Most brain tumors are highly resistant to chemotherapy because many chemotherapeutic drugs poorly cross the blood-brain barrier, the blood-cerebrospinal-fluid barrier, and the plasma membrane of the tumor cells. This restricted drug delivery is largely due to the presence of integral plasma membrane proteins belonging to the solute carriers (SLCs) and to the ATP-binding cassette (ABC) superfamily of transporters that decisively determine substance uptake and efflux, respectively, by the barrier-forming cells and the tumor cells. This review focuses on the localization and function of drug-transporting members of both transporter groups in human brain.