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SLC22A8

Synonyms: MGC24086, OAT3

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Orthologs in other species

rat Slc22a8

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	`0.000504`
Kidney*	Nishimura	`0.818`
Liver	Nishimura	`0.000135`
Placenta	Nishimura	BLQ
Small Intestine	Nishimura	BLQ
Kidney*	Mean across all PMT Samples	`17.974`
Liver	Mean across all PMT Samples	BLQ

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
Amoxicillin	161.4	HEK293-OAT3	Parvez, 2018
Baricitinib	5.54	HEK-PEAK-OAT3	Posada, 2017
Beraprost sodium	ND	S2-OAT3	Oshida, 2017
Bumetanide	1586	S2-OAT3	Hasannejad, 2004
Cefaclor³	ND	HEK293-OAT3	Ueo, 2005
Ceftizoxime³	ND	HEK293-OAT3	Ueo, 2005
Cilostazol	23.6	HEK293-OAT3	Wang, 2014
Cimetidine	57.4	OAT3-expressing oocytes	Cha, 2001
Cimetidine	113	HEK293-OAT3	Tahara, 2006
Cimetidine	174	CHO-OAT3	Chu, 2007
Cortisol	2.4	OAT3-expressing oocytes	Asif, 2005
Dimesna	390	HeLa-OAT3	Cutler, 2012
Edaravone sulfate	15.1	HEK293-OAT3	Mizuno, 2007
Estrone sulfate¹	7.5	S2-OAT3	Takeda, 2000
Estrone sulfate¹	3.1	OAT3-expressing oocytes	Cha, 2001
Estrone sulfate¹	2.21	S2-OAT3	Takeda, 2001
Estrone sulfate¹	6.3	HEK293-OAT3	Ueo, 2005
Estrone sulfate¹	6.3	HEK293 cells	Ueo, 2005
Estrone sulfate¹	2.18	COS7-OAT3	Duan, 2009
Estrone sulfate¹	21.2	HEK293 cells	Bruyere, 2017
Fexofenadine	70.2	HEK293-OAT3	Tahara, 2006
Furosemide³	ND	S2-OAT3	Hasannejad, 2004
Hydrochlorothiazide	134	HEK293-OAT3	Yin, 2019
Methotrexate^1,3	10.9	OAT3-expressing oocytes	Cha, 2001
Methotrexate^1,3	21.1	S2-OAT3	Takeda, 2002
Methotrexate^1,3	17.2	OAT3-expressing oocytes	Uwai, 2004
Methotrexate^1,3	76.6	HEK293-OAT3	Kurata, 2014
Ochratoxin A	0.75	S2-OAT3	Jung, 2001
Olmesartan	0.12	HEK293-OAT3	Yamada, 2007
Oseltamivir acid	ND	HEK293-OAT3	Mathialagan, 2017
Para-aminohippurate⁴	87.2	OAT3-expressing oocytes	Cha, 2001
Para-Aminosalicylic acid (PAS)	100	HEK293-OAT3	Parvez, 2017
Pemetrexed	28.2	HEK293-OAT3	Kurata, 2014
Perfluorooctanoic acid	49.1	HEK293 cells	Nakagawa, 2008
Piperacillin	172	HEK293-OAT3	Wen, 2018
Pitavastatin	3.3	OAT3-expressing oocytes	Fujino, 2005
Pravastatin¹	27.2	S2-OAT3	Nakagomi-Hagihara, 2007
Prostaglandin E2	0.345	S2-OAT3	Kimura, 2002
Prostaglandin F2-alpha	1.092	S2-OAT3	Kimura, 2002
Relebactam	ND	MDCKII-OAT3	Chan, 2019
Rosuvastatin	7.4	OAT3-expressing oocytes	Windass, 2007
Sitagliptin	162	CHO-OAT3	Chu, 2007
Tazobactam	377	HEK293-OAT3	Wen, 2018
Tetracycline	566.2	S2-OAT3	Babu, 2002
Uric acid	380.3	HEK293-OAT3	Sato, 2008
Valsartan	3.58	HEK293-OAT3	Hanna, 2018
Zidovudine	145	S2-OAT3	Takeda, 2002

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
(-)-Zearalenone	6.71		Estrone sulfate¹	S2 cells	Tachampa, 2008
(Noradamantan-3-yl)-1,3-dipropylxanthine (KW-3902)		3.7	Estrone sulfate¹	S2-OAT3	Takeda, 2001
(S)-7-hydroxy warfarin	1.93		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
(S)-ketoprofen b-D-glucuronide	8.07		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
(S)-naproxen acyl-b-D-glucuronide	5.43		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
(S)eO-desmethyl naproxen	3.44		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
1-butanesulfonic acid (BSA)	5098		Estrone sulfate¹	CHO-OAT3	Astorga, 2011
