UCSF home page | About UCSF | UCSF Medical Center

Skip to TransPortal content

Enlarge Text
Click to increase the text size. Restore Text
Click to restore original text size. Reduce Text
Click to decrease the text size.


Decrease the text size \| Restore text size \| Increase the text size

SLC22A2

Synonyms: MGC32628, OCT2

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Orthologs in other species

rat Slc22a2

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	`0.0000494`
Kidney*	Nishimura	`0.139`
Liver	Nishimura	`0.0000367`
Placenta	Nishimura	`0.0000884`
Small Intestine	Nishimura	BLQ
Kidney*	Mean across all PMT Samples	`44.361`
Liver	Mean across all PMT Samples	`0.339`

Note that relative expression values should only be compared between entries of the same source.

Back to top

In Vitro Substrates

Substrate	Km (μM)	Cell System	Reference
1-methyl-4-phenylpyridinium (MPP+)	5.1	CHO-OCT2	Severance, 2017
1-methyl-4-phenylpyridinium (MPP+)	4.6	CHO-OCT2	Sandoval, 2018
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	24	HEK293-OCT2	Biermann, 2006
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	37.6	CHO-OCT2	Sandoval, 2018
Amantadine	27	HEK293-OCT2	Busch, 1998
Amiloride	95	HEK293-OCT2	Biermann, 2006
Amisulpride	167.9	HEK293-OCT2	Dos, 2014
Amphetamine	0.83	HEK293-OCT2	Wagner, 2017
Amphetamine	534	HEK293-OCT2	Wagner, 2017
Anisodine	13.3	HEK293-OCT2	Chen, 2019
Atenonol	280	HEK293-OCT2	Yin, 2015
Berberine	1.01	MDCK-OCT2	Sun, 2014
Cadmium ion (Cd2+)	54	HEK293-OCT2	Thevenod, 2013
Choline	465	CHO-OCT2	Severance, 2017
Cimetidine²	72.6	HEK293-OCT2	Tahara, 2005
Cimetidine²	20.8	CHO-OCT2	Severance, 2017
Cimetidine²	15.1	CHO-OCT2	Sandoval, 2018
Cisplatin	11	HEK293-OCT2	Filipski, 2008
Dopamine	1400	HEK293-OCT2	Amphoux, 2006
Entecavir	300	MDCK-OCT2	Yang, 2016
Epinephrine	420	HEK293-OCT2	Amphoux, 2006
Ethambutol	314	HEK293-OCT2	Te, 2016
Ethambutol	212	HEK293-OCT2	Parvez, 2018
Famotidine	56.1	HEK293-OCT2	Tahara, 2005
Fampridine	51	HEK293-OCT2	Xiao, 2018
Histamine	940	HEK293-OCT2	Amphoux, 2006
Hydrochlorothiazide	812	HEK293-OCT2	Yin, 2019
Lamivudine	46.3	OCT2-expressing oocytes	Choi, 2012
Memantine	34	HEK293-OCT2	Busch, 1998
Metformin^1,3	990	HEK293-OCT2	Kimura, 2005
Metformin^1,3	1072	HEK293-OCT2	Choi, 2007
Metformin^1,3	3356	HEK293-OCT2	Zolk, 2009
Metformin^1,3	3171	HEK293-OCT2	Zolk, 2009
Metformin^1,3	680	HeLa-OCT2	Meyer, 2010
Metformin^1,3	235	OCT2-expressing oocytes	Sogame, 2013
Metformin^1,3	518	CHO-OCT2	Severance, 2017
Metformin^1,3	285.2	CHO-OCT2	Sandoval, 2018
Methamphetamine	2.09	HEK293-OCT2	Wagner, 2017
Monocrotaline	64.7	HEK293-OCT2	Chen, 2019
Morphine	ND	HEK293-OCT2	Zhu, 2018
N-methylpyridinium	19	OCT2-expressing oocytes	Gorboulev, 1997
N-methylpyridinium	16	HEK293-OCT2	Busch, 1998
N-methylpyridinium	19.5	HEK293-OCT2	Zolk, 2009
N-methylpyridinium	19.5	HEK293-OCT2	Zolk, 2009
N1-methyladenosine (m1A)	ND	HEK293-OCT2	Miyake, 2019
Nadolol	122	HEK293-OCT2	Misaka, 2016
NBD-MTMA	14.5	CHO-OCT2	Severance, 2017
NBD-MTMA	8.8	CHO-OCT2	Sandoval, 2018
Nitidine chloride	0.97	MDCK-OCT2	Li, 2016
Norepinephrine	1500	HEK293-OCT2	Amphoux, 2006
P-tyramine	0.0331	Caco-2 cells	Sarkar, 2020
Para-Aminosalicylic acid (PAS)	28.7	HEK293-OCT2	Parvez, 2017
Paraquat	114	HEK293 cells	Chen, 2007
Phenformin	37.4	OCT2-expressing oocytes	Sogame, 2013
Proguanil	9	HEK293-OCT2	van, 2017
Prostaglandin E2	0.0289	S2-OCT2	Kimura, 2002
Prostaglandin F2-alpha	0.344	S2-OCT2	Kimura, 2002
Ranitidine	65.2	HEK293-OCT2	Tahara, 2005
Serotonin	290	HEK293-OCT2	Amphoux, 2006
Sulpiride	187.2	HEK293-OCT2	Dos, 2014
Sulpiride	68	HEK293-OCT2	Takano, 2017
Sulpiride	390	MDCK-OCT2	Li, 2017
Tetraethylammonium¹	76	OCT2-expressing oocytes	Gorboulev, 1997
Tetraethylammonium¹	33.8	OCT2-expressing oocytes	Okuda, 1999
Tetraethylammonium¹	71.9	CHO-OCT2	Severance, 2017
Tetraethylammonium¹	57.7	CHO-OCT2	Sandoval, 2018
Trospium	2.1	MDCK-OCT2	Deutsch, 2019
Varenicline	370	HEK293-OCT2	Feng, 2008
Veliparib	44.6	HEK293-OCT2	Kikuchi, 2013
YM155	2.67	HEK293-OCT2	Minematsu, 2010

