Publication Date: 2013-10-31
Edited by Yuichi Sugiyama and Bente Steffansen
With chapters written by leading researchers in the transporter field from academia, pharmaceutical industry, and regulatory agencies, this volume advises on how membrane transporters can be dealt with in academic-industrial drug discovery and pharmaceutical development, as well as from a regulatory perspective. Methods and examples of in vitro characterization of single transporters in intestine, liver, and kidney are described, as well as characterization of substrate overlap between various transporters. Furthermore, probes and biomarkers are suggested for studies of the transporters’ impact on the pharmacokinetics of drug substrates/candidates interacting on transporters. The challenges of translating in vitro observed interaction of transporters into in vivo relevance are discussed, as are the perspectives of applying targeted proteomics and mechanistic modeling in this process.
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