2,3-Dimercapto-1-propane sulfonate (DMPS)	40		Estrone sulfate¹	CHO-OAT3	Astorga, 2011
3-cis-hydroxycyclohexyl glyburide	0.81		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
3-mercapto-1-propansulfonic acid (MPS)	2139		Estrone sulfate¹	CHO-OAT3	Astorga, 2011
4-hydroxy-trazodone	16.9		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
4-Hydroxy diclofenac	2.03		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
4-Hydroxy flurbiprofen	1.39		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
5-Carboxy-meloxicam	0.7		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
5-Hydroxy Rosiglitazone b-D-Glucuronide	>200		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
5-OH-rosiglitazone sulfate	1.31		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
6-Hydroxy chlorzoxazone	3.21		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Abiraterone	>20		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Abiraterone N-oxide sulfate	1.36		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Abiraterone sulfate	1.83		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Acetazolamide	816		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Adipate	136		Estrone sulfate¹	HEK293-OAT3	Kaufhold, 2011
Aflatoxin B1	13.1		Estrone sulfate¹	S2 cells	Tachampa, 2008
Allethrin	69.4		Fluorescein	HEK293 cells	Chedik, 2017
Alpha-ketoglutarate	92.8		Estrone sulfate¹	HEK293-OAT3	Kaufhold, 2011
Alpha-zearalenol	4.55		Estrone sulfate¹	S2 cells	Tachampa, 2008
Apixaban	289		Estrone sulfate¹	HEK293-OAT3	Tsuruya, 2017
Aristolochic acid I	-	0.5	Estrone sulfate¹	HEK293 cells	Bakhiya, 2009
Aspirin	17	15	Cilostazol	HEK293-OAT3	Wang, 2014
Baricitinib		12.7	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Bendamustin	0.8		Estrone sulfate¹	HEK293-OAT3	Hagos, 2015
Benzbromarone	0.967		Urate	HEK293-OAT3	Taniguchi, 2019
Benzylpenicillin^1,2	137	126	Cilostazol	HEK293-OAT3	Wang, 2014
Betamipron		48.3	Estrone sulfate¹	S2-OAT3	Takeda, 2001
Bisphenol A	9.2		Estrone sulfate¹	HEK293 cells	Bruyere, 2017
Bisphenol F	26.8		Estrone sulfate¹	HEK293 cells	Bruyere, 2017
Bisphenol S	23.3		Estrone sulfate¹	HEK293 cells	Bruyere, 2017
Bumetanide	0.75		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Bumetanide	7.8		Estrone sulfate¹	OAT3-expressing oocytes	Elsby, 2011
Bumetanide	5.4		Methotrexate^1,3	OAT3-expressing oocytes	Elsby, 2011
Cabotegravir	0.41		Estrone sulfate¹	S2-OAT3	Reese, 2016
Candesartan	0.3		Uric acid	HEK293-OAT3	Sato, 2008
Cefaclor³	120.2		Estrone sulfate¹	HEK293 cells	Ueo, 2005
Cefadroxil		8620	Prostaglandin F2-alpha	S2-OAT3	Khamdang, 2003
Cefamandole		50	Prostaglandin F2-alpha	S2-OAT3	Khamdang, 2003
Cefazolin	650		Pemetrexed	HEK-OAT3	Kurata, 2014
Cefazolin		550	Prostaglandin F2-alpha	S2-OAT3	Khamdang, 2003
Cefazolin	99		Relebactam	MDCKII-OAT3	Chan, 2019
Cefdinir	271.5		Estrone sulfate¹	HEK293 cells	Ueo, 2005
Cefoperazone		1890	Prostaglandin F2-alpha	S2-OAT3	Khamdang, 2003
Cefoselis	2925.1		Estrone sulfate¹	HEK293 cells	Ueo, 2005
Cefotaxime		290	Prostaglandin F2-alpha	S2-OAT3	Khamdang, 2003
Cefotiam	212.6		Estrone sulfate¹	HEK293 cells	Ueo, 2005
Ceftibuten	247.3		Estrone sulfate¹	HEK293 cells	Ueo, 2005
Ceftizoxime³	956.7		Estrone sulfate¹	HEK293 cells	Ueo, 2005
