| | ABC transporter | Substrates | Inhibitors |
| | P-glycoprotein (ABCB1) | Anticancer drugs, for example, doxorubicin, daunorubicin, vincristine, etoposide, teniposide, paclitaxel, and methotrexate | 1st generation, for example, verapamil, cyclosporine A, quinidine, quinine, amiodarone, and detergents such as Cremophor EL | | Immunosuppressive agents, for example, cyclosporine A | 2nd generation, for example, PSC-833 (valspodar), GF120918 (elacridar), VX-710 (biricodar), and dexverapamil | | Corticoids, for example, dexamethasone, hydrocortisone, corticosterone, cortisol, and aldosterone | 3rd generation, for example, OC 144-093 (ONT-093), LY335979 (zosuquidar), XR9576 (tariquidar), R101933 (laniquidar), and GF120918 | Analgesics, for example, morphine
HIV protease inhibitors, for example, amprenavir, indinavir, and saquinavir
Cytokines, for example, IL-2, IL-4, and IFN-γ
Antidiarrheal agents, for example, loperamide
Anthelminthic agents, for example, ivermectin and abamectin
Antigout agents, for example, colchicines
Histamine H2-receptor antagonists, for example, cimetidine
Calcium channel blockers, for example, verapamil
Antiepileptic drugs, for example, phenytoin, carbamazepine, lamotrigine, phenobarbital, felbamate, gabapentin, and topiramate
Antiemetics, for example, domperidone and ondansetron
Cardiac glycosides, for example, digoxin
Diagnostic (fluorescent) dyes, for example, rhodamine-123
Antidepressants, for example, amitriptyline, nortriptyline, doxepin, venlafaxine, and paroxetine
Antibiotics, for example, erythromycin, valinomycin, tetracyclines, and fluoroquinolones | |
| | MRP1 (ABCC1) | Anticancer drugs, for example, etoposide, teniposide, vincristine, doxorubicin, daunorubicin, and methotrexate; leukotriene C4 (LTC4), D4, and E4; various glutathione, glucuronide, and sulfate conjugates as well as unconjugated compounds (e.g., fluorescein) | Sulfinpyrazone, probenecid, MK571, LTC4, and some P-gp inhibitors (e.g., cyclosporine A, verapamil, and PSC 833) |
| | MRP2 (ABCC2) | Similar to MRP1 | Similar to MRP1 |
| | MRP3 (ABCC3) | Organic anion transporter with considerable overlap in drug substrates with MRP1 and MRP2 | Classical organic anion transport inhibitors, for example, sulfinpyrazone, indomethacin, and probenecid |
| | MRP4 (ABCC4) | Anticancer drugs, for example, methotrexate, 6-mercaptopurine, and thioguanine | |
| | MRP5 (ABCC5) | cGMP, cAMP, 6-mercaptopurine, thioguanine, and fluorescein | Probenecid and phosphodiesterase inhibitors, for example, trequinsin or sildenafil |
| | MRP6 (ABCC6) | BQ-123 (an anionic cyclopentapeptide and endothelin receptor antagonist) | |
| | BCRP (ABCG2) | Several anticancer drugs; considerable overlap with P-gp, MRP1, and MRP2. Anthracyclines, mitoxantrone, bisantrene, the camptothecins topotecan
and SN-38, prazosin, BNP1350, tomudex, and chlorine E6 | GF120918 (also inhibits P-gp), fumitremorgin C (FTC), and FTC analogs, for example, Ko132, Ko134, CI1033, and estrone |
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