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	24.8		Tetraethylammonium¹	S2 cells	Tachampa, 2008
1-ethylpyridinium chloride (EtPy-Cl)	36.7		Tetraethylammonium¹	CHO-OCT2	Cheng, 2011
1-hexylpyridinium chloride (HePy-Cl)	0.35		Tetraethylammonium¹	CHO-OCT2	Cheng, 2011
1-methyl-3-butylimidazolium chloride (Bmim-Cl)	1.5		Tetraethylammonium¹	CHO-OCT2	Cheng, 2011
1-methyl-4-phenylpyridinium (MPP+)	7		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
1-methyl-4-phenylpyridinium (MPP+)	3		NBD-MTMA	CHO-OCT2	Belzer, 2013
3,4-methylenedioxymetamphetamine (MDMA)		1.63	N-methylpyridinium	HEK293-OCT2	Amphoux, 2006
Aconitine	59.2	145.6	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Aflatoxin B1	121		Tetraethylammonium¹	S2 cells	Tachampa, 2008
Allethrin	42.6		Rhodamine 123	HEK293 cells	Chedik, 2017
Alpha-zearalenol	34.3		Tetraethylammonium¹	S2 cells	Tachampa, 2008
Amantadine	51		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Amantadine	10.1		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Amantadine	27.1		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Amantadine		28.4	N-methylpyridinium	HEK293-OCT2	Amphoux, 2006
Amantadine	24.5		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Amantadine	32.1		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Amantadine	45.9		YM155	HEK293-OCT2	Minematsu, 2010
Amitriptyline	11.3		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Amitriptyline	1.8		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Amitriptyline	0.51		Metformin^1,3	HEK293-OCT2	Hacker, 2015
Amitriptyline	2.4		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Amitriptyline	14		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Amitriptyline	2.5		NBD-MTMA	CHO-OCT2	Belzer, 2013
Amitriptyline	4		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Amitriptyline	2.4	2.5	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Amitriptyline	5		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Amodiaquine	11		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	van, 2017
Amphetamine	20.3		Metformin^1,3	HEK293-OCT2	Wagner, 2017
Anastrozole	327.6		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Anastrozole	39.2		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Anastrozole	51.1		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Anastrozole	86		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Anastrozole	113.4		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Anisodine	139.6		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Chen, 2019
Atomoxetine	20.4		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Atomoxetine	3.5		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Atomoxetine	6.6		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Atomoxetine	7.6		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Atomoxetine	12.8		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Atropine	12.4		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Atropine	1.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Atropine	1.3		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Atropine	39		N-methylpyridinium	HEK293-OCT2	Muller, 2005
Atropine	2.3		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Atropine	2	2.4	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Atropine	3.4		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Benztropine	13.4		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Benztropine	0.3		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Benztropine	0.4		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Benztropine	0.8		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Benztropine	1		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Berberine	8		1-methyl-4-phenylpyridinium (MPP+)	MDCK-OCT2	Sun, 2014
Berberine	0.438		Norepinephrine	MDCK-OCT2	Sun, 2014
Berberine	0.371		Serotonin	MDCK-OCT2	Sun, 2014
Bithionol	1.9		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Bupropion	32.2		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Bupropion	11.1		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Bupropion	8.6		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Bupropion	10.8		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Bupropion	13.4		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Buspirone	68.5		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Buspirone	12		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Buspirone	8.6		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Buspirone	10.2		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Buspirone	19.6		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Buspirone	19.8		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Butylscopolamine	764		N-methylpyridinium	HEK293-OCT2	Muller, 2005
