Inhibitor |
IC50 (μM) |
Ki (μM) |
Substrate used |
Cell System |
Reference |
17beta-estradiol |
12.9 |
|
Estradiol-17beta-glucuronide1,2 |
CHO-OATP1B3 |
Gui, 2008 |
Amprenavir |
19.1 |
13.1 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Amprenavir |
38 |
|
Estradiol-17beta-glucuronide1,2 |
HEK-OATP1B3 |
Chiou, 2014 |
Antamanide |
0.7 |
0.7 |
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Antamanide |
15 |
|
Bromsulphthalein |
MDCK II-OATP1B3 |
Letschert, 2006 |
Asunaprevir3 |
0.65 |
|
CCK-81 |
HEK293-OATP1B3 |
Furihata, 2014 |
Atazanavir |
3 |
2 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Atazanavir |
0.4 |
0.37 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Boceprevir |
4.9 |
|
Bromsulphthalein |
MDCKII-OATP1B3 |
Chu, 2013 |
Bromsulphthalein |
3 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Bromsulphthalein |
1.4 |
1 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Carbamazepine |
510 |
|
Estradiol-17beta-glucuronide1,2 |
CHO-OATP1B3 |
Gui, 2008 |
Carfilzomib |
0.9 |
|
FMTX |
CHO-OATP1B3 |
Leibovici, 1989 |
Cholecystokinin octapeptide |
10 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Clarithromycin4 |
32 |
|
Bromsulphthalein |
HEK293-OATP1B3 |
Seithel, 2007 |
Cyclosporine2,4 |
0.3 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Cyclosporine2,4 |
0.8 |
|
Bosentan3 |
CHO-OATP1B1 |
Treiber, 2007 |
Cyclosporine2,4 |
0.3 |
|
Bromsulphthalein |
MDCK II-OATP1B3 |
Letschert, 2006 |
Cyclosporine2,4 |
1.3 |
1.2 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Cyclosporine2,4 |
0.06 |
|
Rosuvastatin1,3 |
HeLa-OATP1B3 |
Ho, 2006 |
Dabrafenib |
4.7 |
|
Estradiol-17beta-glucuronide1,2 |
HEK-MSRII-OATP1B3 |
Ellens, 2017 |
Daclatasvir |
3.27 |
|
CCK-81 |
HEK293-OATP1B3 |
Furihata, 2014 |
Darolutamide |
39.3 |
|
Atorvastatin3 |
HEK293-OATP1B3 |
Zurth, 2019 |
Darunavir |
4.8 |
3.3 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Dasatinib |
5.76 |
|
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Pahwa, 2017 |
Digoxin |
1 |
0.7 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Dovtinib |
105.2 |
|
8-fluorescein-cAMP |
HEK293-OATP1B3 |
Weiss, 2014 |
Doxorubicin |
41 |
38 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Dronedarone hydrochloride |
1.12 |
|
FMTX |
CHO-OATP1B3 |
Leibovici, 1989 |
Erlotinib |
44 |
41 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Erythromycin4 |
34 |
|
Bromsulphthalein |
HEK293-OATP1B3 |
Seithel, 2007 |
Estrone sulfate1,2 |
97.1 |
|
Cholecystokinin octapeptide |
HEK293-OATP1B3 |
Ishiguro, 2006 |
Everolimus |
3.7 |
|
Mycophenolic acid 7-O-glucuronide |
HEK293-OATP1B3 |
Farasyn, 2019 |
Fexofenadine3 |
83.3 |
|
CCK-81 |
HEK293-OATP1B3 |
Shimizu, 2005 |
Fexofenadine3 |
|
205 |
Estrone sulfate1,2 |
HEK293-OATP1B3 |
Shimizu, 2005 |
Fosinopril |
5.19 |
|
FMTX |
CHO-OATP1B3 |
Leibovici, 1989 |
Glibenclamide |
9.8 |
8.1 |
Bromsulphthalein |
HEK293-OATP1B3 |
Klatt, 2013 |
Glimepiride |
40.9 |
|
Bromsulphthalein |
HEK293-OATP1B3 |
Klatt, 2013 |
Gliquidone |
1.17 |
|
FMTX |
CHO-OATP1B3 |
Leibovici, 1989 |
Indinavir |
12.3 |
8.5 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Indinavir |
16 |
|
Estradiol-17beta-glucuronide1,2 |
HEK-OATP1B3 |
Chiou, 2014 |
Indometacin |
41 |
8 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Lapayonib |
33.78 |
|
FMTX |
CHO-OATP1B3 |
Leibovici, 1989 |
Lithocholate |
6.8 |
|
Estradiol-17beta-glucuronide1,2 |
CHO-OATP1B3 |
Gui, 2008 |
Lopinavir |
2 |
1.4 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Mevinolin |
92.6 |
|
Estradiol-17beta-glucuronide1,2 |
CHO-OATP1B3 |
Gui, 2008 |
Mifepristone |
5.3 |
|
Estradiol-17beta-glucuronide1,2 |
CHO-OATP1B3 |
Gui, 2008 |
MK-571 |
0.5 |
0.2 |
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
