AAPS Transporter 2013 - Uptake and Efflux Transporters

AAPS Transporter 2013 - Uptake and Efflux Transporters

Published:  05 March 2013

Comparison of IC50 Values for Prototypical and Clinically-Relevant Probe Substrates and Inhibitors of Selected Uptake and Efflux Transporters

The EMEA Guideline on the Investigation of Drug Interactions (2012) recommends the incorporation of more than one positive control inhibitor into experiments to evaluate the inhibitory potential of investigational drugs on drug transporters. Therefore, the present study was designed to compare the effect of compounds that are prototypical inhibitors or that cause clinically-significant transporter interactions on the transport of compounds that represent either prototypical and/or clinically-relevant transporter substrates with in vitro, cell-based test systems.