Ceftriaxone		4390	Prostaglandin F2-alpha	S2-OAT3	Khamdang, 2003
Celecoxib	>200		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Celecoxib carboxylic acid	8.43		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Cephaloridine	626.4		Estrone sulfate¹	HEK293 cells	Ueo, 2005
Cephaloridine		2460	Prostaglandin F2-alpha	S2-OAT3	Khamdang, 2003
Cephalothin		40	Prostaglandin F2-alpha	S2-OAT3	Khamdang, 2003
Chlorambucil	9.5		Estrone sulfate¹	HEK293-OAT3	Hagos, 2015
Chlorothiazide	65.3		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Chlorzoxazone	10.2		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Cilastatin		231	Estrone sulfate¹	S2-OAT3	Takeda, 2001
Cimetidine	79		Sitagliptin	CHO-OAT3	Chu, 2007
Citreoviridin A	6.63		Estrone sulfate¹	S2 cells	Tachampa, 2008
Citrinin		15.4	Ochratoxin A	S2-OAT2	Jung, 2001
Cyclopiazonic acid	1.9		Estrone sulfate¹	S2 cells	Tachampa, 2008
Cyclothiazide	27.9		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Dabrafenib	3.4		6-CF	S2-OAT3	Ellens, 2017
Dantrolene	0.3		Estrone sulfate¹	HEK293-OAT3	Burckhardt, 2017
Darolutamide	4.5		Furosemide³	HEK293-OAT3	Zurth, 2019
Darunavir		37.9	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Diclofenac	0.62		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Diclofenac	3.7		Baricitinib	HEK-PEAK-OAT3	Posada, 2017
Diclofenac	7.78		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Diclofenac	2		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
Diflunisal	0.72		6-CF	COS-7-OAT3	Duan, 2012
Dotinurad	1.32		Urate	HEK293-OAT3	Taniguchi, 2019
Epacadostat	21		Estrone sulfate¹	HEK293-Flp-In-OAT3	Zhang, 2017
Eprosartan	3.8		Bestatin	HEK293-OAT3	Huo, 2014
Esomeprazole	1.2		Methotrexate^1,3	HEK293-OAT3	Narumi, 2017
Estrone sulfate¹	1		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Ethacrynic acid	0.662		6-CF	COS-7-OAT3	Duan, 2012
Ethacrynic acid	0.58		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Favipiravir		84.2	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Fenofibric acid	2.2		Sitagliptin	CHO-OAT3	Chu, 2007
Flurbiprofen	1.8		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Fluvastatin	5.79		Estrone sulfate¹	S2-OAT3	Takeda, 2004
Fumonisin B1	181		Estrone sulfate¹	S2 cells	Tachampa, 2008
Furosemide³	7.31		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Furosemide³	1.7		Sitagliptin	CHO-OAT3	Chu, 2007
Gemfibrozil	6.8		Pravastatin¹	S2-OAT3	Nakagomi-Hagihara, 2007
Glafenine	5.31		Estrone sulfate¹	HEK293-OAT3	Burckhardt, 2017
Gliotoxin	73.9		Estrone sulfate¹	S2 cells	Tachampa, 2008
Glutarate	78.5		Estrone sulfate¹	HEK293-OAT3	Kaufhold, 2011
Glyburide	0.21		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Hydrochlorothiazide	942		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Hydrochlorothiazide	213		Estrone sulfate¹	HEK293-OAT3	Yin, 2019
Hydroxy pioglitazone	1.37		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Ibuprofen	4.46		Baricitinib	HEK-PEAK-OAT3	Posada, 2017
Ibuprofen	6		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Ibuprofen	6.1		Isoniazid	HEK293-OAT3	Parvez, 2018
Ibuprofen	1.98		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
Ibuprofen	27.9		Pemetrexed	HEK-OAT3	Kurata, 2014
Ibuprofen	3.7		Sitagliptin	CHO-OAT3	Chu, 2007
