TABLE 1

Drugs known to be substrates for liver transporters

Drugs that are given in boldface have pediatric applications. Drugs that are given in italics have high fT values. Drugs that are given in both boldface and italics have pediatric applications and high fT values. SN-38 is the active metabolite of irinotecan.

TransporterSubstrate
NTCPAtorvastatin, fluvastatin, pitavastatin, rosuvastatin, and taurocholate covalently bound drugs
OATP1A2Acebutolol, atenolol, atrasentan, celiprolol, D-penicillamine, deltorphin-II, erythromycin, fexofenadine, imatinib, levofloxacin, lopinavir, methotrexate, microcystin-LR, ouabain, pitavastatin, rosuvastatin, rocuronium, N-methyl quinine, saquinavir, sotalol, thyroxine, talinolol, tebipenem pivoxil, and unaprostone
OATP1B1Atrasentan, atorvastatin, benzylpenicillin, bosentan, caspofungin, cerivastatin, D-penicillamine, enalapril, ezetimibe glucouronide, fexofenadine, fluvastatin, methotrexate, microcystin-LR, olmesartan, ouabain, pitavastatin, phalloidin, pravastatin, repaglinide, rifampicin, rosuvastatin, simvastatin, SN-38, troglitazone-sulfate, temocapril, and valsartan
OATP1B3Atrasentan, amanitin, bosentan, cyclosporin, digoxin, docetaxel, deltorphin-II, D-penicillamine, enalapril, erythromycin, fexofenadine, fluvastatin, imatinib, methotrexate, microcystin, olmesartan, ouabain, paclitaxel, pitavastatin, phalloidin, pravastatin, rifampicin, rosuvastatin, SN-38, telmisartan, and valsartan
OATP2B1Atorvastatin, benzylpenicillin, bosentan, fluvastatin, fexofenadine, glibenclamide, pravastatin, pitavastatin, rosuvastatin, and unaprostone
OAT2Allopurinol, L-ascorbic acid, bumetanide, erythromycin, 5-fluorouracil, methotrexate, paclitaxel, ranitidine, salicylate, tetracycline, taxol, theophylline, and zidovudine
OCT1Acyclovir, azidoprocainamide, berberine, citalopram, cimetidine, cisplatin, famotidine, furamidine, ganciclovir, imatinib, irinotecan, lamivudine, metformin, methoiodide, morphine, oxaliplatin, ondansetron, procainamide, pentamidine, picoplatin, paclitaxel, quinidine, ranitidine, tropisetron, tramadol, and verapamil
OCT3Adefovir, atropine, amantadine, d-amphetamine, cimetidine, clonidine, citalopram, desipramine, diphenhydramine, dizoclipine, etilefrine, granisetron, imipramine, ketamine, lidocaine, Lamivudine, Metformin, Mitoxantrone, Memantine, O-methylisoprenaline, nicotine, phenoxybenzamine, phencyclidine, prazosin, procainamide, quinidine, ranitidine, tropisetron, and verapamil
P-gpAmprenavir, atorvastatin, aldosterone, berberine, corticosterone; cimetidine, cyclosporin A, dexamethasone, digoxin, daunorubicin, doxorubicin, debrisoquine, diltiazem, erythromycin, etoposide, fexofenadine, grapafloxacin, hydrocortisone, indinavir, imatinib, irinotecan, lovastatin, losartan, levofloxacin, loperamide, mitoxantrone, morphine, norverapamil, nelfinavir, paclitaxel, pitavastatin, phenytoin, quinidine, rosuvastatin, ritonavir, rhodamine 123, saquinavir, simvastatin, tacrolimus, taxanes, talinolol, terfenadine, verapamil, vinblastine, and vincristine
BSEPFexofenadine, pravastatin, vinblastine
MRP2Acetaminophen glucuronide, carboxydichlorofluorescein, camptothecin, cerivastatin, cisplatin, doxorubicin, etoposide, fexofenadine, glibenclamide, indomethacin, MTX, mitoxantrone, olmesartan, pitavastatin, pravastatin, rifampin conjugates, rosuvastatin, spiramycin, SN-38 glucouronide, vincristine, and valsartan
BCRPAlbendazole sulfoxide, cerivastatin, ciprofloxacin, daunorubicin, doxorubicin, dirithromycin, erythromycin, epirubicin, genistein, irinotecan, imatinib, lamivudine, methotrexate, MX, norfloxacin, nitrofurantoin, oxfendazole, ofloxacin, pitavastatin, prazosin, pantoprazole, rifampicin, rhodamine 123, rosuvastatin, sulfasalazine, SN-38, testosterone, tamoxifen, topotecan, and zidovudine
MATE1Acyclovir, cephalexin, fexofenadine, gancyclovir, metformin, oxaliplatin
MRP1Adfovir, apicidin, berberine, camptothecins, ciprofloxacin, citalopram, daunorubicin, doxorubicin, difloxacin, etoposide, edatrexate, epirubicin, flutamide, fifloxacin, grepafloxacin, irinotecan, indinavir, idarubicin, methotrexate, pirarubicin, paclitaxel, ritonavir, romidepsin, raltitrexed, SN-38, saquinavir, tomudex, vincristine, and vinblastine
MRP3Acetaminophen glucuronide, etoposide, fexofenadine, MTX, teniposide, and vincristine
MRP4Azidothymidine, lamivudine, methotrexate, PMEA, and stavudine zidovudine
MRP5Adefovir, atorvastatin, 5-flurouracil, methotrexate, PMEA, and rosuvastatin
MRP6Endothelin receptor antagonist BQ-123
OSTα/OSTβDigoxin
  • MTX, methotrexate.