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SLCO1B1

Synonyms: LST-1, LST1, MGC133282, OATP-C, OATP1B1, OATP2, OATPC, SLC21A6

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	`0.0000357`
Kidney	Nishimura	BLQ
Liver*	Nishimura	`0.252`
Placenta	Nishimura	BLQ
Small Intestine	Nishimura	BLQ
Kidney	Mean across all PMT Samples	`0.0809`
Liver*	Mean across all PMT Samples	`19.561`

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	8.2	HEK293-OATP1B1	Cui, 2001
Atorvastatin³	12.4	HEK293-OATP1B1	Kameyama, 2005
Atorvastatin³	18.9	HEK293-OATP1B1	Lau, 2007
Atorvastatin³	0.761	HEK-OATP1B1	Izumi, 2015
Bilirubin	0.00076	OATP1B1-expressing oocytes	Briz, 2003
Bisglucuronosyl bilirubin	0.28	HEK293-OATP1B1	Cui, 2001
Bosentan³	44	CHO-OATP1B1	Treiber, 2007
Bosentan³	4.27	HEK-OATP1B1	Izumi, 2015
Bromsulphthalein	0.14	HEK293-OATP1B1	Cui, 2001
Bromsulphthalein	0.3	OATP1B1-expressing oocytes	Kullak-Ublick, 2001
Cefazolin	20.8	OATP1B1-expressing oocytes	Nakakariya, 2008
Cefditoren	3.45	OATP1B1-expressing oocytes	Nakakariya, 2008
Cefoperazone	4.84	OATP1B1-expressing oocytes	Nakakariya, 2008
Cholate	11.4	HEK293-OATP1B1	Cui, 2001
Cholyl-glycylamido-fluorescein (CGamF)	7.9	CHO-OATP1B1	Annaert, 2010
Cholyltaurine	10	HEK293-OATP1B1	Cui, 2001
Cilostazol	17.7	HEK-OATP1B1	Wang, 2017
Dehydroepiandrosterone sulfate	21.5	HEK293-OATP1B1	Cui, 2001
Docetaxel³	7.6	CHO-OATP1B1	de, 2012
Enalapril	262	HEK-OATP1B1	Liu, 2006
Estradiol-17beta-glucuronide^1,2	8.29	HEK293-OATP1B1	Hirano, 2004
Estradiol-17beta-glucuronide^1,2	2.5	HEK293-OATP1B1	Yamazaki, 2005
Estradiol-17beta-glucuronide^1,2	5.4	CHO-OATP1B1	Gui, 2008
Estradiol-17beta-glucuronide^1,2	5.9	CHO-OATP1B1	Gui, 2009
Estradiol-17beta-glucuronide^1,2	10	HEK-OATP1B1	Gozalpour, 2014
Estrone sulfate^1,2	12.5	HEK293-OATP1B1	Cui, 2001
Estrone sulfate^1,2	0.46	HEK293-OATP1B1	Hirano, 2004
Estrone sulfate^1,2	0.23	CHO-OATP1B1	Noe, 2007
Estrone sulfate^1,2	2.4	CHO-OATP1B1	Gui, 2008
Estrone sulfate^1,2	0.0872	HEK-OATP1B1	Chapy, 2015
Fexofenadine³	61.6	HEK-OATP1B1	Izumi, 2015
Fluo-3	2.3	CHO-OATP1B1	Gui, 2008
Fluvastatin	1.4	CHO-OATP1B1	Noe, 2007
Fluvastatin	3.5	CHO-OATP1B1	Noe, 2007
Fluvastatin	31.1	OATP1B1-expressing oocytes	Deng, 2008
Fluvastatin	4.8	HEK-OATP1B1	Izumi, 2015
Gadoxetic Acid	700	HEK-OATP1B1	Leonhardt, 2010
Glyburide³	1.24	HEK-OATP1B1	Izumi, 2015
Glycoursodeoxycholate	5.17	HEK293-OATP1B1	Maeda, 2006
Irbesartan	0.695	HEK-OATP1B1	Chapy, 2015
Maraviroc	33.9	OATP1B1-expressing oocytes	Siccardi, 2010
Methotrexate	ND	OATP1B1-expressing oocytes	Abe, 2001
Monoglucuronosyl bilirubin	0.1	HEK293-OATP1B1	Cui, 2001
Nafcillin	11.1	OATP1B1-expressing oocytes	Nakakariya, 2008
Nateglinide³	36.4	HEK-OATP1B1	Izumi, 2015
Olmesartan	42.6	OATP1B1-expressing oocytes	Nakagomi-Hagihara, 2006
Olmesartan	12.8	HEK293-OATP1B1	Yamada, 2007
Paclitaxel³	0.6	OATP1B1-expressing oocytes	Svoboda, 2011
Para-Aminosalicylic acid (PAS)	50	HEK-OATP1B1	Parvez, 2017
Phalloidin	39	HEK293 cells	Fehrenbach, 2003
Pitavastatin^1,3	3	HEK293-OATP1B1	Hirano, 2004
Pitavastatin^1,3	3.6	OATP1B1-expressing oocytes	Fujino, 2005
Pitavastatin^1,3	6.7	OATP1B1-expressing oocytes	Deng, 2008