Imatinib	14.5		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Imatinib (piperidine)-4-oxide	64.2		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Indapamide	11		Sitagliptin	CHO-OAT3	Chu, 2007
Indomethacin	0.11		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Indomethacin	0.61		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Indomethacin	2.18		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
Irbesartan	0.41		Bestatin	HEK293-OAT3	Huo, 2014
JBP485	185	160	Bestatin	HEK293-OAT3	Zhu, 2012
Keto pioglitazone	0.73		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Ketoconazole	0.86		Estrone sulfate¹	HEK293-OAT3	Vermeer, 2016
Ketoconazole	64		Estrone sulfate¹	HEK293-OAT3	Tsuruya, 2017
Ketoconazole	15.77		Rivaroxaban	HEK293-OAT3	Cheong, 2019
Ketoprofen	1.61		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Ketoprofen	5.98		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Lansoprazole	0.4		Methotrexate^1,3	HEK293-OAT3	Narumi, 2017
Lansoprazole	2.18		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
Leflunomide	4.1		6-CF	HEK293-OAT3	Liao, 2020
Lesinurad	1.07		Urate	HEK293-OAT3	Taniguchi, 2019
Linezolid	21.9		Estrone sulfate¹	HEK293-OAT3	Parvez, 2016
Linezolid	53		Relebactam	MDCKII-OAT3	Chan, 2019
Losartan	0.36		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Losartan	1.6		Uric acid	HEK293-OAT3	Sato, 2008
Losartan carboxylic acid	0.1		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Loxoprofen	34.2		Pemetrexed	HEK-OAT3	Kurata, 2014
Mefenamic acid	1.75		6-CF	COS-7-OAT3	Duan, 2012
Mefenamic acid	0.78		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Meloxicam	0.54		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Methazolamide	97.5		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Methotrexate^1,3	92.2		Baricitinib	HEK-PEAK-OAT3	Posada, 2017
Metronidazole	6.51	6.48	Estrone sulfate¹	HEK293-OAT3	Lu, 2018
Mycophenolic acid	4.3		Methotrexate^1,3	HEK293-OAT3	El-Sheikh, 2013
N-desmethyl rosiglitazone	1.15		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Nalidixic acid	24.87		Estrone sulfate¹	HEK293-OAT3	Burckhardt, 2017
Naproxen	4.75		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Naproxen	4.67		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Naproxen	4.6		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
Nateglinide	0.86		6-CF	COS-7-OAT3	Duan, 2012
Nilotinib	0.41		Estrone sulfate¹	HEK293-OAT3	Johnston, 2014
Nitazoxanide	0.154		6-CF	COS-7-OAT3	Duan, 2012
Nitrofurantoin	6.23	5.86	Estrone sulfate¹	HEK293-OAT3	Lu, 2018
Novobiocin	4.99	4.77	Estrone sulfate¹	COS7-OAT3	Duan, 2009
O-desmethyl indomethacin	0.27		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Octanoate		8.6	Ochratoxin A	S2-OAT2	Jung, 2001
Olaparib	18.4		Furosemide³	HEK293-OAT3	McCormick, 2017
Olmesartan	0.027		Uric acid	HEK293-OAT3	Sato, 2008
Omeprazole	5.5		Methotrexate^1,3	HEK293-OAT3	Narumi, 2017
Omeprazole	5.1		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
Oxaprozin	0.87		6-CF	COS-7-OAT3	Duan, 2012
Para-aminohippurate⁴		19.6	Ochratoxin A	S2-OAT2	Jung, 2001
Para-Aminosalicylic acid (PAS)	24.6		Estrone sulfate¹	HEK293-OAT3	Parvez, 2016
Penicillin G³	102	88	Bestatin	HEK293-OAT3	Zhu, 2012
