This presentation will provide an overview of drug-drug interaction (DDI) guidances as they relate to transporters. The goal of these guidances is to determine whether an investigational drug is a substrate or inhibitor of an efflux or uptake transporter. The guidances describe a general framework for a) performing in vitro experiments, b) interpreting in vitro data to determine the need for clinical DDIs, and c) conducting clinical studies to evaluate the DDI potential of an investigational drug. The classification of investigational drugs as substrates or inhibitors is discussed for each transporter. In vitro assay systems are discussed together with cutoff values based on inhibition potency and inhibitor systemic concentration. The types of clinical DDI studies are defined for classifying investigational drugs as substrates or inhibitors.
Understand the role of uptake and efflux transporters in drug development and regulatory review.
Identify the transporters of interest in regulatory guidances.
Define how an investigational drug is categorized as a transporter substrate or inhibitor.
Understand how in vitro and in vivo transporter studies are conducted.