Table 2.

Drug transporters putatively involved in forming the BBB, as well as chemotherapy agents that are substrates for each transporter, and compounds used as potential inhibitors of transporter function

TransporterHUGO nameSubstratesInhibitors
P-glycoproteinABCB1Doxorubicin, daunorubicin, docetaxel, paclitaxel, epirubicin, idarubicin, vinblastine, vincristine, etoposideVerapamil, cyclosporine A, quinidine, PSC 833 (valspodar), GF120918 (elacridar), VX-710 (biricodar), LY335979 (zosuquidar), XR9576 (tariquidar)
MRP1ABCC1Etoposide, teniposide, daunorubicin, doxorubicin, epirubicin, melphalan, vincristine, vinblastineProbenecid, sulfinpyrazone, MK-571, some P-glycoprotein inhibitors (e.g., cyclosporin A, verapamil, PSC 833)
MRP2ABCC2Similar to MRP1Probenecid, MK-571, leukotriene C4
MRP3ABCC3Similar to MRP1Sulfinpyrazone, indomethacin, probenecid
MRP4ABCC4Methotrexate, 6-mercaptopurine, thioguianineProbenecid
MRP5ABCC56-Mercaptopurine, thioguanineProbenecid, sildenafil
MRP6ABCC6Actinomycin D, cisplatin, daunorubicin, doxorubicin, etoposideProbenecid, indomethacin
BCRPABCG2Mitoxantrone, methotrexate, SN-38, topotecan, imatinib, erlotinib, gefitinibGF120918, fumitremorgin C