Phenacetin	19.4		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Piclidenoson		8.7	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Pimelate	634		Estrone sulfate¹	HEK293-OAT3	Kaufhold, 2011
Pioglitazone	1.02		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Piperacillin	108		Relebactam	MDCKII-OAT3	Chan, 2019
Piroxicam	2.52		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Piroxicam		4.88	Ochratoxin A	S2-OAT2	Jung, 2001
Pratosartan	0.095		Uric acid	HEK293-OAT3	Sato, 2008
Pravastatin¹	13.7		Estrone sulfate¹	S2-OAT3	Takeda, 2004
Pravastatin¹	76.3		Pemetrexed	HEK-OAT3	Kurata, 2014
Prazosin	29.84		Estrone sulfate¹	HEK293-OAT3	Burckhardt, 2017
Probenecid^2,4	1.25		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Probenecid^2,4	14.4		Amoxicillin	HEK293-OAT3	Parvez, 2018
Probenecid^2,4	4.41		Baricitinib	HEK-PEAK-OAT3	Posada, 2017
Probenecid^2,4	3.1		Cimetidine	CHO-OAT3	Chu, 2007
Probenecid^2,4		32	Dimesna	HeLa-OAT3	Cutler, 2012
Probenecid^2,4		9	Estrone sulfate¹	S2-OAT3	Takeda, 2001
Probenecid^2,4		1.3	Fexofenadine	HEK293-OAT3	Tahara, 2006
Probenecid^2,4	5.8		Hydrochlorothiazide	HEK293-OAT3	Yin, 2019
Probenecid^2,4	12.5		Isoniazid	HEK293-OAT3	Parvez, 2018
Probenecid^2,4		4.41	Ochratoxin A	S2-OAT3	Jung, 2001
Probenecid^2,4	24.6		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
Probenecid^2,4	1.9		Relebactam	MDCKII-OAT3	Chan, 2019
Probenecid^2,4	5.6		Sitagliptin	CHO-OAT3	Chu, 2007
Probenecid acyl b-D-glucuronide	19.9		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Quinapril	6.2		Sitagliptin	CHO-OAT3	Chu, 2007
Rabeprazole	4.8		Methotrexate^1,3	HEK293-OAT3	Narumi, 2017
Raltegravir	18.8		Estrone sulfate¹	MDCKII-OAT3	Rizk, 2014
Remdesivir		14	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Rifabutin	54		Estrone sulfate¹	HEK293-OAT3	Parvez, 2016
Rifampin	30.2		Estrone sulfate¹	HEK293-OAT3	Parvez, 2016
Rifapentine	52.9		Estrone sulfate¹	HEK293-OAT3	Parvez, 2016
Rivaroxaban	8.2		Estrone sulfate¹	HEK293-OAT3	Tsuruya, 2017
Rosiglitazone	0.59		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Ruxolitinib		6.1	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Sacubitril	0.795		Estrone sulfate¹	HEK293-OAT3	Hanna, 2018
Selexipag	1.7		Furosemide³	HEK293-OAT3	Gnerre, 2018
Sildenafil		20.5	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Simvastatin	32.3		Estrone sulfate¹	S2-OAT3	Takeda, 2004
Sitagliptin	160		Cimetidine	CHO-OAT3	Chu, 2007
Suberate	232		Estrone sulfate¹	HEK293-OAT3	Kaufhold, 2011
Sulfadiazine	6.65	3.98	Estrone sulfate¹	HEK293-OAT3	Lu, 2018
Sulfasalazine	3		Methotrexate^1,3	OAT3-expressing oocytes	Elsby, 2011
Sulindac	1.65		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Sulindac	3.62		Estrone sulfate¹	S2-OAT3	Khamdang, 2002
Sulindac sulfide	0.66		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Sulindac sulfone	0.6		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Telmisartan	1.38		Bestatin	HEK293-OAT3	Huo, 2014
Telmisartan	1.6		Uric acid	HEK293-OAT3	Sato, 2008
Teriflunomide	0.87		6-CF	HEK293-OAT3	Liao, 2020
Tetrabromobisphenol A	0.5		Estrone sulfate¹	HEK293 cells	Bruyere, 2017
Tetramethrin	77.6		Fluorescein	HEK293 cells	Chedik, 2017
