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SLC22A6

Synonyms: FLJ55736, HOAT1, MGC45260, OAT1, PAHT, ROAT1

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Orthologs in other species

rat Slc22a6

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	`0.00114`
Kidney*	Nishimura	`0.853`
Liver	Nishimura	`0.0000606`
Placenta	Nishimura	BLQ
Small Intestine	Nishimura	BLQ
Kidney*	Mean across all PMT Samples	`38.271`
Liver	Mean across all PMT Samples	`0.0578`

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
6-carboxyfluorescein	3.93	CHO-OAT1	Cihlar, 2000
Acamprosate	700	HEK293-Flp-In-OAT1	Antonescu, 2020
Acyclovir	342	S2-OAT1	Takeda, 2002
Adefovir^1,3	30	OAT1-expressing oocytes	Cihlar, 1999
Adefovir^1,3	23.8	CHO-OAT1	Ho, 2000
Adefovir^1,3	23.8	CHO-OAT1	Cihlar, 2000
Cidofovir¹	46	OAT1-expressing oocytes	Cihlar, 1999
Cidofovir¹	58	CHO-OAT1	Ho, 2000
Cidofovir¹	58	CHO-OAT1	Cihlar, 2000
Cidofovir¹	30	CHO-OAT1	Chu, 2007
Dimesna	636	HeLa-OAT1	Cutler, 2012
Edaravone sulfate	10.8	HEK293-OAT1	Mizuno, 2007
Ganciclovir³	896	S2-OAT1	Takeda, 2002
Glutarate	10.7	CHO-OAT1	Cihlar, 2000
Hydrochlorothiazide	112	HEK293-OAT1	Yin, 2019
Methotrexate³	554	S2-OAT1	Takeda, 2002
Methotrexate³	724	OAT1-expressing oocytes	Uwai, 2004
Ochratoxin A	0.42	S2-OAT1	Jung, 2001
Olmesartan	0.0683	HEK293-OAT1	Yamada, 2007
Para-aminohippurate^1,4	9.3	OAT1-expressing oocytes	Hosoyamada, 1999
Para-aminohippurate^1,4	5	HeLa-OAT1	Lu, 1999
Para-aminohippurate^1,4	4	OAT1-expressing oocytes	Cihlar, 1999
Para-aminohippurate^1,4	15.4	CHO-OAT1	Ho, 2000
Para-aminohippurate^1,4	15.4	CHO-OAT1	Cihlar, 2000
Para-aminohippurate^1,4	20.1	S2-OAT1	Takeda, 2001
Para-aminohippurate^1,4	3.9	OAT1-expressing oocytes	Islinger, 2001
Para-aminohippurate^1,4	28	HEK293-OAT1	Ueo, 2005
Para-aminohippurate^1,4	28	HEK293 cells	Ueo, 2005
Para-Aminosalicylic acid (PAS)	78	HEK293-OAT1	Parvez, 2017
Perfluorooctanoic acid	48	HEK293 cells	Nakagawa, 2008
Piperacillin	37	HEK293-OAT1	Wen, 2018
Prostaglandin E2	0.97	S2-OAT1	Kimura, 2002
Prostaglandin F2-alpha	0.575	S2-OAT1	Kimura, 2002
Tazobactam	431	HEK293-OAT1	Wen, 2018
Tenofovir¹	33.8	CHO-OAT1	Cihlar, 2001
Uric acid	197.6	HEK293-OAT1	Sato, 2008
Valsartan	4.72	HEK293-OAT1	Hanna, 2018
Zalcitabine	ND	CHO-OAT1	Jin, 2006
Zidovudine	45.9	S2-OAT1	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	147		Para-aminohippurate^1,4	S2 cells	Tachampa, 2008
(Noradamantan-3-yl)-1,3-dipropylxanthine (KW-3902)		7.82	Para-aminohippurate^1,4	S2-OAT1	Takeda, 2001
(S)-7-hydroxy warfarin	14.5		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
(S)-ketoprofen b-D-glucuronide	40.2		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
(S)-naproxen acyl-b-D-glucuronide	>200		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
(S)eO-desmethyl naproxen	4.7		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
1-butanesulfonic acid (BSA)	514		Para-aminohippurate^1,4	CHO-OAT1	Astorga, 2011
1-propanesulfonic acid (PSA)	2036		Para-aminohippurate^1,4	CHO-OAT1	Astorga, 2011
2,3-Dimercapto-1-propane sulfonate (DMPS)	19		Para-aminohippurate^1,4	OAT1-expressing oocytes	Islinger, 2001
2,3-Dimercapto-1-propane sulfonate (DMPS)	83		Para-aminohippurate^1,4	CHO-OAT1	Astorga, 2011
3-cis-hydroxycyclohexyl glyburide	10.1		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
3-mercapto-1-propansulfonic acid (MPS)	204		Para-aminohippurate^1,4	CHO-OAT1	Astorga, 2011
