In vitro chemical safety testing methods offer the potential for efficient and economical tools
to provide relevant assessments of human health risk. To realize this potential, methods are …

This white paper addresses current approaches and knowledge gaps concerning methods
to assess the role of transport proteins in drug/metabolite disposition in humans. The …

With efforts to reduce cytochrome P450-mediated clearance (CL) during the early stages of
drug discovery, transporter-mediated CL mechanisms are becoming more prevalent …

Protein expression of major hepatic uptake and efflux drug transporters in human pediatric
(n= 69) and adult (n= 41) livers was quantified by liquid chromatography/tandem mass …

Purpose To develop physiologically based pharmacokinetic (PBPK) model to predict the
pharmacokinetics and drug-drug interactions (DDI) of pravastatin, using the in vitro transport …

Introduction: The sandwich-cultured hepatocyte (SCH) model has become an invaluable in
vitro tool for studying hepatic drug transport, metabolism, biliary excretion and toxicity. The …

Recent studies of membrane transporters have revealed their importance in determining the
pharmacokinetics of transporter substrates. When drug-drug interactions (DDIs) or genetic …

Drug transporter expression in tissues (in vivo) usually differs from that in cell lines used to
measure transporter activity (in vitro). Therefore, quantification of transporter expression in …

Transporters responsible for hepatic uptake and biliary clearance (CLBile) of rosuvastatin
(RSV) have been well characterized. However, the contribution of basolateral efflux …

Since the substrate specificities of OATP1B1, 1B3, and 2B1 are broad and overlapping, the
contribution of each isoform to the overall hepatic uptake is of concern when assessing …