Background: The last 15 years have marked an expansion in our understanding of how ABC transporters modulate the pharmacokinetic properties of drugs. Assays based on different membrane preparations were one of the first methods developed to study ABC transporters. Later, they turned out to be valuable tools to gain insight into the nature of drug-ABC transporter interactions.
Objectives: Membranes prepared from different sources have been used and characterized; based on the biochemical characteristics of the transport process, a number of different assay types have been developed.
Methods: This review focuses on the current experiences on how different membrane-based assays can be utilized in pharmaceutical R&D. Sources of membrane preparations, available assay types and correlation studies between different in-vitro and in-vivo methods are discussed.
Results/conclusion: Membrane-based assays are valuable tools in drug discovery to characterize drug-ABC transporter interactions.