4-hydroxy-trazodone	>200		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
4-Hydroxy diclofenac	0.48		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
4-Hydroxy flurbiprofen	1.6		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
5-Carboxy-meloxicam	19.6		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
5-Hydroxy Rosiglitazone b-D-Glucuronide	>200		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
5-OH-rosiglitazone sulfate	33.7		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
6-Hydroxy chlorzoxazone	3.6		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Abiraterone	>20		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Abiraterone N-oxide sulfate	>100		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Abiraterone sulfate	38.2		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Acetazolamide	75		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
Acetominophen	639		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Acetylsalicylate	769		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Adefovir^1,3	1.5		Ibuprofen	CHO-OAT1	Mulato, 2000
Adefovir^1,3	0.9		Ketoprofen	CHO-OAT1	Mulato, 2000
Adefovir^1,3	1.8		Naproxen	CHO-OAT1	Mulato, 2000
Adefovir^1,3	8.1		PAH	HeLa-OAT1	Mandikova, 2013
Adipate	6.2		Para-aminohippurate^1,4	HEK293-OAT1	Kaufhold, 2011
Aflatoxin B1	12.3		Para-aminohippurate^1,4	S2 cells	Tachampa, 2008
Alpha-ketoglutarate	4.7		Para-aminohippurate^1,4	HEK293-OAT1	Kaufhold, 2011
Alpha-zearalenol	28.4		Para-aminohippurate^1,4	S2 cells	Tachampa, 2008
Aristolochic acid I	-	0.6	Para-aminohippurate^1,4	HEK293 cells	Bakhiya, 2009
Benzbromarone	3.14		Urate	HEK293-OAT1	Taniguchi, 2019
Betamipron	6		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Betamipron	16.2		Para-aminohippurate^1,4	CHO-OAT1	Ho, 2000
Betamipron		23.6	Para-aminohippurate^1,4	S2-OAT1	Takeda, 2001
Bumetanide	7.6		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
Cabotegravir	0.81		PAH	S2-OAT1	Reese, 2016
Candesartan	17		Uric acid	HEK293-OAT1	Sato, 2008
Cefaclor³	1095.6		Para-aminohippurate^1,4	HEK293 cells	Ueo, 2005
Cefadroxil		6140	Prostaglandin F2-alpha	S2-OAT1	Khamdang, 2003
Cefamandole		30	Prostaglandin F2-alpha	S2-OAT1	Khamdang, 2003
Cefazolin		180	Prostaglandin F2-alpha	S2-OAT1	Khamdang, 2003
Cefdinir	691.8		Para-aminohippurate^1,4	HEK293 cells	Ueo, 2005
Cefoperazone		210	Prostaglandin F2-alpha	S2-OAT1	Khamdang, 2003
Cefoselis	2600.5		Para-aminohippurate^1,4	HEK293 cells	Ueo, 2005
Cefotaxime		3130	Prostaglandin F2-alpha	S2-OAT1	Khamdang, 2003
Cefotiam	639.7		Para-aminohippurate^1,4	HEK293 cells	Ueo, 2005
Ceftibuten	563.1		Para-aminohippurate^1,4	HEK293 cells	Ueo, 2005
Ceftizoxime³	3598.6		Para-aminohippurate^1,4	HEK293 cells	Ueo, 2005
Ceftriaxone		230	Prostaglandin F2-alpha	S2-OAT1	Khamdang, 2003
Celecoxib	>200		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Celecoxib carboxylic acid	262		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Cephaloridine	1250		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
Cephaloridine	2470		Para-aminohippurate^1,4	HEK293 cells	Ueo, 2005
Cephaloridine		740	Prostaglandin F2-alpha	S2-OAT1	Khamdang, 2003
Cephalothin		220	Prostaglandin F2-alpha	S2-OAT1	Khamdang, 2003
Cephradine	1600		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
Chlorambucil	44.3		PAH	HEK293-OAT1	Hagos, 2015
