Application of transporter assays for drug discovery and development: an update of the literature.

INTRODUCTION

Determining whether a new drug is a substrate, inhibitor or inducer of efflux or uptake membrane transporters has become a routine process during drug discovery and development. assays are utilized to establish whether a new drug has the potential to be an object (substrate) or precipitant (inhibitor, inducer) in transporter-mediated clinical drug-drug interactions. The findings from these experiments are then used to determine whether further drug interaction studies are necessary for a new drug.

AREAS COVERED

This article provides an update on transporter assays, focusing on new uses of transfected cells, time-dependent inhibition, transporter induction, and complex model systems.

EXPERT OPINION

The newer assays add to the toolbox in defining new drugs as transporter substrates, inhibitors, or inducers. Complex models such as spheroids, organoids, and microphysiological systems require standardization and further research with model transporter substrates and inhibitors. In drug discovery, the more traditional transporter assays may be employed as substrate and inhibitor screening assays. In drug development, more complex cell models can be employed in later drug development to better understand how transporter(s) are involved in the absorption, distribution, and excretion of new drugs.