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SLCO2B1

Synonyms: DKFZp686E0517, KIAA0880, OATP-B, OATP2B1, OATPB, SLC21A9

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
Brain Nishimura    0.00975
Kidney Nishimura    0.0262
Liver* Nishimura    0.0677
Placenta* Nishimura    0.0557
Small Intestine* Nishimura    0.0277
Kidney Mean across all PMT Samples 6.496
Liver* Mean across all PMT Samples 65.867
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
Atorvastatin 0.2 MDCK II-OATP2B1 Grube, 2006
Bosentan 202 CHO-OATP2B1 Treiber, 2007
Bromsulphthalein 0.7 OATP2B1-expressing oocytes Kullak-Ublick, 2001
Dibromofluorescein 4.7 HEK293-OATP2B1 Zou, 2020
Estrone sulfate 6.3 OATP2B1-expressing oocytes Kullak-Ublick, 2001
Estrone sulfate 8.09 HEK293-OATP2B1 Nozawa, 2004
Estrone sulfate 7.14 HEK293-OATP2B1 Satoh, 2005
Estrone sulfate 20.9 HEK293-OATP2B1 Hirano, 2006
Estrone sulfate 10.2 HEK293-OATP2B1 Noe, 2007
Fexofenadine ND HEK293-OATP2B1 Nozawa, 2004
Fluvastatin 0.75 HEK293-OATP2B1 Noe, 2007
Glyburide 6.26 HEK293-OATP2B1 Satoh, 2005
Methotrexate >300 OATP2B1-expressing oocytes Visentin, 2012
Pemetrexed 300 OATP2B1-expressing oocytes Visentin, 2012
Pemetrexed 348 OATP2B1-expressing HeLa R1-11 Visentin, 2012
Pitavastatin 1.17 HEK293-OATP2B1 Hirano, 2006
Pravastatin 2250 HEK293-OATP2B1 Nozawa, 2004
Rosuvastatin 2.4 HeLa-OATP2B1 Ho, 2006
Rosuvastatin 6.42 HEK293-OATP2B1 Kitamura, 2008
Taurocholate 71.8 HEK293-OATP2B1 Nozawa, 2004
Telmisartan glucuronide 1.09 HEK293-OATP2B1 Ishiguro, 2008