Thalidomide		54.6	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Tofacitinib		51.6	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Tolmetin	0.81		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Tolmetin b-D-glucuronide	2.92		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Trazodone	2.94		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
Triazavirin		2.3	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Trichlormethiazide	71.2		Estrone sulfate¹	S2-OAT3	Hasannejad, 2004
Umifenovir		58.6	Estrone sulfate¹	HEK293-OAT3	Yee, 2021
Valsartan	0.25		6-CF	COS-7-OAT3	Duan, 2012
Valsartan	0.36		Bestatin	HEK293-OAT3	Huo, 2014
Valsartan	1.11		Estrone sulfate¹	HEK293-OAT3	Hanna, 2018
Valsartan	2.3		Hydrochlorothiazide	HEK293-OAT3	Yin, 2019
Valsartan	0.2		Uric acid	HEK293-OAT3	Sato, 2008
Warfarin	3.11		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021

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	OATs	Cefiderocol	Furosemide³	1.01	1.00	ND	ND	1.25	ND	Katsube, 2018	DDI 1
2	OATs/OCTs	Cotrimoxazole (trimethoprim/sulfamethoxazole)	Apricitabine	1.7	1.3	0.6	0.6	1.4	ND	Shiveley, 2008	DDI 2
3	OATs/OCTs	Cotrimoxazole (trimethoprim/sulfamethoxazole)	Zidovudine	NS	ND	0.4	NS	NS	ND	Chatton, 1992	DDI 3
4	OATs	Furosemide³	Lomefloxacin	1.1	NS	0.7	0.9	NS	ND	Sudoh, 1994	DDI 4
5	OATs/BCRP	Isavuconazole	Methotrexate^1,3	0.97	0.89	ND	ND	ND	ND	Yamazaki, 2017	DDI 5
6	OATs	Nitisinone	Furosemide³	1.72	1.12	ND	ND	ND	ND	Huledal, 2019	DDI 6
7	OATs	PAH (120 mg)	Adefovir³	1.73	ND	0.49	ND	ND	ND	Maeda, 2014	DDI 7
8	OATs	PAH (120 mg)	Benzylpenicillin^1,2	0.69	ND	1.25	ND	ND	ND	Maeda, 2014	DDI 8
9	OATs	PAH (210 mg)	Adefovir³	1.44	ND	0.54	ND	ND	ND	Maeda, 2014	DDI 9
10	OATs	PAH (210 mg)	Benzylpenicillin^1,2	0.44	ND	1.47	ND	ND	ND	Maeda, 2014	DDI 10
11	OATs	Probenecid^2,4	Acyclovir	1.4	ND	0.7	NS	ND	ND	Laskin, 1982	DDI 11
12	OATs	Probenecid^2,4	Baricitinib	2.03	1.03	0.31	0.49	1.63	ND	Posada, 2017	DDI 12
13	OATs	Probenecid^2,4	Cefaclor³	2.1	1.5	ND	ND	1.6	ND	Welling, 1979	DDI 13
14	OATs	Probenecid^2,4	Cefonicid	2.1	1.2	0.3	ND	1.5	ND	Pitkin, 1981	DDI 14
15	OATs	Probenecid^2,4	Cefoxitin	2.4	ND	0.4	ND	2.0	ND	Vlasses, 1980	DDI 15
16	OATs	Probenecid^2,4	Ceftriaxone	0.7	ND	ND	1.3	0.8	ND	Stoeckel, 1988	DDI 16
17	OATs	Probenecid^2,4	Cephradine	2.4	1.9	ND	ND	1.5	ND	Welling, 1979	DDI 17
18	OATs	Probenecid^2,4	Cidofovir	ND	ND	0.5	0.6	ND	ND	Cundy, 1995	DDI 18
19	OATs/MRPs	Probenecid^2,4	Ciprofloxacin	1.7	NS	0.4	0.6	1.5	ND	Jaehde, 1995	DDI 19
20	OATs	Probenecid^2,4	Dicloxacillin	1.9	1.8	0.3	0.5	ND	ND	Beringer, 2008	DDI 20
21	OATs	Probenecid^2,4	Empagliflozin	1.52	1.24	0.46	ND	1.10	ND	Macha, 2014	DDI 21
22	OATs	Probenecid^2,4	Famotidine³	1.8	1.5	0.4	0.1	NS	ND	Inotsume, 1990	DDI 22
23	OATs/MRPs	Probenecid^2,4	Furosemide³	2.7	1.5	0.3	0.4	1.7	ND	Vree, 1995	DDI 23
24	OATs	Probenecid^2,4	Mesna	1.89	1.44	0.44	ND	1.05	ND	Cutler, 2012	DDI 24
25	OATs	Probenecid^2,4	Mesna	1.89	1.44	0.44	ND	1.05	ND	Cutler, 2012	DDI 25
26	OATs	Probenecid (1500 mg)	Adefovir³	1.82	ND	0.52	ND	ND	ND	Maeda, 2014	DDI 26
27	OATs	Probenecid (1500 mg)	Benzylpenicillin^1,2	3.27	ND	0.22	ND	ND	ND	Maeda, 2014	DDI 27
28	OATs	Probenecid (750 mg)	Adefovir³	2.09	ND	0.44	ND	ND	ND	Maeda, 2014	DDI 28
29	OATs	Probenecid (750 mg)	Benzylpenicillin^1,2	1.83	ND	0.46	ND	ND	ND	Maeda, 2014	DDI 29

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