A. Ghosal, M. Barecki‐Roach, R. Ramanathan
Dec 8, 2005
Citations
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Influential Citations
2
Citations
Journal
Retrovirology
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.