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
Acemetacin 0.1 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Atazanavir 3.6 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Atorvastatin 0.09 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Atorvastatin 0.4 Estrone sulfate MDCK II-OATP2B1 Grube, 2006
Benzbromarone 0.1 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Bicalutamide 16.3 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Bicalutamide 12.9 Estrone sulfate CHO-OATP2B1 Khuri, 2017
Bromsulphthalein 1.7 Estrone sulfate COS1-OATP2B1 Lan, 2009
Bromsulphthalein 2 1.5 Estrone sulfate Caco-2 Annaert, 2010
Bromsulphthalein 6 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Butylparaben 44.3 Dibromofluorescein HEK293-OATP2B1 Zou, 2020
Calcitriol 7.5 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Celecoxib 13.7 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Cerivastatin 66.2 Estrone sulfate MDCK II-OATP2B1 Grube, 2006
Cyclosporine 20 Bromsulphthalein MDCK II-OATP2B1 Letschert, 2006
Cyclosporine 0.07 Rosuvastatin HEK293-OATP2B1 Ho, 2006
Darunavir 26 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
D&C Orange No. 4 2.11 Dibromofluorescein HEK293-OATP2B1 Zou, 2020
Desogestrel 30.3 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Diacerein 19.98 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Didymin 3.8 4',5'-dibromofluorescein HEK293 cells Bajraktari-Sylejmani, 2020
Diethylstilbestrol 1.6 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Diflunisal 12 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Dipyridamole 2 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Doxazosin Mesylate 15 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Drospirenone 11.1 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Efavirenz 9.6 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Erlotinib 0.07 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Estradiol 2.7 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Estrone 2.5 1.9 Estrone sulfate Caco-2 Annaert, 2010
Ethinyl estradiol 1.3 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Ezetimibe 1.8 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
FD&C Red No. 40 2.59 Dibromofluorescein HEK293-OATP2B1 Zou, 2020
Felodipine 3.5 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Flutamide 32.4 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Fluvastatin 0.1 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Gemfibrozil 8 Rosuvastatin HeLa-OATP2B1 Ho, 2006
Glimepiride 1.6 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Glyburide 1.9 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Hesperetin 67.6 Estrone sulfate OATP2B1-expressing oocytes Shirasaka, 2013
Hesperidin 8.3 4',5'-dibromofluorescein HEK293 cells Bajraktari-Sylejmani, 2020
Hesperidin 1.92 Estrone sulfate OATP2B1-expressing oocytes Shirasaka, 2013
Indinavir 3.9 3 Estrone sulfate Caco-2 Annaert, 2010
Indomethacin 16.3 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Irbesartan 1.3 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Itraconazole 24.8 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Kaempferol 21.3 Estrone sulfate OATP2B1-expressing oocytes Shirasaka, 2013
Ketoconazole 5.7 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Latanoprost 6.76 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Levothyroxine 10.4 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Lopinavir 0.72 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Loratadine 13.3 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Lornoxicam 1.8 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Losartan 8 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Lovastatin 9.92 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Meloxicam 1.59 Estrone sulfate CHO-OATP2B1 Khuri, 2017
MK-571 0.2 Bromsulphthalein MDCK II-OATP2B1 Letschert, 2006
Montelukast 1 Bromsulphthalein MDCK II-OATP2B1 Letschert, 2006
Montelukast 0.38 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Naringenin 49.2 Estrone sulfate OATP2B1-expressing oocytes Shirasaka, 2013
Naringin 6.9 4',5'-dibromofluorescein HEK293 cells Bajraktari-Sylejmani, 2020
Naringin 4.63 Estrone sulfate OATP2B1-expressing oocytes Shirasaka, 2013
Narirutin 14.2 4',5'-dibromofluorescein HEK293 cells Bajraktari-Sylejmani, 2020
Nelfinavir 0.9 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Neohesperidin dihydrochalone 20.1 Dibromofluorescein HEK293-OATP2B1 Zou, 2020
Nobiletin 1.6 4',5'-dibromofluorescein HEK293 cells Bajraktari-Sylejmani, 2020
Norethindrone 14.2 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Novobiocin 3.4 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Olmesartan 4.71 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Olsalazine 2.8 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Oxybutynin 27.79 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Paclitaxel 25 Bromsulphthalein MDCK II-OATP2B1 Letschert, 2006
Phloretin 1.31 Estrone sulfate OATP2B1-expressing oocytes Shirasaka, 2013
Phloridzin 23.2 Estrone sulfate OATP2B1-expressing oocytes Shirasaka, 2013
Piroxicam 35.42 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Prasurgel 5.9 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Quercetin 9.47 Estrone sulfate OATP2B1-expressing oocytes Shirasaka, 2013
Quetiapine 19.1 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Raloxifene 7.4 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Raltitrexed 70 Pemetrexed OATP2B1-expressing HeLa R1-11 Visentin, 2012
Repaglinide 5.2 Bromsulphthalein HEK293-OATP2B1 Bachmakov, 2008
Reserpine 3.5 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Rifampicin 90 Bromsulphthalein MDCK II-OATP2B1 Letschert, 2006
Rifampicin 2.1 1.6 Estrone sulfate Caco-2 Annaert, 2010
Rifamycin SV 3 Bromsulphthalein OATP2B1-expressing oocytes Vavricka, 2002
Rifamycin SV 3 2.3 Estrone sulfate Caco-2 Annaert, 2010
Rifamycin SV 2.7 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Ritonavir 6.3 4.8 Estrone sulfate Caco-2 Annaert, 2010
Ritonavir 2.2 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Ronacaleret 12 Rosuvastatin HEK293-OATP2B1 Johnson, 2017
Rosiglitazone 5.2 Bromsulphthalein HEK293-OATP2B1 Bachmakov, 2008
Saquinavir 5.3 4 Estrone sulfate Caco-2 Annaert, 2010
Saquinavir 4.6 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Silibinin dihemisuccinate 1 Bromsulphthalein MDCK II-OATP2B1 Letschert, 2006
Silymarin 2.5 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Simvastatin 9.4 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Simvastatin 84.7 Estrone sulfate MDCK II-OATP2B1 Grube, 2006
Sinensetin 5.4 4',5'-dibromofluorescein HEK293 cells Bajraktari-Sylejmani, 2020
Sucrose monolaurate 47.7 Dibromofluorescein HEK293-OATP2B1 Zou, 2020
Sulfasalazine 2.7 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Tangeretin 1.6 4',5'-dibromofluorescein HEK293 cells Bajraktari-Sylejmani, 2020
Ticagrelor 4.8 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Ticagrelor 2.12 Estrone sulfate CHO-OATP2B1 Khuri, 2017
Tipranavir 0.2 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Tipranavir 0.88 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
Tropesin 0.03 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Vilazodone hydrochloride 47.1 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
Zafirlukast 1.4 Dibromofluorescein HEK293-OATP2B1 Unger, 2020

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 / Ritonavir Rosuvastatin 3.1 7.0 ND ND ND ND Busti, 2008 DDI 1
2 ABCB1/OATPs Cyclosporine Docetaxel 7.3 5.7 ND ND ND ND Malingre, 2001 DDI 2
3 ABCB1/OATPs Cyclosporine Paclitaxel 8.5 2.0 ND ND ND ND Meerum, 1999 DDI 3
4 ABCG2/OATPs Cyclosporine Pitavastatin 4.6 6.6 ND ND ND ND Livalo Drug Label DDI 4
5 ABCG2/OATPs Cyclosporine Rosuvastatin 5.0 10.6 ND ND ND ND Simonson, 2004 DDI 5
6 ABCG2/OATPs Cyclosporine Rosuvastatin 6.4 18.2 ND ND ND ND Simonson, 2004 DDI 6
7 ABCB1/OATPs Erythromycin Simvastatin 6.2 3.5 ND ND NS ND Kantola, 1998 DDI 7
8 ABCB1/OATPs Indinavir / Ritonavir Fexofenadine 4.8 2.5 ND 0.2 0.7 ND Kharasch, 2009 DDI 8
9 OATPs Lopinavir / Ritonavir Rosuvastatin 2.1 4.7 ND 0.5 NS yes Kiser, 2008 DDI 9
10 OATPs Rifampicin Glyburide 2.2 1.8 NS 0.5 ND yes Zheng, 2009 DDI 10
11 ABCB1/OATPs Ritonavir Digoxin 1.9 ND 0.6 0.6 2.6 ND Ding, 2004 DDI 11
12 ABCB1/OATPs Ritonavir Saquinavir 29.9 22.5 ND ND ND ND la, 2007 DDI 12
13 SLCO2B1 Ronacaleret Rosuvastatin 0.52 0.66 ND ND 1 ND Johnson, 2017 DDI 13
14 ABCB1/OATPs Verapamil Simvastatin 4.6 2.6 ND ND NS ND Kantola, 1998 DDI 14

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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