TABLE 3

Endogenous and xenobiotic substrates


Transporter

Substrates
P-gp Daunorubicin, doxorubicin, vinblastine, vincristine, irinotecan, topotecan, etoposide, colchicine, paclitaxel, ritonavir, indinavir, digoxin, fexofenadine, cortisol, morphine, loperamide, ivermectin
MDR3 Phosphatidylcholine, digoxin, vinblastine, paclitaxel, aureobasidin A
BSEP Bile salts
MRP1 Glutathione-, glucuronate-, and sulfate-conjugated organic anions; estradiol 17-β-d-glucuronide (E217βG), leukotriene C4 (LTC4), S-(2,4-dinitrophenyl) glutathione (DNP-SG)
MRP2 Glutathione-, glucuronate-, and sulfate-conjugated organic anions; E217βG, LTC4, bilirubin glucuronide, DNP-SG, pravastatin, SN-38 glucuronide, irinotecan
MRP3 Epipodophyllotoxins, methotrexate, vincristine, etoposide, E217βG, LTC4, glycocholate, glycochenodeoxycholate, taurodeoxycholate, taurochenodeoxycholate, glucuronides
MRP4 Steroid and bile acid conjugates, nucleoside analogs, 6-mercaptopurine (6-MP), 9-(2-phosphonylmethoxyethyl)adenine (PMEA), cAMP, cGMP
MRP5 6-MP, PMEA, low affinity for cyclic nucleotides
MXR
Anthracyclines, mitoxantrone, bisantrene, topotecan, SN-38