MK-571 |
0.3 |
|
Bromsulphthalein |
MDCK II-OATP1B3 |
Letschert, 2006 |
Montelukast |
15 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Montelukast |
0.5 |
|
Bromsulphthalein |
MDCK II-OATP1B3 |
Letschert, 2006 |
Nateglinide3 |
45.6 |
|
CCK-81 |
MDCKII-OATP1B3 |
Meyer, 2014 |
Nobiletin |
6.6 |
|
8-fluorescein-cAMP |
HEK293 cells |
Bajraktari-Sylejmani, 2020 |
Paclitaxel3 |
2 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Paclitaxel3 |
4 |
|
Bromsulphthalein |
MDCK II-OATP1B3 |
Letschert, 2006 |
Paclitaxel3 |
0.5 |
|
Estradiol-17beta-glucuronide1,2 |
CHO-OATP1B3 |
Gui, 2008 |
Penicillin G |
25 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Pravastatin1,3 |
62 |
57 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Prednisolone phosphate |
75 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Probenecid |
|
130 |
Fexofenadine3 |
HEK293-OATP1B3 |
Tahara, 2006 |
Rapamycin |
0.4 |
|
FMTX |
CHO-OATP1B3 |
Leibovici, 1989 |
Repaglinide3 |
5.6 |
|
Bromsulphthalein |
HEK293-OATP1B3 |
Bachmakov, 2008 |
Rifampicin2 |
2.1 |
|
8-fluorescein-cAMP |
HEK293 cells |
Bajraktari-Sylejmani, 2020 |
Rifampicin2 |
0.8 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Rifampicin2 |
1.6 |
|
Bosentan3 |
CHO-OATP1B1 |
Treiber, 2007 |
Rifampicin2 |
|
5 |
Bromsulphthalein |
OATP1B3-expressing oocytes |
Vavricka, 2002 |
Rifampicin2 |
1.5 |
|
Bromsulphthalein |
MDCK II-OATP1B3 |
Letschert, 2006 |
Rifampicin2 |
1.3 |
0.9 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Rifampicin2 |
2.6 |
|
Estradiol-17beta-glucuronide1,2 |
CHO-OATP1B3 |
Gui, 2008 |
Rifampicin2 |
1.5 |
1.4 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Rifamycin SV2 |
|
3 |
Bromsulphthalein |
OATP1B3-expressing oocytes |
Vavricka, 2002 |
Rilpivirine |
6.1 |
|
8-fluorescein-cAMP |
HEK293-OATP1B3 |
Weiss, 2013 |
Ritonavir4 |
3.6 |
2.5 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Ritonavir4 |
4.4 |
4 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Rosiglitazone |
10.9 |
|
Bromsulphthalein |
HEK293-OATP1B3 |
Bachmakov, 2008 |
Roxithromycin |
37 |
|
Bromsulphthalein |
HEK293-OATP1B3 |
Seithel, 2007 |
Sacubitril |
3.81 |
|
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Ayalasomayajula, 2016 |
Saquinavir |
4.1 |
2.8 |
Cholyl-glycylamido-fluorescein (CGamF) |
CHO-OATP1B3 |
Annaert, 2010 |
Saquinavir |
0.47 |
|
Estradiol-17beta-glucuronide1,2 |
HEK-OATP1B3 |
Chiou, 2014 |
Sildenafil |
0.8 |
|
Bosentan3 |
CHO-OATP1B1 |
Treiber, 2007 |
Silibinin dihemisuccinate |
0.4 |
|
Amanitin |
MDCK II-OATP1B3 |
Letschert, 2006 |
Silibinin dihemisuccinate |
1 |
|
Bromsulphthalein |
MDCK II-OATP1B3 |
Letschert, 2006 |
Simeprevir4 |
0.22 |
|
CCK-81 |
HEK293-OATP1B3 |
Furihata, 2014 |
Sinensetin |
21.1 |
|
8-fluorescein-cAMP |
HEK293 cells |
Bajraktari-Sylejmani, 2020 |
Sirolimus |
1.3 |
|
Mycophenolic acid 7-O-glucuronide |
HEK293-OATP1B3 |
Farasyn, 2019 |
Sofosbuvir |
61.9 |
|
CCK-81 |
HEK293-OATP1B3 |
Furihata, 2014 |
Sulfasalazine |
12 |
11 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Tangeretin |
5.6 |
|
8-fluorescein-cAMP |
HEK293 cells |
Bajraktari-Sylejmani, 2020 |
Telaprevir |
9.69 |
|
CCK-81 |
HEK293-OATP1B3 |
Furihata, 2014 |
Telithromycin |
11 |
|
Bromsulphthalein |
HEK293-OATP1B3 |
Seithel, 2007 |
Tetrabromobisphenol A |
12.1 |
|
Fluorescein |
CHO cells |
Bruyere, 2017 |
Tolbutamide |
10 |
|
CCK-81 |
MDCKII-OATP1B3 |
Meyer, 2014 |
Trametinib |
30.82 |
|
FMTX |
CHO-OATP1B3 |
Leibovici, 1989 |
Troglitazone |
15.7 |
|
Estradiol-17beta-glucuronide1,2 |
CHO-OATP1B3 |
Gui, 2008 |
Vincristine |
11 |
9.8 |
Estradiol-17beta-glucuronide1,2 |
HEK293-OATP1B3 |
Karlgren, 2012 |
Zafirlukast |
4.96 |
|
FMTX |
CHO-OATP1B3 |
Leibovici, 1989 |
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022