Human breast cancer resistance protein (BCRP), an ATP-binding cassette (ABC) efflux transporter, is mainly responsible for the transport of many endogenous and xenobiotics. BCRP is expressed in different tissues, such as placental, intestinal epithelium, endothelial cells of brain microvessels, and renal proximal tubular cells. BCRP is considered as one of the key factor for the drug-drug interaction and individual difference in drug therapy. The review will provide an overview of the current knowledge on the discovery of BCRP and its physical function, transport mechanism, substrate and inhibitors, as well as its effect on the drug pharmacokinetics.