Abstract
Vicriviroc (formerly SCH 417690), a CCR5 receptor antagonist, is currently under investigation for the treatment of HIV infection. Human liver microsomes (HLM) metabolized vicriviroc via N-oxidation (M2/M3), Odemethylation (M15), N, N-dealkylation (M16), Ndealkylation (M41) and carboxylic acid formation (M35b/M37a). The metabolites generated under in vitro conditions were also detected in clinical studies after oral doses of vicriviroc. Incubation with recombinant human CYP3A4 formed all metabolites listed above, while CYP2C9 formed M15 and CYP3A5 formed M2/M3 and M41.
Highlights
Characterization of the In Vitro Human Liver Cytochrome P450 (CYP) Mediated Metabolism and Inhibition Potential of Vicriviroc
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
The metabolites generated under in vitro conditions were detected in clinical studies after oral doses of vicriviroc
Summary
Characterization of the In Vitro Human Liver Cytochrome P450 (CYP) Mediated Metabolism and Inhibition Potential of Vicriviroc Anima Ghosal*, Mary Barecki-Roach, Ragulan Ramanathan, Yuan Yuan and Address: Schering-Plough Research Institute, Kenilworth, NJ 07033, USA Email: Anima Ghosal* - anima.ghosal@spcorp.com * Corresponding author ‡Presenting author from 2005 International Meeting of The Institute of Human Virology Baltimore, USA, 29 August – 2 September 2005
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