The treatment of brain tumors and neurodegenerative diseases, represents an ongoing challenge. In
Central Nervous System (CNS) the achievement of therapeutic concentration of chemical agents is complicated by
the presence of distinct set of efflux proteins, such as ATP-Binding Cassette (ABC) transporters localized on the
Blood-Brain Barrier (BBB). The activity of ABC transporters seems to be a common mechanism that underlies the
poor response of CNS diseases to therapies.
The molecular characterization of Breast Cancer Resistance Protein (BCRP/ABCG2), as an ABC transporter
conferring multidrug resistance (MDR), has stimulated many studies to investigate its activity on the BBB, its involvement in physiology
and CNS diseases and its role in limiting the delivery of drugs in CNS.
In this review, we highlight the activity and localization of BCRP on the BBB and the action that this efflux pump has on many
conventional drugs or latest generation molecules used for the treatment of CNS tumors and other neurodegenerative diseases.