Details

Autor(en) / Beteiligte

• 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

Titel

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

Ist Teil von

• Clinical pharmacology and therapeutics, 2013-07, Vol.94 (1), p.126-141

Ort / Verlag

United States: Blackwell Publishing Ltd

Erscheinungsjahr

2013

Quelle

Wiley Online Library Journals Frontfile Complete

Beschreibungen/Notizen

• 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. Clinical Pharmacology & Therapeutics (2013); 94 1, 126–141. doi:10.1038/clpt.2013.78