Table 1. List of the most important hepatic transporters, their locations, functions and drugs that act as their inhibitors.

Hepatic transporter	Location in hepatocytes	Function	Inhibitors
BSEP	Canalicular membrane	ATP-dependent transport of bile salts, taxol and pravastatin	Bosentan, cyclosporine, rifampin, troglitazone, sulindac, erythromycin, glibenclamide, progesterone metabolites, estradiol 17β-glucuronide
MDR3	Canalicular membrane	ATP-dependent excretion of phosphatidylcholine	Itraconazole, chlorpromazine, imipramine, haloperidol, ketoconazole, clotrimazole, troglitazone
MRP2	Canalicular membrane	ATP-dependent efflux of numerous drugs, organic anions and bile acids, bile salt-independent bile flow by GSH transport	Cyclosporine, efavirenz, benzbromarone, probenecid
MDR1	Canalicular membrane	ATP-dependent efflux of numerous drugs, organic cations and bile acids	Cyclosporine, carvedilol, clarithromycin, amiodarone, itraconazole, lapatinib, verapamil
BCRP	Canalicular membrane	ATP-dependent efflux of anticancer drugs	Gefitinib, mesylate, 17ß-estradiol, ritonavir, omeprazole, cyclosporine
MRP3	Basolateral membrane	ATP-dependent efflux of drug glucuronide conjugates	Tenofovir, indomethacin, furosemide, probenecid, non-nucleoside reverse transcriptase inhibitors (delavirdine, efavirenz, and nevirapine), and nucleoside reverse transcriptase inhibitors (emtricitabine and lamivudine)
MRP4	Basolateral membrane	ATP-dependent efflux of sulfated drugs and bile acids	Troglitazone sulfate, NSAIDs, phosphodiesterase inhibitors, verapamil, losartan, silymarin, probenecid
NTCP	Basolateral membrane	Uptake of bile-salts from portal blood, transport of rosuvastatin	Cyclosporine, bosentan, troglitazone, propranolol, furosemide, ketoconazole, renin inhibitors and a somatostatin analogue, rifamycin
OATPs	Basolateral membrane	Sodium-independent uptake of bile salts, organic anions, and numerous drugs	Itraconazole, nefazodone, nifedipine, reserpine, diazepam, sulfasalazine

Data from Yang et al.,1 solvobiotech.com,44 Kim et al.,48 and Kalgren et al.51

Abbreviations: BCRP, Breast cancer resistance protein; BSEP, bile salt export pump; MDR, multidrug resistance; MRP, multidrug resistance-associated protein; NSAID, nonsteroidal anti-inflammatory drugs; NTCP, sodium-taurocholate cotransporting polypeptide; OATPs, organic anion transporting polypeptides.