety of clades as well as those resistant to current HIV therapies targeting RT, PR, and gp41. In vitro studies suggest prolonged CCR5 receptor occupancy (RO) by aplaviroc with an offset halflife of >100 hours. In vivo studies following short term aplaviroc administration using CCR5-specific mAb demonstrate substantial and prolonged CCR5 RO (>50%) by aplaviroc, when plasma drug levels were undetectable, observed for approximately 5 days.
Highlights
national Meeting of The Institute of Human Virology Meeting abstracts – A single PDF containing all abstracts in this Supplement is available here. [link 'here' using 'a href' to: http://www.biomedcentral.com/content/pdf/1742-4690-2-S1
Aplaviroc has exhibited potent in vivo antiviral activity (1.66 log decrease in viral load at nadir) following 10 days of monotherapy
In vitro studies of antiviral activity demonstrate that aplaviroc is active against HIV isolates from a variety of clades as well as those resistant to current HIV therapies targeting RT, PR, and gp41
Summary
Update on Aplaviroc: An HIV Entry Inhibitor Targeting CCR5 James F Demarest*‡ and the Aplaviroc Project Team Address: Duke University AIDS Center, Durham, North Carolina, USA * Corresponding author ‡Presenting author from 2005 International Meeting of The Institute of Human Virology Baltimore, USA, 29 August – 2 September 2005 Published: 8 December 2005 Retrovirology 2005, 2(Suppl 1):S13 doi:10.1186/1742-4690-2-S1-S13
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