ORGANIC ANION–TRANSPORTING POLYPEPTIDES - Drug Transporters: Molecular Characterization and Role in Drug Disposition - page 85

TABLE 5.3. Substrates and Inhibitors of Human OATPs a
Transporter Substrates Nonsubstrates Inhibitors

Fexofenadine 124 , BSP 15 , 27 , 125 ,T 3 27 ,T 4 27 ,E 2 G 27 ,
E 1 S 27 , 125 , GCA 15 , TCA 15 , 27 , DHEAS 27 ,
deltophin 27 , DPDPE 27 , BQ-123 27 , oubain 27 , 125 ,
PGE 2 2 , N -methylquinine 27 , rosuvastatin 39 ,
pitavastatin 126 , MTX 127 , microcystin-LR 128

Digoxin 27 ,LTC 2 4 Grapefruit juice 94 , orange juice 94 , apple juice 94

OATP1A2

E 1 S 27 , benzylpenicillin, PGE 2 2 ,E 2 G 27 , BSP 27 ,T 2 3 ,
T 2 4 ,E 2 G 27 ,E 1 S 27 , GCA, TCA 27 , DHEAS 27 ,
DPDPE 27 , BQ-123 27 , cerivastatin 73 , 129 ,
atorvastatin 73 , 130 , rosuvastatin 39 , pitavastatin 126 ,
caspofungin 131 , phalloidin 132 , 133 ,
troglitazone-sulfate 134 , rifampin 66 , bilirubin 96 , 97 ,
bilirubin-glucuronides 96 , arsenic 135 , atrasentan 81 ,
valsartan 136 , olmesartan 137 , enalapril 138 , MTX 38 ,
temocaprilat 75 , DADLE 64 , microcystin-LR 128 ,
SN-38 74

Digoxin 27 , oubain 27 ,
N -methylquinine 27 , deltorphin 27

CyA 66 , 67 , FK-506 67 , 132 , rapamycin 132 , glycirrizic
acid 139 , glibenclamide 67 , ketoconazole 140 ,
gemfibrozil 129 , gemfibrozil-glucuronide 129 ,
ciprofibrate 141 , bezafibrate 67 , 141 , clarithromycin 67 ,
erythromycin 67 , indinavir 66 , nelfinavir 66 ,
ritonavir 66 , saquinavir 66 , probenacid 67 , rifamycin
SV 142 , digoxin 67 , verapamil 67 , warfarin 67 ,
MK-571 141 , biochanin A 143 , Genistein 143 ,
epigallocatechin-3-gallate 143 , hyperforin 66

OATP1B1

Fexofenadine 144 , BSP 27 ,T3 27 ,T4 27 ,E 2 G 27 ,E 1 S 27 ,
GCA 27 , TCA 27 , TUDC 145 , GUDC 145 , DHEAS 27 ,
deltophin 27 , DPDPE 27 , BQ-123 27 , oubain 27 ,
PGE 2 , digoxin 27 , rosuvastatin 39 , valsartan 136 ,
pitavastatin 126 , fluo-3 146 , docetaxel 140 ,
paclitaxel 140 , CCK-8 147 , phalloidin 132 , 133 ,
rifampin 66 , 146 , MTX, bilirubin 97 , repaglinide,
telmisartan 65 , olmesartan 137 , enalapril 138 ,
temocaprilat 75 , microcystin-LR 128

N -Methylquinine 27 , PGE 2 2 ,
caspofungin 131 , folate

Ketoconazole 140 , glycirrizic acid 139 , rifamycin SV 142 OATP1B3

BSP 9 ,T 3 ,T 4 ,E 2 G 9 ,E 1 S 9 GCA 9 , TCA 9 , DHEAS 9 ,

deltophin 9 , DPDPE 9 , BQ-123 9 ,
digoxin 9 , oubain 9 ,LTC 4 9 ,

OATP1C1