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

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.

SUBMITTER: Chu X 

PROVIDER: S-EPMC3898878 | biostudies-literature | 2013 Jul

REPOSITORIES: biostudies-literature