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. Author manuscript; available in PMC: 2014 Apr 24.
Published in final edited form as: Curr Neurol Neurosci Rep. 2008 May;8(3):235–241. doi: 10.1007/s11910-008-0036-8

Table 1.

Drug efflux transporters at the blood-brain barrier

Transporter Location Anticancer agent substrates
P glycoprotein Luminal of BBB, luminal
of B-CSF barrier		 Doxorubicin, epirubicin, daunorubicin, docetaxel, paclitaxel,
vinblastine, vincristine, etoposide, methotrexate
MRP1 Luminal of BBB, basolateral
of B-CSF barrier		 Similar to P-gp plus teniposide and melphan
MRP2 Luminal Similar to P-gp
MRP3 Luminal Similar to P-gp
MRP4 Luminal and basolateral Methotrexate, 6-mercaptopurine, thioguanine
MRP5 Luminal 6-mercaptopurine, thioguanine
MRP6 Luminal Cisplatin, doxorubicin, etoposide, actinomycin D
Breast cancer
 resistance protein		 Luminal Methotrexate, topotecan, mitoxantrone,
imatinib, eriotinib, gefitinib
Organic anion and
 cation transporters		 Luminal and basolateral
of BBB, B-CSF barrier		 Unknown, but likely operate via ionic and drug gradients
rather than energy-dependent transport

BBB—blood-brain barrier; B-CSF—blood-cerebrospinal fluid barrier; MRP—multidrug resistance protein; P-gp—P glycoprotein.