Chlorothiazide	3.78		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
Chlorzoxazone	52.3		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Cidofovir¹	60		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
Cilastatin		1470	Para-aminohippurate^1,4	S2-OAT1	Takeda, 2001
Ciprofloxacin	35.1		PAH	HEK293-OAT1	Parvez, 2016
Citreoviridin A	16.9		Para-aminohippurate^1,4	S2 cells	Tachampa, 2008
Citrinin		3080	Ochratoxin A	S2-OAT1	Jung, 2001
Cyclopiazonic acid	6.59		Para-aminohippurate^1,4	S2 cells	Tachampa, 2008
Cyclothiazide	84.3		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
Dabrafenib	6.9		6-CF	S2-OAT1	Ellens, 2017
Dantrolene	78.3		Glutarate	HEK293-OAT1	Burckhardt, 2017
Dantrolene	1.89		PAH	HEK293-OAT1	Burckhardt, 2017
Diclofenac	1.67		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Diclofenac	4		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Diclofenac	4.46		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Diclofenac	1.8		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
Diflunisal	0.85		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Dotinurad	4.08		Urate	HEK293-OAT1	Taniguchi, 2019
Eprosartan	0.13		Bestatin	HEK293-OAT1	Huo, 2014
Estrone sulfate	170		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Ethacrynic acid	29.6		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
Etodolac	50		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Flurbiprofen	1.91		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Flurbiprofen	1.5		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Fluvastatin	26.3		Para-aminohippurate^1,4	S2-OAT1	Takeda, 2004
Fumarate	1733		Para-aminohippurate^1,4	HEK293-OAT1	Kaufhold, 2011
Fumonisin B1	768		Para-aminohippurate^1,4	S2 cells	Tachampa, 2008
Furosemide³	18		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
Glafenine	54.5		Glutarate	HEK293-OAT1	Burckhardt, 2017
Gliotoxin	117		Para-aminohippurate^1,4	S2 cells	Tachampa, 2008
Glutarate	4.9		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
Glutarate	3.3		Para-aminohippurate^1,4	HEK293-OAT1	Kaufhold, 2011
Glyburide	5.7		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Hippuric acid	20		Para-aminohippurate^1,4	OK-OAT1	Motojima, 2002
Hydrochlorothiazide	126		PAH	HEK293-OAT1	Yin, 2019
Hydrochlorothiazide	67.3		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
Hydroxy pioglitazone	27.6		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Ibuprofen	8		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Ibuprofen	55.6		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Ibuprofen	5.1		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
Imatinib	29.2		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Imatinib (piperidine)-4-oxide	>200		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Indoleacetic acid	83		Para-aminohippurate^1,4	OK-OAT1	Motojima, 2002
Indomethacin	4.35		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Indomethacin	3		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Indomethacin	3.83		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Indomethacin	1.91		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
Indoxyl sulfate	83		Para-aminohippurate^1,4	OK-OAT1	Motojima, 2002
Irbesartan	0.039		Bestatin	HEK293-OAT1	Huo, 2014
JBP485	226	197	Bestatin	HEK293-OAT1	Zhu, 2012