Pitavastatin^1,3	2.48	HEK-OATP1B1	Izumi, 2015
Pitavastatin^1,3	0.429	HEK-OATP1B1	Chapy, 2015
Pravastatin^1,3	85.7	HEK293-OATP1B1	Kameyama, 2005
Pravastatin^1,3	57.5	OATP1B1-expressing oocytes	Deng, 2008
Pravastatin^1,3	27	HEK-OATP1B1	Izumi, 2015
Regorafenib	15.9	HEK-OATP1B1	Ohya, 2015
Repaglinide³	1.36	HEK-OATP1B1	Izumi, 2015
Rifampicin²	13	OATP1B1-expressing oocytes	Vavricka, 2002
Rifampicin²	1.5	HeLa-OATP1B1	Tirona, 2003
Rosuvastatin^1,3	8.5	OATP1B1-expressing oocytes	Simonson, 2004
Rosuvastatin^1,3	4	HeLa-OATP1B1	Ho, 2006
Rosuvastatin^1,3	7.3	HeLa-OATP1B1	Ho, 2006
Rosuvastatin^1,3	0.8	HEK293-OATP1B1	Kitamura, 2008
Rosuvastatin^1,3	9.31	HEK-OATP1B1	Izumi, 2015
Sincalide	1.67	HEK-OATP1B1	Chapy, 2015
Sorafenib	23.5	HEK-OATP1B1	Zimmerman, 2013
Tauroursodeoxycholate	7.47	HEK293-OATP1B1	Maeda, 2006
Torasemide	6.2	HEK-OATP1B1	Werner, 2010
Torasemide	20.9	HEK-OATP1B1	Izumi, 2015
Valsartan	1.39	HEK293-OATP1B1	Yamashiro, 2006
Valsartan	17.8	CHO-OATP1B1	Poirier, 2009
Valsartan	7.48	HEK-OATP1B1	Izumi, 2015

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

In Vitro Inhibitors

Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
17beta-estradiol	3.9		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2008
17beta-estradiol		3.3	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
5beta-Androstane		374	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Allethrin	16.5		Estrone sulfate^1,2	CHO cells	Chedik, 2017
Amlodipine	35.5		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Amlodipine	39.6		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Amoxicillin	36.2		Estrone sulfate^1,2	HEK-OATP1B1	Parvez, 2016
Amprenavir	16.8	9.52	Atorvastatin³	HEK-OATP1B1	Karlgren, 2012
Amprenavir	14.4	12.8	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Antamanide	100		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
Antamanide	1		Demethylphalloin	HEK293 cells	Fehrenbach, 2003
Atazanavir	1.61	0.91	Atorvastatin³	HEK-OATP1B1	Karlgren, 2012
Atazanavir	1.7	1.5	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Atazanavir	1.4	1.3	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Atorvastatin³	0.87		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Chen, 2005
Atorvastatin lactone	2.6		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Chen, 2005
Azithromycin	>250		Bromsulphthalein	HEK-OATP1B1	Seithel, 2007
Beclomethasone	6.7		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Bezafibrate		45.2	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Bisphenol A	18.7		Estrone sulfate^1,2	CHO cells	Bruyere, 2017
Bisphenol F	13.4		Estrone sulfate^1,2	CHO cells	Bruyere, 2017
Bromocriptine	0.7		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Bromsulphthalein	0.7	0.6	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Bromsulphthalein	0.05		Demethylphalloin	HEK293 cells	Fehrenbach, 2003
Bromsulphthalein	0.08		Estradiol-17beta-glucuronide^1,2	HeLa-OATP1B1	Tirona, 2003
Bromsulphthalein	1.7		Estrone sulfate^1,2	COS1-OATP1A2	Lan, 2009
Ceftriaxone	470		Lithocholyl-(Ne-NBD)-lysine	HEK-OATP1B1	Yamaguchi, 2011
Cerivastatin	1.7		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Hinton, 2008
