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SLCO1B3

Synonyms: LST-3TM13, LST3, OATP1B3, OATP8, SLC21A8

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Expression Data

Expression data for other tissues could be found in http://pharmacogenetics.ucsf.edu/gtex/index.html

Asterisk indicates important transporters in the organ as identified in the organ diagram.

Organ Source Relative Expression
Kidney Mean across all PMT Samples    0.0689
Liver* Mean across all PMT Samples 8.511
Note that relative expression values should only be compared between entries of the same source.

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In Vitro Substrates

Substrate Km (μM) Cell System Reference
17beta-Glucuronosyl estradiol 5.4 HEK293-OATP1B3 Cui, 2001
Amanitin 3.7 MDCK II-OATP1B3 Letschert, 2006
Amanitin 3.7 MDCK--OATP1B3 McFeely, 2019
Atorvastatin3 0.73 HEK293-OATP1B3 Karlgren, 2012
Bilirubin 0.0391 OATP1B3-expressing oocytes Briz, 2003
Bosentan3 141 CHO-OATP1B3 Treiber, 2007
Bromsulphthalein 3.3 HEK293-OATP1B3 Cui, 2001
Bromsulphthalein 0.4 OATP1B3-expressing oocytes Kullak-Ublick, 2001
Bromsulphthalein 2.2 MDCKII-ABCC2-OATP1B3 Kopplow, 2005
Cefadroxil 4.15 oocytes-OATP1B3 Nakakariya, 2008
Cefazolin 3.89 oocytes-OATP1B3 Nakakariya, 2008
Cefditoren 5.87 oocytes-OATP1B3 Nakakariya, 2008
Cefmetazole 0.71 oocytes-OATP1B3 Nakakariya, 2008
Cefoperazone 1.95 oocytes-OATP1B3 Nakakariya, 2008
Cephalexin 1.19 oocytes-OATP1B3 Nakakariya, 2008
Cholecystokinin octapeptide 3.82 HEK293-OATP1B3 Hirano, 2004
Cholecystokinin octapeptide 16.5 CHO-OATP1B3 Poirier, 2009
Cholyl-glycylamido-fluorescein (CGamF) 2.2 CHO-OATP1B3 Annaert, 2010
Digoxin ND OATP1B3-expressing oocytes Kullak-Ublick, 2001
Dioscin 2.08 HEK293-OATP1B3 McFeely, 2019
Docetaxel3 2.2 CHO-OATP1B3 de, 2012
Estradiol-17beta-glucuronide1,2 24.6 HEK293-OATP1B1 Hirano, 2004
Estradiol-17beta-glucuronide1,2 15.8 CHO-OATP1B3 Gui, 2008
Estrone sulfate1,2 58 CHO-OATP1B3 Gui, 2008
Fexofenadine3 108 HEK293-OATP1B3 Shimizu, 2005
Fluo-3 3.1 CHO-OATP1B3 Gui, 2008
Fluvastatin 7 MDCK II-OATP1B3 Kopplow, 2005
Gadoxetic Acid 0.532 HEK293-OATP1B3 Nassif, 2012
Glibenclamide 15.36 HEK-OATP1B3 Chen, 2018
Glipizide 41.29 HEK293-OATP1B3 Chen, 2018
Glycoursodeoxycholate 24.7 HEK293-OATP1B3 Maeda, 2006
Irbesartan 11.9 HEK293-OATP1B3 McFeely, 2019
Mesalazine 77.4 HEK293-OATP1B3 Konig, 2011
Methotrexate 24.7 OATP1B3-expressing oocytes Abe, 2001
Methotrexate 39.4 MDCK-OATP1B3 Abe, 2001
Monoglucuronosyl bilirubin 0.5 HEK293-OATP1B3 Cui, 2001
Nafcillin 0.07 oocytes-OATP1B3 Nakakariya, 2008
Nilotinib 7.84 HEK293-OATP1B3 McFeely, 2019
Olmesartan 71.8 OATP1B3-expressing oocytes Nakagomi-Hagihara, 2006
Olmesartan 44.2 HEK293-OATP1B3 Yamada, 2007
Paclitaxel3 6.79 OATP1B3-expressing oocytes Smith, 2005
Pitavastatin1,3 3.25 HEK293-OATP1B3 Hirano, 2004
Pitavastatin1,3 3.8 OATP1B3-expressing oocytes Fujino, 2005
Rifampicin2 2.3 OATP1B3-expressing oocytes Vavricka, 2002
Rosuvastatin1,3 9.8 HeLa-OATP1B3 Ho, 2006
Rosuvastatin1,3 14.2 HEK293-OATP1B3 Kitamura, 2008
Taurocholate 5.8 OATP1B3-expressing oocytes Abe, 2001
Tauroursodeoxycholate 15.9 HEK293-OATP1B3 Maeda, 2006
Telmisartan1 0.81 HEK293-OATP1B3 Ishiguro, 2006
Telmisartan glucuronide 3.4 HEK293-OATP1B3 Ishiguro, 2008
Triiodothyronine 6.4 OATP1B3-expressing oocytes Abe, 2001
Valsartan 18.2 HEK293-OATP1B3 Kreel, 1991
Valsartan 18.2 HEK293-OATP1B3 Yamashiro, 2006
Valsartan 23.5 CHO-OATP1B3 Poirier, 2009
Vandetanib 4.37 CHO-OATP1B3 McFeely, 2019

