In vitro and in vivo models for assessing drug efflux transporter activity

Determining the activity of drug efflux transport proteins has important implications in the identification of substrates and/or inhibitors of the various transport systems, as well as mechanistic determination of localization, and functional role of the transporters in absorption, distribution and elimination of compounds in the body. This review examines both in vitro and in vivo approaches used to determine drug efflux transporter activity, their applications, and advantages and potential limitations.