Chenodeoxycholic acid		3.4	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Cholic acid		25	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Clarithromycin⁴	96		Bromsulphthalein	HEK-OATP1B1	Seithel, 2007
Clarithromycin⁴	5.3		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Vermeer, 2016
Clarithromycin⁴	75		Lithocholyl-(Ne-NBD)-lysine	HEK-OATP1B1	Yamaguchi, 2011
Clopidogrel	3.95		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Clopidogrel	>100		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Clotrimazole	9		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2008
Clotrimazole		7.6	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Cyclosporine^2,4	1.88	0.82	Atorvastatin³	HEK-OATP1B1	Karlgren, 2012
Cyclosporine^2,4	0.3		Bosentan³	CHO-OATP1B1	Treiber, 2007
Cyclosporine^2,4	3.5		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
Cyclosporine^2,4		0.238	Cerivastatin	MDCK II-OAT1B1	Shitara, 2003
Cyclosporine^2,4		2.32	Cilostazol	HEK-OATP1B1	Wang, 2017
Cyclosporine^2,4	0.5	0.051	Demethylphalloin	HEK293 cells	Fehrenbach, 2003
Cyclosporine^2,4		0.116	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Cyclosporine^2,4	0.37		Estradiol-17beta-glucuronide^1,2	HeLa-OATP1B1	Tirona, 2003
Cyclosporine^2,4	0.05		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Hinton, 2008
Cyclosporine^2,4	1.4	1.3	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Cyclosporine^2,4		0.24	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Cyclosporine^2,4	2.2		Rosuvastatin^1,3	OATP1B1-expressing oocytes	Simonson, 2004
Cyclosporine^2,4	0.31		Rosuvastatin^1,3	HeLa-OATP1B1	Ho, 2006
Dabrafenib	1.4		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Ellens, 2017
Darolutamide	3.8		Pravastatin^1,3	HEK-OATP1B1	Zurth, 2019
Darunavir	3.5	3.1	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Dasatinib	2.33		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Pahwa, 2017
Dehydrocholic acid		29.7	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Deoxycholic acid		3.2	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Digitoxin	14.2		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Gozalpour, 2014
Digoxin	7.9	7	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Digoxin	63		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Gozalpour, 2014
Doxorubicin	160	150	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Eltrombopag	0.09		Rosuvastatin^1,3	HEK-OATP1B1	Takeuchi, 2014
Erlotinib	21	21	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Erythromycin⁴	217		Bromsulphthalein	HEK-OATP1B1	Seithel, 2007
Erythromycin⁴		5.27	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Estrone sulfate^1,2		0.0449	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Estrone sulfate^1,2	0.79		Estradiol-17beta-glucuronide^1,2	HEK293-OATP1B1	Ishiguro, 2006
Estrone sulfate^1,2		0.2	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Estrone sulfate^1,2	0.06		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Ethambutol	57.6		Estrone sulfate^1,2	HEK-OATP1B1	Parvez, 2016
Etomidate	>100		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Everolimus	0.23		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Farasyn, 2019
