Table 2.

Substrates transported by the different human OATPs

OATP1A2	OATP1B1	OATP1B3	OATP1C1
Hormones and conjugates Estradiol-17β-glucuronide Estrone-3-sulfate DHEA-S Reverse triiodothyronine (rT3) Thyroxine (T4) Triiodothyronine (T3) Prostaglandins Prostaglandin E2 Bile acids Cholate Taurocholate Glycocholate Taurochenodeoxycholate Tauroursodeoxycholate Others DPDPE Drugs Acebutolol, Rosuvastatin, Atenolol, Pitavastatin, Sotalol, Ouabain, Labetalol, Deltorphin II, Nadolol, Ciprofloxacin, Talinolol, Fexofenadine, Saquinavir, Gatifloxacin, Darunavir, Levofloxacin, Imatinib, Methotrexate	Hormones and conjugates Estradiol-17β-glucuronide Estrone-3-sulfate Thyroxine (T4) Triiodothyronine (T3) DHEA-S Prostaglandins Prostaglandin E2 Bile acids Cholate Taurocholate Tauroursodeoxycholate Drugs Atorvastatin, Olmesartan, Bosentan, Phalloidin, Caspofungin, Pitavastatin, Cefazolin, Pravastatin, Cerivastatin, Rapamycin, Darunavir, Rifampicin, Enalapril, Rosuvastatin, Ezetimibe, Saquinavir, Flavopiridol, SN-38, Fluvastatin, Temocapril, Gimatecan, Troglitazone, Lopinavir, Valsartan, Methotrexate	Hormones and conjugates Estradiol-17β-glucuronide Estrone-3-sulfate DHEA-S Testosterone Drugs Atrasentan, Bosentan, Cefadroxil, Cefazolin, Cephalexin, Digoxin, Enalapril, Fexofenadine, Fluvastatin, Gimatecan, Lopinavir, Methotrexate, Demethylphalloin, Paclitaxel, Docetaxel, Methotrexate, Imatinib, Olmesartan, Phalloidin, Pitavastatin, Telmisartan, Rapamycin, Rifampicin, Rosuvastatin, Valsartan, SN-38	Hormones and conjugates Estradiol-17β-glucuronide Estrone-3-sulfate Thyroxine (T4) Triiodothyronine (T3) Reverse triiodothyronine (rT3) Thyroxine sulfate (T4S) Others BSP

OATP2A1	OATP2B1	OATP3A1	OATP4A1
Prostaglandins Prostaglandin E1 ProstaglandinE2 ProstaglandinF2α Prostaglandin H2 Prostaglandin D2 8-iso-prostaglandin F2α Others Thromboxane B2 Drugs Latanoprost	Hormones and conjugates Estrone-3-sulfate DHEA-S Thyroxine (T4) Prostaglandins Prostaglandin E2 Drugs Atorvastatin Bosentan Ezetimibe Fluvastatin Glibenclamide Pitavastatin Pitavastatin Montelukast Rosuvastatin Talinolol	Hormones and conjugates Thyroxine (T4) Estrone-3-sulfate Prostaglandins Prostaglandin E1 Prostaglandin E2 Prostaglandin F2α Drugs Deltorphin BQ-123 Benzylpenicillin Others Vasopressin Arachidonic acid	Hormones and conjugates Estradiol-17β-glucuronide Estrone-3-sulfate Thyroxine (T4) Triiodothyronine (T3) Reverse triiodothyronine (rT3) Bile acids Taurocholate ProstaglandinsProstaglandin E2 Drugs Benzylpenicillin Unoprostone metabolite

Anticancer drugs are highlighted in red.

Abbreviations: BSP, bromosulfophthalein; DHEA-S, dehydroepiandrosterone sulfate; DPDPE, [D-penicillamine²,⁵]enkephalin.