ND = not determined
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


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In Vitro Inhibitors

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

ND = not determined
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


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Clinical Drug-Drug Interactions

DDI Implicated Transporter Interacting Drug Affected Drug AUC Cmax CLR CL/F t1/2 Effect on PD Reference More Details
Clinical PK Impact(fold change)
1 ABCG2/OATPs Atazanavir / Ritonavir4 Rosuvastatin1,3 3.1 7.0 ND ND ND ND Busti, 2008 DDI 1
2 OATP1B1, OATP1B3 Atazanavir/ritonavir Glecaprevir 6.53 4.51 ND ND ND Yu, 2019 DDI 2
3 OATP1B1/OATP1B3 (ABCB1/ABCG2) Atazanavir/ritonavir Glecaprevir 6.53 4.51 ND ND ND ND Yu, 2019 DDI 3
4 OATP1B1, OATP1B3 Atorvastatin3 Glecaprevir/pibrentasvir 8.28 22.00 ND ND ND Yu, 2019 DDI 4
5 OATP1B3 Cefiderocol Rosuvastatin1,3 1.18 1.25 ND NR 1.21 Katsube, 2018 DDI 5
6 OATP1B1, OATP1B3,OATP2B1 Clarithromycin4 Atorvastatin3 4.45 5.38 ND ND ND Jacobson, 2004 DDI 6
7 OATP1B1, OATP1B3 Clarithromycin4 Bosentan3 3.73 3.82 ND 0.27 NR Markert, 2014 DDI 7
8 OATP1B1, OATP1B3,OATP2B1 Clarithromycin4 Pravastatin1,3 2.11 2.28 ND ND ND Jacobson, 2004 DDI 8
9 OATP1B1, OATP1B3,OATP2B1 Clarithromycin4 Simvastatin3 9.95 7.14 ND ND ND Jacobson, 2004 DDI 9
10 ABCB1/OATPs Cyclosporine2,4 Docetaxel3 7.3 5.7 ND ND ND ND Malingre, 2001 DDI 10
11 OATP1B1/OATP1B3 (CYP3A4) Cyclosporine2,4 Fluvastatin 3.55 4.1 ND 0.31 NS ND Park, 2001 DDI 11
12 ABCB1/ABCG2/OATP1B1/OATP1B3 Cyclosporine2,4 Glecaprevir 5.08 4.51 ND ND ND ND Yu, 2019 DDI 12
13 ABCB1/OATPs Cyclosporine2,4 Paclitaxel3 8.5 2.0 ND ND ND ND Meerum, 1999 DDI 13
14 ABCG2/OATPs Cyclosporine2,4 Pitavastatin1,3 4.6 6.6 ND ND ND ND Livalo Drug Label DDI 14
15 OATP1B1, OATP1B3,OATP2B1 Cyclosporine2,4 Pitavastatin1,3 4.60 ND ND ND ND Gessner, 2019 DDI 15
16 ABCG2/OATPs Cyclosporine2,4 Rosuvastatin1,3 5.0 10.6 ND ND ND ND Simonson, 2004 DDI 16