Everolimus	0.16		Estrone sulfate^1,2	HEK-OATP1B1	Farasyn, 2019
Everolimus	0.19		Rosuvastatin^1,3	HEK-OATP1B1	Farasyn, 2019
Fenofibrate		105.2	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Fexofenadine³		257	Estrone sulfate^1,2	HEK293-OATP1B1	Shimizu, 2005
Fusidic Acid	3.9		Rosuvastatin^1,3	HEK-OATP1B1	Gupta, 2016
Gadoxetic Acid	600		Bromsulphthalein	HEK-OATP1B1	Leonhardt, 2010
Gemfibrozil⁴	156.2	68.05	Atorvastatin³	HEK-OATP1B1	Karlgren, 2012
Gemfibrozil⁴		18.1	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Gemfibrozil⁴		12.5	Estradiol-17beta-glucuronide^1,2	HEK293-OATP1B1	Yamazaki, 2005
Gemfibrozil⁴	7.4		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Hinton, 2008
Gemfibrozil⁴	25		Rosuvastatin^1,3	HeLa-OATP1B1	Ho, 2006
Glimepiride	3.55		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	van, 2013
Glimepiride	3.62		Rosuvastatin^1,3	HEK-OATP1B1	van, 2013
Glipizide	45.3		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	van, 2013
Glipizide	110		Rosuvastatin^1,3	HEK-OATP1B1	van, 2013
Glyburide³	0.26		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Glyburide³	2.99		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	van, 2013
Glyburide³	1.4		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Glyburide³		0.75	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Glyburide³	1.77		Rosuvastatin^1,3	HEK-OATP1B1	van, 2013
Glycocholic acid		22	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
GW1929		0.3	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
GW4064		32.4	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Hyperforin	0.82		Estradiol-17beta-glucuronide^1,2	HeLa-OATP1B1	Tirona, 2003
Indinavir	12.2	10.8	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Indinavir	5.84		Estradiol-17beta-glucuronide^1,2	HeLa-OATP1B1	Tirona, 2003
Indomethacin	12	11	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Irbesartan	4.65		Estrone sulfate^1,2	HEK-OATP1B1	Pei, 2018
Ketoconazole		11.5	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Ketoconazole	1.8		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Vermeer, 2016
Lesinurad	9.3		Bromsulphthalein	MDCK II-OAT1B1	Shen, 2016
Levothyroxine	0.88		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Levothyroxine	2.04		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Linezolid	65.9		Estrone sulfate^1,2	HEK-OATP1B1	Parvez, 2016
Lithocholate	0.7		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2008
Lithocholate		1.2	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Lopinavir	0.74	0.32	Atorvastatin³	HEK-OATP1B1	Karlgren, 2012
Lopinavir	0.5	0.5	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Lovastatin	4		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Chen, 2005
Lovastatin Lactone	28		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Chen, 2005
Metronidazole	>100		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Mevinolin	6.1		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2008
Mevinolin		12.7	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Mifepristone	3.3		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2008
