Currently, chemotherapy is one of the mainstays of oncologic therapies. But the efficacy
of chemotherapy is often limited by drug resistance and severe side effects. Consequently, it is
becoming increasingly important to investigate the underlying mechanism and overcome the
problem of anticancer chemotherapy resistance. The solute carrier organic anion transporter family
member 1B3 (SLCO1B3), a functional transporter normally expressed in the liver, transports a
variety of endogenous and exogenous compounds, including hormones and their conjugates as well
as some anticancer drugs. The extrahepatic expression of SLCO1B3 has been detected in different
cancer cell lines and cancer tissues. Recently, accumulating data indicates that the abnormal
expression and function of SLCO1B3 are involved in resistance to anticancer drugs, such as
taxanes, camptothecin and its analogs, SN-38, and Androgen Deprivation Therapy (ADT) in breast,
prostate, lung, hepatic, and colorectal cancer, respectively. Thus, more investigations have been
implemented to identify the potential SLCO1B3-related mechanisms of cancer drug resistance. In
this review, we focus on the emerging roles of SLCO1B3 protein in the development of cancer
chemotherapy resistance and briefly discuss the mechanisms of resistance. Elucidating the function
of SLCO1B3 in chemoresistance may bring out novel therapeutic strategies for cancer treatment.