Keto pioglitazone	12.5		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Ketoconazole	5.7		PAH	HEK293-OAT1	Vermeer, 2016
Ketoconazole	319		Para-aminohippurate^1,4	OAT1-expressing oocytes	Choi, 2011
Ketoprofen	1.4		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
Ketoprofen	1.73		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Ketoprofen	1.3		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Ketoprofen	4.34		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Ketorolac tromethamine	0.653		6-CF	COS-7-OAT1	Duan, 2012
Lansoprazole	4.13		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
Lesinurad	6.99		Urate	HEK293-OAT1	Taniguchi, 2019
Linezolid	31.1		PAH	HEK293-OAT1	Parvez, 2016
Losartan	11.4		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Losartan	12		Uric acid	HEK293-OAT1	Sato, 2008
Losartan carboxylic acid	0.69		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Mefenamic acid	1.085		6-CF	COS-7-OAT1	Duan, 2012
Mefenamic acid	0.83		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Meloxicam	6.88		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Methazolamide	438		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
N-desmethyl rosiglitazone	33.3		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Nalidixic acid	10.8		Glutarate	HEK293-OAT1	Burckhardt, 2017
Nalidixic acid	110.6		PAH	HEK293-OAT1	Burckhardt, 2017
Naproxen	3.23		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Naproxen	5.8		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Naproxen	5.67		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Naproxen	4.13		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
Novobiocin	34.8	14.9	Para-aminohippurate^1,4	COS7-OAT1	Duan, 2009
O-desmethyl indomethacin	1.62		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Octanoate		5.41	Ochratoxin A	S2-OAT1	Jung, 2001
Olmesartan	0.28		Uric acid	HEK293-OAT1	Sato, 2008
Omeprazole	1.76		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
Ortho-Hydroxyhippuric acid	27		Para-aminohippurate^1,4	OK-OAT1	Motojima, 2002
Oxaprozin	0.891		6-CF	COS-7-OAT1	Duan, 2012
Para-aminohippurate^1,4	8.8		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
Para-aminohippurate^1,4	106	92	Bestatin	HEK293-OAT1	Zhu, 2012
Para-aminohippurate^1,4		6.02	Ochratoxin A	S2-OAT1	Jung, 2001
Para-Aminosalicylic acid (PAS)	37.6		PAH	HEK293-OAT1	Parvez, 2016
Para-Hydroxyhippuric acid	25		Para-aminohippurate^1,4	OK-OAT1	Motojima, 2002
Patulin	44.8		Para-aminohippurate^1,4	S2 cells	Tachampa, 2008
Phenacetin	200		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Phenacetin	275		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Pimelate	18.6		Para-aminohippurate^1,4	HEK293-OAT1	Kaufhold, 2011
Pioglitazone	6.3		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Piroxicam	20.5		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Piroxicam		19.8	Ochratoxin A	S2-OAT1	Jung, 2001
Piroxicam	62.8		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Pratosartan	1.5		Uric acid	HEK293-OAT1	Sato, 2008
Pravastatin	408		Para-aminohippurate^1,4	S2-OAT1	Takeda, 2004
Prazosin	4.89		PAH	HEK293-OAT1	Burckhardt, 2017
Probenecid^2,4	6.3		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
Probenecid^2,4	7.74		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Probenecid^2,4	7.4		Adefovir^1,3	CHO-OAT1	Mulato, 2000
Probenecid^2,4	3.9		Cidofovir¹	CHO-OAT1	Chu, 2007
