The P-glycoprotein (P-gp) encoded by the multi-drug resistance 1 (MDR1/ABCB1) gene, the breast cancer resistance protein encoded by the ABCG2 gene, and the multidrug resistance-associated proteins 4 and 5 are expressed by the brain endothelial cells and ensure active efflux of lipid-soluble molecules from the brain, reducing penetration of drugs into the brain. This evidence concerns the gene ABCB1 and breast cancer.