Intracellular Drug Concentrations and Transporters: Measurement, Modeling, and Implications for the Liver. Issue 1 (10th April 2013)

• Record Type: Journal Article
• Authors: Chu, X; Korzekwa, K; Elsby, R; Fenner, K; Galetin, A; Lai, Y; Matsson, P; Moss, A; Nagar, S; Rosania, G R; Bai, J P F; Polli, J W; Sugiyama, Y; Brouwer, K L R; International Transporter Consortium
• Is Part Of: Clinical pharmacology & therapeutics. Volume 94:Issue 1(2013)
• Page Start: 126
• Page End: 141
• Publication Date: 2013-04-10
• Subjects: Pharmacology -- Periodicals; Therapeutics -- Periodicals; 615.5
• DOI: 10.1038/clpt.2013.78
• Languages: English
• ISSNs: 0009-9236

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Intracellular concentrations of drugs and metabolites are often important determinants of efficacy, toxicity, and drug interactions. Hepatic drug distribution can be affected by many factors, including physicochemical properties, uptake/efflux transporters, protein binding, organelle sequestration, and metabolism. This white paper highlights determinants of hepatocyte drug/metabolite concentrations and provides an update on model systems, methods, and modeling/simulation approaches used to quantitatively assess hepatocellular concentrations of molecules. The critical scientific gaps and future research directions in this field are discussed.</p> <p> <italic>Clinical Pharmacology &amp; Therapeutics</italic> (2013); <bold>94</bold> 1, 126–141. doi:<ext-link ext-link-type="doi" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink">10.1038/clpt.2013.78</ext-link></p> </abstract>