Mifepristone		2.2	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
MK-571	5		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
MK-571	0.3		Estradiol-17beta-glucuronide^1,2	HEK293-OATP1B1	Yamazaki, 2005
Montelukast	10		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
Montelukast	2.04		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Montelukast	1.4		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Moricizine	8.1		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Nelfinavir	0.93		Estradiol-17beta-glucuronide^1,2	HeLa-OATP1B1	Tirona, 2003
Nilotinib	2.78		Estrone sulfate^1,2	CHO-OATP1B1	Khurana, 2014
Nisoldipine		7.4	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Yoshida, 2012
Nobiletin	2.1		8-fluorescein-cAMP	HEK293 cells	Bajraktari-Sylejmani, 2020
Octreotide	24.1		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Visentin, 2015
Olaparib	20.3		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	McCormick, 2017
Olaparib	27.1		Pravastatin^1,3	HEK-OATP1B1	McCormick, 2017
Paclitaxel³	50		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
Paclitaxel³	0.03		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2008
Para-Aminosalicylic acid (PAS)	72.6		Estrone sulfate^1,2	HEK-OATP1B1	Parvez, 2016
Pazopanib	3.89		Estrone sulfate^1,2	CHO-OATP1B1	Khurana, 2014
Pioglitazone	39.6		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Pioglitazone	5.09		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	van, 2013
Pioglitazone	6.8		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Pioglitazone	32.2		Rosuvastatin^1,3	HEK-OATP1B1	van, 2013
Pravastatin^1,3	>100		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Chen, 2005
Pravastatin^1,3		21.8	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Pravastatin^1,3	3.6	3.4	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Probenecid		39.8	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Progesterone	5.4		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Ramipril	4		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Repaglinide³	2.2		Bromsulphthalein	HEK293-OATP1B1	Bachmakov, 2008
Repaglinide³	0.32		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Hinton, 2008
Repaglinide³	1.1		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Rifabutin	35.4		Estrone sulfate^1,2	HEK-OATP1B1	Parvez, 2016
Rifampicin²	2.4		8-fluorescein-cAMP	HEK293 cells	Bajraktari-Sylejmani, 2020
Rifampicin²	3.25	3.08	Atorvastatin³	HEK293-OATP1B1	Lau, 2007
Rifampicin²	3.2		Bosentan³	CHO-OATP1B1	Treiber, 2007
Rifampicin²		17	Bromsulphthalein	OATP1B1-expressing oocytes	Vavricka, 2002
Rifampicin²	120		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
Rifampicin²	11.9		Bromsulphthalein	HEK-OATP1B1	Leonhardt, 2010
Rifampicin²	5.65		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Rifampicin²	1.8	1.6	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Rifampicin²		6.75	Cilostazol	HEK-OATP1B1	Wang, 2017
Rifampicin²		0.355	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Rifampicin²	0.94		Estradiol-17beta-glucuronide^1,2	HeLa-OATP1B1	Tirona, 2003
Rifampicin²	0.94		Estradiol-17beta-glucuronide^1,2	HeLa cells	Tirona, 2003
