Table 3.
Major drug transporters, their location, and common substrates.
| Transporter | Tissues/cells | Selected substrates | Selected inhibitors |
|---|---|---|---|
| P-gp | Intestinal enterocytes, kidney proximal tubule, hepatocytes, brain endothelial cells, and placenta | Glyburide, digoxin, loperamide, ritonavir, and St. John's Wort | Verapamil and cyclosporine |
| BCRP | Intestinal enterocytes, hepatocytes, kidney proximal tubule, brain endothelial cells, placenta, and mammary glands | Glyburide, statins, porphyrins, and methotrexate | Oestrone and 17 β-estradiol |
| MRP2 | Hepatocytes, kidney proximal tubule, and enterocytes (luminal) | Glutathione and glucuronide conjugates and methotrexate | Cyclosporine and efavirenz |
| MRP3 | Hepatocytes, kidney proximal tubule, and enterocytes (basolateral) | Glyburide, estradiol 17 β-glucuronide, methotrexate, and glucuronate conjugates | Delavirdine and efavirenz |
| MRP4 | Kidney proximal tubule, choroid plexus, hepatocytes, and platelets | Furosemide, adefovir, tenofovir, and methotrexate | Celecoxib and diclofenac |
| MDR3 | Hepatocytes | Digoxin | Verapamil and cyclosporine |
| OAT1 | Kidney proximal tubule and placenta | Acyclovir, zidovudine, lamivudine, adefovir, and cidofovir | Probenecid and novobiocin |
| OAT3 | Kidney proximal tubule, choroid plexus, and blood–brain barrier | NSAIDs, cefaclor, ceftizoxime, and furosemide | Probenecid and novobiocin |
| OCT1 | Hepatocytes and endothelial cells | Metformin, N-methylpyridinium, pindolol, procainamide, ranitidine, and amantadine | Quinine, quinidine, and disopyramide |
| OCT2 | Kidney proximal tubules and peripheral neurons | Metformin and N-methylpyridinium | Cimetidine, cetirizine, and quinidine |
| OATP2B1 | Hepatocytes and endothelial cells | Glyburide, statins, and fexofenadine | Rifampicin and cyclosporine |
| MATE1 | Kidney proximal tubule, liver, and skeletal muscle | Metformin and N-methylpyridinium | Cimetidine, quinidine, and procainamide |
| MATE2-K | Kidney proximal tubule | Metformin and N-methylpyridinium | Cimetidine, quinidine, and pramipexole |
| PEPT1 | Intestinal enterocytes and kidney proximal tubule | Cephalexin, cefadroxil, valacyclovir, enalapril, and captopril | Glycyl-proline |
| PEPT2 | Kidney proximal tubule, choroid plexus, and lung | Cephalexin, valacyclovir, enalapril, and captopril | Zofenopril and fosinopril |