This article is part of the supplement: Abstracts of the Ninth International Congress on Drug Therapy in HIV Infection .

Poster presentation

Antivirals and nuclear receptor activation of CYP3A4 and 2B6

J Svard¹, JP Spiers¹, F Mulcahy² and M Hennessy¹

¹  Trinity College Dublin, Dublin, Ireland

²  St James' Hospital, Dublin, Ireland

corresponding author email

from Ninth International Congress on Drug Therapy in HIV Infection
Glasgow, UK. 9–13 November 2008

Journal of the International AIDS Society 2008, 11(Suppl 1):P236doi:10.1186/1758-2652-11-S1-P236

Published:	10 November 2008

First paragraph (this article has no abstract)

The orphan nuclear receptors PXR (pregnane × receptor) and CAR (constitutive androstane receptor) are xenosensors that mediate drug-induced transcription of genes involved in drug metabolism, clearance and disposition. Early studies indicate that ritonavir (RTV), saquinavir (SQV) and efavirenz (EFV) modulate CYP3A4 expression via PXR, albeit at non-clinical concentrations. However, little information is available regarding newer antiretroviral agents or the effects on transcriptional regulation of CYP2B6. This study investigates the role of PXR and CAR in the transcriptional regulation of CYP3A4 and CYP2B6 by ART.