Rifampicin²	1.5		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2008
Rifampicin²	1.2	1.1	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Rifampicin²	0.24		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Pahwa, 2017
Rifampicin²	0.88		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Rifampicin²	10.46		Estrone sulfate^1,2	CHO-OATP1B1	Khurana, 2014
Rifampicin²	1.9		Estrone sulfate^1,2	HEK-OATP1B1	Parvez, 2016
Rifampicin²	1.3		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
Rifampicin²	8.8		Lithocholyl-(Ne-NBD)-lysine	HEK-OATP1B1	Yamaguchi, 2011
Rifampicin²		0.48	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Rifamycin SV²		2	Bromsulphthalein	OATP1B1-expressing oocytes	Vavricka, 2002
Rifamycin SV²	0.23		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Chen, 2005
Rifamycin SV²		0.17	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Rifapentine	26.7		Estrone sulfate^1,2	HEK-OATP1B1	Parvez, 2016
Rilpivirine	4.1		8-fluorescein-cAMP	HEK-OATP1B1	Weiss, 2013
Ritonavir⁴	1.6	1.4	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Ritonavir⁴		0.32	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Ritonavir⁴	0.71		Estradiol-17beta-glucuronide^1,2	HeLa-OATP1B1	Tirona, 2003
Ritonavir⁴	1.3	1.3	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Ritonavir⁴	0.68		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Vermeer, 2016
Ritonavir⁴		0.78	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Rosiglitazone	6		Bromsulphthalein	HEK293-OATP1B1	Bachmakov, 2008
Rosiglitazone	43.4		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Rosiglitazone	4.27		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Roxithromycin	153		Bromsulphthalein	HEK-OATP1B1	Seithel, 2007
Sacubitril	1.91		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Ayalasomayajula, 2016
Saquinavir	2.1	1.8	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
Saquinavir	1.23		Estradiol-17beta-glucuronide^1,2	HeLa-OATP1B1	Tirona, 2003
Saquinavir		1.59	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Sildenafil	1.5		Bosentan³	CHO-OATP1B1	Treiber, 2007
Silibinin dihemisuccinate	10		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
Simeprevir⁴	0.72		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Huisman AASLD Poster 2010
Simvastatin³	3.6		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Chen, 2005
Simvastatin lactone	9.7		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Chen, 2005
Sinensetin	8		8-fluorescein-cAMP	HEK293 cells	Bajraktari-Sylejmani, 2020
Sirolimus	6.49		Bromsulphthalein	HEK-OATP1B1	Oswald, 2010
Sirolimus	1.1		Demethylphalloin	HEK293 cells	Fehrenbach, 2003
Sirolimus	0.22		Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Farasyn, 2019
Sirolimus	0.65		Estrone sulfate^1,2	HEK-OATP1B1	Farasyn, 2019
Sirolimus	0.32		Rosuvastatin^1,3	HEK-OATP1B1	Farasyn, 2019
Sorafenib	0.0696		Docetaxel³	T-Rex293-OATP1B1	Hu, 2014
Sulfasalazine	0.56	0.53	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
Sulfinpyrazone		32	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Yoshida, 2012
Tacrolimus	3.7		Demethylphalloin	HEK293 cells	Fehrenbach, 2003
