Diabetes is a group of systematic metabolic diseases. In addition to cytochromes P450s, some ATP-binding cassette drug transporters are also under diabetic conditions. Breast cancer resistance protein (BCRP) , an important member of ATP-binding cassette drug transporters, expressed in most of the tissues, is thought to play an important protective role in normal tissues. It was reported that BCRP function and expression were impaired in intestine of diabetes rats, which affects the absorption and efflux of some drugs. Therefore, the alteration of BCRP expression and activity could be of critical importance for the treatment of diabetes mellitus. In this article, we reviewed the relationship between diabetes and