17 ABCG2/OATPs Cyclosporine2,4 Rosuvastatin1,3 6.4 18.2 ND ND ND ND Simonson, 2004 DDI 17
18 ABCB1/ABCG2/OATP1B1/OATP1B3 Cyclosporine2,4 Voxilaprevir 9.73 14.29 ND ND ND ND Yu, 2019 DDI 18
19 ABCG2/OATP1B1/OATP1B3 Darolutamide Rosuvastatin1,3 ~5 ~5 NS ND NS ND Zurth, 2019 DDI 19
20 ABCG2/OATP Elvitegravir + Cobicistat Rosuvastatin1,3 1.38 1.89 ND ND ND Custodio, 2014 DDI 20
21 ABCB1/OATPs Erythromycin4 Simvastatin3 6.2 3.5 ND ND NS ND Kantola, 1998 DDI 21
22 OATP1B1/OATP1B3 (CYP3A) Glecaprevir/pibrentasvir Atorvastatin3 8.28 22 ND ND ND ND Yu, 2019 DDI 22
23 ABCB1/OATPs Indinavir / Ritonavir4 Fexofenadine3 4.8 2.5 ND 0.2 0.7 ND Kharasch, 2009 DDI 23
24 OATPs Lopinavir / Ritonavir4 Rosuvastatin1,3 2.1 4.7 ND 0.5 NS yes Kiser, 2008 DDI 24
25 OATP1B1, OATP1B3,OATP2B1 Rifamin Pitavastatin1,3 5.70 4.36 ND ND 0.75 Prueksaritanont, 2014 DDI 25
26 OATP1B1, OATP1B3,OATP2B1 Rifamin Rosuvastatin1,3 4.37 9.93 ND ND 0.24 Prueksaritanont, 2014 DDI 26
27 OATP1B1/OATP1B3 Rifampicin2 Glecaprevir 8.55 6.52 ND ND ND ND Yu, 2019 DDI 27
28 OATPs Rifampicin2 Glyburide3 2.2 1.8 NS 0.5 ND yes Zheng, 2009 DDI 28
29 OATP1B1/OATP1B3 Rifampicin2 Voxilaprevir 7.96 8.74 ND ND ND ND Yu, 2019 DDI 29
30 ABCB1/OATPs Ritonavir4 Digoxin 1.9 ND 0.6 0.6 2.6 ND Ding, 2004 DDI 30
31 ABCB1/OATPs Ritonavir4 Saquinavir 29.9 22.5 ND ND ND ND la, 2007 DDI 31
32 ABCB1/OATP1B1/OATP1B3 (CYP3A) Simeprevir4 Atorvastatin3 2.12 1.7 ND ND ND ND Simeprevir NDA application DDI 32
33 OATP1B1/OATP1B3 Simeprevir4 Rosuvastatin1,3 2.81 3.17 ND ND ND ND Simeprevir NDA application DDI 33
34 ABCG2/OATP Tipranavir + Ritonavir Rosuvastatin1,3 1.37 2.23 ND ND ND Pham, 2009 DDI 34
35 ABCB1/OATPs Verapamil Simvastatin3 4.6 2.6 ND ND NS ND Kantola, 1998 DDI 35
36 ABCG2/OATP1B1/OATP1B3 Voxilaprevir Rosuvastatin1,3 7.35 17.96 ND ND ND ND Yu, 2019 DDI 36

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


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