Main description:

Transporters in Drug Development examines how membrane transporters can be dealt with in academic-industrial drug discovery and pharmaceutical development as well as from a regulatory perspective. The book describes methods and examples of in vitro characterization of single transporters in the intestines, liver and kidneys 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 explored, and the book highlights perspectives of applying targeted proteomics and mechanistic modeling in this process.

Contents:

Membrane Transporters in ADME.- In Vitro Characterization of Transporter Mediated Permeability.- In Vitro Characterization of Interactions with Drug Transporting Proteins.- In Vivo Characterization of Interactions on Transporters.- Application of Targeted Proteomics in ADME for IVIVE.- Prediction of Transporter Mediated Drug-Drug Interaction from In Vitro Data.- Accounting for Transporters in Renal Clearance: Towards a Mechanistic Kidney Model (Mech KiM).- Analysis of Intestinal Transporters.- Analysis of Hepatic Transport Proteins.- Analysis of Renal Transporters.- The Role of Transporters During Drug Development: Regulatory Science Perspective from the FDA.- Industrial Evaluation of Drug Transporters in ADME.