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Intracellular Drug Concentrations and Transporters : Measurement, Modeling, and Implications for the Liver

Chu, X. (author)
Korzekwa, K. (author)
Elsby, R. (author)
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Fenner, K. (author)
Galetin, A. (author)
Lai, Y. (author)
Matsson, Pär (author)
Uppsala universitet,Institutionen för farmaci
Moss, A. (author)
Nagar, S. (author)
Rosania, G. R. (author)
Bai, J. P. F. (author)
Polli, J. W. (author)
Sugiyama, Y. (author)
Brouwer, K. L. R. (author)
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 (creator_code:org_t)
2013-04-10
2013
English.
In: Clinical Pharmacology and Therapeutics. - : Springer Science and Business Media LLC. - 0009-9236 .- 1532-6535. ; 94:1, s. 126-141
  • Research review (peer-reviewed)
Abstract Subject headings
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  • 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.

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