Tacrolimus		0.533	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Tacrolimus		0.61	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Tangeretin	4.8		8-fluorescein-cAMP	HEK293 cells	Bajraktari-Sylejmani, 2020
Taurocholate		11.4	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Telithromycin	121		Bromsulphthalein	HEK-OATP1B1	Seithel, 2007
Telmisartan¹		4.88	Cilostazol	HEK-OATP1B1	Wang, 2017
Telmisartan¹		0.44	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Tetrabromobisphenol A	0.6		Estrone sulfate^1,2	CHO cells	Bruyere, 2017
Tetramethrin	5.7		Estrone sulfate^1,2	CHO cells	Chedik, 2017
Thyroxine		3.5	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Tipranavir		1.1	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Yoshida, 2012
Tolbutamide	368		Rosuvastatin^1,3	HEK-OATP1B1	van, 2013
Trimethoprim		>100	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Yoshida, 2012
Troglitazone	1.2		Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2008
Troglitazone		1	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009
Ursodeoxycholic acid		10	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Yoshida, 2012
Valsartan	14.98		Estrone sulfate^1,2	HEK-OATP1B1	Pei, 2018
Valsartan		8.96	Pitavastatin^1,3	HEK293-OATP1B1	Hirano, 2006
Venetoclax	47.8		8-fluorescein-cAMP	HEK-OATP1B1	Weiss, 2016
Verapamil	>100		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
Verapamil		15.3	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
Verapamil	75.7		Estrone sulfate^1,2	HEK-OATP1B1	Tamraz, 2013
Vincristine	44	42	Estradiol-17beta-glucuronide^1,2	HEK-OATP1B1	Karlgren, 2012
WY-14643		1.6	Estradiol-17beta-glucuronide^1,2	CHO-OATP1B1	Gui, 2009

Clinical Drug-Drug Interactions

DDI	Implicated Transporter	Interacting Drug	Affected Drug	AUC	Cmax	CLR	CL/F	t1/2	Effect on PD	Reference	More Details
DDI	Implicated Transporter	Interacting Drug	Affected Drug	Clinical PK Impact(fold change)					Effect on PD	Reference	More Details
1	ABCG2/OATPs	Atazanavir / Ritonavir⁴	Rosuvastatin^1,3	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	Rosuvastatin^1,3	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	Pravastatin^1,3	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/OATP1B1 (CYP3A4)	Cyclosporine^2,4	Atorvastatin³	15.3	13.7	ND	ND	ND	NS	Lemahieu, 2005	DDI 10
11	ABCB1/OATPs	Cyclosporine^2,4	Docetaxel³	7.3	5.7	ND	ND	ND	ND	Malingre, 2001	DDI 11
12	OATP1B1/OATP1B3 (CYP3A4)	Cyclosporine^2,4	Fluvastatin	3.55	4.1	ND	0.31	NS	ND	Park, 2001	DDI 12
13	ABCB1/ABCG2/OATP1B1/OATP1B3	Cyclosporine^2,4	Glecaprevir	5.08	4.51	ND	ND	ND	ND	Yu, 2019	DDI 13
14	ABCB1/OATPs	Cyclosporine^2,4	Paclitaxel³	8.5	2.0	ND	ND	ND	ND	Meerum, 1999	DDI 14
15	ABCG2/OATPs	Cyclosporine^2,4	Pitavastatin^1,3	4.6	6.6	ND	ND	ND	ND	Livalo Drug Label	DDI 15
16	OATP1B1, OATP1B3,OATP2B1	Cyclosporine^2,4	Pitavastatin^1,3	4.60	ND	ND	ND	ND		Gessner, 2019	DDI 16
17	ABCC2/OATP1B1	Cyclosporine^2,4	Pravastatin^1,3	9.93	7.78	ND	ND	0.75	ND	Hedman, 2004	DDI 17
18	OATP1B1 (CYP3A4)	Cyclosporine^2,4	Repaglinide³	2.44	1.72	NS	ND	NS	NS	Kajosaari, 2005	DDI 18
19	ABCG2/OATPs	Cyclosporine^2,4	Rosuvastatin^1,3	5.0	10.6	ND	ND	ND	ND	Simonson, 2004	DDI 19
