Table 1

Xenobiotics, used as drugs, which interact with MDR1 or MRP2 either as (predominantly) inhibitor and/or substrate (current state of knowledge)

MDR1MRP2
All compounds in the respective upper (common) boxes are substrates or inhibitors of both MDR1 and MRP2. Several inhibitors might also be found to be substrates in the future. Vice versa, substrates may also inhibit or stimulate MDR1 activity. Additional explanations as well as other xenobiotic substrates are given in the text.
Substrates
Grepafloxacin22,23
Octreotide24
Saquinavir25,26
Vinblastine27,28
Celiprolol,29 cyclosporine11Arsenite44,45
Digitoxin,30 digoxin30Cisplatin46
Docetaxel,31 doxorubicin32Methotrexate47
Erythromycin,33 fexofenadine16Rifampicin48
Hypericin (from St John’s wort),34 indinavir35Sulphinpyrazone28
Ivermectin,36 lansoprazole37Vincristine46
Loperamide,38 losartan39Ceftriaxone49
Lovastatin,33 mibefradil40
Morphine,38 nelfinavir35
Phenytoin,41 tacrolimus12
Talinolol,42 terfenadine33
Vecuronium43
Inhibitors
Ritonavir26
Carvedilol,50 doxazosin50Furosemide55
Hydroxyzine,51 ketoconazole52Glibenclamide56
Omeprazole,37 pantoprazole37MK-57123
Quinidine,53 simvastatin54Probenecid55
Valspodar (PSC-833),52 verapamil53