Probenecid^2,4		26	Dimesna	HeLa-OAT1	Cutler, 2012
Probenecid^2,4	7.1		Hydrochlorothiazide	HEK293-OAT1	Yin, 2019
Probenecid^2,4	17		Methotrexate³	OAT1-expressing oocytes	Elsby, 2011
Probenecid^2,4		4.29	Ochratoxin A	S2-OAT1	Jung, 2001
Probenecid^2,4	6.5		Para-aminohippurate^1,4	CHO-OAT1	Ho, 2000
Probenecid^2,4		12.1	Para-aminohippurate^1,4	S2-OAT1	Takeda, 2001
Probenecid^2,4	17		Para-aminohippurate^1,4	OAT1-expressing oocytes	Elsby, 2011
Probenecid^2,4	16.3		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
Probenecid acyl b-D-glucuronide	130		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Raltegravir	108		Cidofovir¹	MDCKII-OAT1	Rizk, 2014
Rifabutin	55.1		PAH	HEK293-OAT1	Parvez, 2016
Rifampin		62.2	Olmesartan	OAT1-expressing oocytes	Choi, 2011
Rifampin	48.1		PAH	HEK293-OAT1	Parvez, 2016
Rifampin	79.1		Para-aminohippurate^1,4	OAT1-expressing oocytes	Choi, 2011
Rifapentine	61.8		PAH	HEK293-OAT1	Parvez, 2016
Rosiglitazone	4.2		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Salicylate	280		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
Salicylate	325		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Selexipag	1.4		PAH	CHO-OAT1	Gnerre, 2018
Simvastatin	73.6		Para-aminohippurate^1,4	S2-OAT1	Takeda, 2004
Simvastatin	41.5		Para-aminohippurate^1,4	OAT1-expressing oocytes	Windass, 2007
Suberate	19.3		Para-aminohippurate^1,4	HEK293-OAT1	Kaufhold, 2011
Sulfasalazine	4.6		Methotrexate³	OAT1-expressing oocytes	Elsby, 2011
Sulindac	56.8		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Sulindac	36.2		Para-aminohippurate^1,4	S2-OAT1	Khamdang, 2002
Sulindac sulfide	3.68		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Sulindac sulfone	23		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Telmisartan	0.44		Bestatin	HEK293-OAT1	Huo, 2014
Telmisartan	0.46		Uric acid	HEK293-OAT1	Sato, 2008
Tenofovir¹	29.3		PAH	HeLa-OAT1	Mandikova, 2013
Teriflunomide	3.39		6-CF	HEK293-OAT1	Liao, 2020
Tolmetin	3.01		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Tolmetin b-D-glucuronide	7.17		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Trazodone	19.9		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
Triazavirin		4.1	Para-aminohippurate^1,4	HEK293-OAT1	Yee, 2021
Trichlormethiazide	19.2		Para-aminohippurate^1,4	S2-OAT1	Hasannejad, 2004
Valsartan	1.97		Bestatin	HEK293-OAT1	Huo, 2014
Valsartan	14.8		Cidofovir¹	HEK293-OAT1	Hanna, 2018
Valsartan	9		Hydrochlorothiazide	HEK293-OAT1	Yin, 2019
Valsartan	16		Uric acid	HEK293-OAT1	Sato, 2008
Warfarin	15.8		6-carboxyfluorescein	HEK293-OAT1	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	Methotrexate³	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)	Adefovir^1,3	1.73	ND	0.49	ND	ND	ND	Maeda, 2014	DDI 7
8	OATs	PAH (120 mg)	Benzylpenicillin²	0.69	ND	1.25	ND	ND	ND	Maeda, 2014	DDI 8
9	OATs	PAH (210 mg)	Adefovir^1,3	1.44	ND	0.54	ND	ND	ND	Maeda, 2014	DDI 9
10	OATs	PAH (210 mg)	Benzylpenicillin²	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	Cidofovir¹	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)	Adefovir^1,3	1.82	ND	0.52	ND	ND	ND	Maeda, 2014	DDI 26
27	OATs	Probenecid (1500 mg)	Benzylpenicillin²	3.27	ND	0.22	ND	ND	ND	Maeda, 2014	DDI 27
28	OATs	Probenecid (750 mg)	Adefovir^1,3	2.09	ND	0.44	ND	ND	ND	Maeda, 2014	DDI 28
29	OATs	Probenecid (750 mg)	Benzylpenicillin²	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