20	ABCG2/OATPs	Cyclosporine^2,4	Rosuvastatin^1,3	6.4	18.2	ND	ND	ND	ND	Simonson, 2004	DDI 20
21	ABCB1/ABCG2/OATP1B1/OATP1B3	Cyclosporine^2,4	Voxilaprevir	9.73	14.29	ND	ND	ND	ND	Yu, 2019	DDI 21
22	ABCG2/OATP1B1/OATP1B3	Darolutamide	Rosuvastatin^1,3	~5	~5	NS	ND	NS	ND	Zurth, 2019	DDI 22
23	ABCG2/OATP1B1	Eltrombopag	Rosuvastatin^1,3	1.55	2.03	ND	ND	ND	ND	Allred, 2011	DDI 23
24	ABCG2/OATP	Elvitegravir + Cobicistat	Rosuvastatin^1,3	1.38	1.89	ND	ND	ND		Custodio, 2014	DDI 24
25	ABCB1/OATPs	Erythromycin⁴	Simvastatin³	6.2	3.5	ND	ND	NS	ND	Kantola, 1998	DDI 25
26	ABCG2/OATP1B1	Fostamatinib	Rosuvastatin^1,3	1.96	1.88	ND	ND	ND		Martin, 2016	DDI 26
27	OATP1B1	Gemfibrozil⁴	Atorvastatin³	1.24	1.17	ND	ND	0.84	ND	Backman, 2005	DDI 27
28	OATP1B1	Gemfibrozil⁴	Atorvastatin³	1.35	NS	ND	ND	0.74	ND	Whitfield, 2011	DDI 28
29	OATP1B1	Gemfibrozil⁴	Lovastatin	2.79	2.81	ND	ND	ND	ND	Kyrklund, 2001	DDI 29
30	OATP1B1	Gemfibrozil⁴	Pravastatin^1,3	2.02	NS	0.57	ND	NS	ND	Kyrklund, 2003	DDI 30
31	OATP1B1 (CYP2C8)	Gemfibrozil⁴	Repaglinide³	8.22	2.6	ND	ND	2.27	Yes	Kalliokoski, 2008	DDI 31
32	OATP1B1	Gemfibrozil⁴	Rosuvastatin^1,3	1.88	2.21	ND	ND	NS	ND	Schneck, 2004	DDI 32
33	OATP1B1	Gemfibrozil⁴	Simvastatin³	2.91	2.12	ND	ND	1.51	ND	Backman, 2000	DDI 33
34	OATP1B1/OATP1B3 (CYP3A)	Glecaprevir/pibrentasvir	Atorvastatin³	8.28	22	ND	ND	ND	ND	Yu, 2019	DDI 34
35	ABCB1/OATPs	Indinavir / Ritonavir⁴	Fexofenadine³	4.8	2.5	ND	0.2	0.7	ND	Kharasch, 2009	DDI 35
36	OATP1B1	Irbesartan	Repaglinide³	1.33	1.84	ND	ND	NS	Yes	Pei, 2018	DDI 36
37	OATPs	Lopinavir / Ritonavir⁴	Rosuvastatin^1,3	2.1	4.7	ND	0.5	NS	yes	Kiser, 2008	DDI 37
38	OATP1B1, OATP1B3,OATP2B1	Rifamin	Pitavastatin^1,3	5.70	4.36	ND	ND	0.75		Prueksaritanont, 2014	DDI 38
39	OATP1B1, OATP1B3,OATP2B1	Rifamin	Rosuvastatin^1,3	4.37	9.93	ND	ND	0.24		Prueksaritanont, 2014	DDI 39
40	OATP1B1	Rifampicin²	Atorvastatin³	7.25	10.5	ND	0.13	0.37	ND	Lau, 2007	DDI 40
41	OATP1B1/OATP1B3	Rifampicin²	Glecaprevir	8.55	6.52	ND	ND	ND	ND	Yu, 2019	DDI 41
42	OATPs	Rifampicin²	Glyburide³	2.2	1.8	NS	0.5	ND	yes	Zheng, 2009	DDI 42
43	OATP1B1	Rifampicin²	Pitavastatin^1,3	5.28	7.65	ND	0.15	0.51	ND	Chen, 2013	DDI 43
44	OATP1B1	Rifampicin²	Pitavastatin^1,3	5.41	4.77	ND	ND	NS	ND	Prueksaritanont, 2014	DDI 44
45	OATP1B1	Rifampicin²	Pravastatin^1,3	2.27	2.73	ND	0.5	NS	ND	Deng, 2009	DDI 45
46	ABCG2/OATP1B1	Rifampicin²	Rosuvastatin^1,3	4.09	9.39	ND	ND	NS	ND	Prueksaritanont, 2014	DDI 46
47	OATP1B1/OATP1B3	Rifampicin²	Voxilaprevir	7.96	8.74	ND	ND	ND	ND	Yu, 2019	DDI 47
48	ABCB1/OATPs	Ritonavir⁴	Digoxin	1.9	ND	0.6	0.6	2.6	ND	Ding, 2004	DDI 48
49	ABCB1/OATPs	Ritonavir⁴	Saquinavir	29.9	22.5	ND	ND	ND	ND	la, 2007	DDI 49
50	ABCB1/OATP1B1/OATP1B3 (CYP3A)	Simeprevir⁴	Atorvastatin³	2.12	1.7	ND	ND	ND	ND	Simeprevir NDA application	DDI 50
51	OATP1B1/OATP1B3	Simeprevir⁴	Rosuvastatin^1,3	2.81	3.17	ND	ND	ND	ND	Simeprevir NDA application	DDI 51
52	ABCG2/OATP	Tipranavir + Ritonavir	Rosuvastatin^1,3	1.37	2.23	ND	ND	ND		Pham, 2009	DDI 52
53	ABCB1/OATPs	Verapamil	Simvastatin³	4.6	2.6	ND	ND	NS	ND	Kantola, 1998	DDI 53
54	ABCG2/OATP1B1/OATP1B3	Voxilaprevir	Rosuvastatin^1,3	7.35	17.96	ND	ND	ND	ND	Yu, 2019	DDI 54

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