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Clin Pharmacol Ther. 2013 Jul;94(1):126-41. doi: 10.1038/clpt.2013.78. Epub 2013 Apr 10.

Intracellular drug concentrations and transporters: measurement, modeling, and implications for the liver.

Author information

1
Department of Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Rahway, New Jersey, USA. xiaoyan_chu@merck.com

Abstract

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.

PMID:
23588320
PMCID:
PMC3898878
DOI:
10.1038/clpt.2013.78
[Indexed for MEDLINE]
Free PMC Article

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