Role of drug transporters: an overview based on knockout animal model studies

Abstract

Drug transporters play an important role in the absorption, distribution, and elimination of drugs and their metabolites. Drug transporters can be subdivided into solute carrier (SLC) and ATP-binding cassette (ABC) family. SLC transporters are secondary active transporters that work as uptake transporters, whereas ABC transporters are primary active transporters that work as efflux transporters. Knockout animal models that lack a specific transporter gene(s) are excellent tools to study the function of a drug transporter. In recent times, various gene knockout animal models have been developed that have significantly contributed in defining the roles of these transporters in vivo; for example, the roles of multidrug resistance protein, breast cancer resistance protein, multidrug resistance–related proteins, organic anionic transporters, organic cationic transporters, and organic anion transporting polypeptides have received great attention after their knockout models were generated. In this review, we aim to summarize the in vivo roles of drug transporters based on studies using knockout animal models.