Camostat	16.5		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Carvedilol	55.2		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Carvedilol	63		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Carvedilol	13.1		NBD-MTMA	CHO-OCT2	Belzer, 2013
Cetirizine	ND		Tetraethylammonium¹	OCT2-expressing oocytes	Tsuruoka, 2006
Chelerythrine	10.8		1-methyl-4-phenylpyridinium (MPP+)	OCT2	Shams, 2018
Chlorhexidine	0.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Chloroquine	129		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Chloroquine	9.6		Metformin^1,3	CHO-OCT2	Belzer, 2013
Chloroquine	1096		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Chloroquine	117		NBD-MTMA	CHO-OCT2	Belzer, 2013
Chlorpromazine	14		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Chlorpromazine	2.6		NBD-MTMA	CHO-OCT2	Belzer, 2013
Chlorpyrifos	20.7	24.8	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Choline	435		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Cimetidine²		146	1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Ito, 2012
Cimetidine²	171		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Cimetidine²	113		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Cimetidine²		104	4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Ito, 2012
Cimetidine²		95	m-iodobenzylguanidine (MIBG)	HEK293-OCT2	Ito, 2012
Cimetidine²		124	Metformin^1,3	HEK293-OCT2	Ito, 2012
Cimetidine²	25.4		Metformin^1,3	CHO-OCT2	Belzer, 2013
Cimetidine²	120		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Cimetidine²	70.4		NBD-MTMA	CHO-OCT2	Belzer, 2013
Cimetidine²	111.5		Para-Aminosalicylic acid (PAS)	HEK293-OCT2	Parvez, 2017
Cimetidine²	373		Tetraethylammonium¹	OCT2-expressing oocytes	Okuda, 1999
Cimetidine²		144	Tetraethylammonium¹	HEK293-OCT2	Ito, 2012
Cimetidine²	110		YM155	HEK293-OCT2	Minematsu, 2010
Citreoviridin A	17.7		Tetraethylammonium¹	S2 cells	Tachampa, 2008
Clonidine	6		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Clonidine	0.68		Metformin^1,3	CHO-OCT2	Belzer, 2013
Clonidine	23		N-methylpyridinium	HEK293-OCT2	Muller, 2005
Clonidine	16		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Clonidine	4.5		NBD-MTMA	CHO-OCT2	Belzer, 2013
Cocaine		113	N-methylpyridinium	HEK293-OCT2	Amphoux, 2006
Corticosterone	6.7	9.1	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Corticosterone	5.35		YM155	HEK293-OCT2	Minematsu, 2010
Creatinine	580		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Ciarimboli, 2012
D-amphetamine		10.5	N-methylpyridinium	HEK293-OCT2	Amphoux, 2006
Decynium-22	0.0014		1-methyl-4-phenylpyridinium (MPP+)	MDCK-OCT2	Sun, 2014
Decynium-22	0.005		Norepinephrine	MDCK-OCT2	Sun, 2014
Decynium-22	0.0012		Serotonin	MDCK-OCT2	Sun, 2014
Decynium-22		0.1	Tetraethylammonium¹	OCT2-expressing oocytes	Gorboulev, 1997
Decynium-22	13.8		Tetraethylammonium¹	OCT2-expressing oocytes	Okuda, 1999
Desipramine	16		Tetraethylammonium¹	OCT2-expressing oocytes	Gorboulev, 1997
Desloratadine	60		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Diazepam	32.3		Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Dihydroergotamine	49.9		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Diphenhydramine	15		N-methylpyridinium	HEK293-OCT2	Muller, 2005
Diphenhydramine	21		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Diphenhydramine	5.8		NBD-MTMA	CHO-OCT2	Belzer, 2013
Diphenidol	34.3		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Disopyramide	324		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Disopyramide	39		NBD-MTMA	CHO-OCT2	Belzer, 2013
Dolutegravir	1.9		Metformin^1,3	MDCKII_OCT2	Reese, 2013
Domperidone	7.9		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Doravirine	67		Metformin^1,3	CHO-K1-OCT2	Bleasby, 2019
Doxepin	0.25		Metformin^1,3	HEK293-OCT2	Hacker, 2015
Doxepin	13		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Doxepin	1.5		NBD-MTMA	CHO-OCT2	Belzer, 2013
DX-619		0.94	Creatinine	S2-OCT2	Imamura, 2011
Efavirenz	5.66		Metformin^1,3	MDCK-OCT2	Ceckova, 2018
Epinastine	4.3		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Ethambutol	229		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Parvez, 2016
Ethambutol	189.2		Metformin^1,3	HEK293-OCT2	Parvez, 2016
Ethidium	0.8		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Ethinyl estradiol	2.2		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Ethylacridinium	0.08		NBD-MTMA	CHO-OCT2	Belzer, 2013
Etilefrine	4009		N-methylpyridinium	HEK293-OCT2	Muller, 2005
Famotidine	36.1		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Famotidine	114		N-methylpyridinium	OCT2-expressing oocytes	Bourdet, 2005
Fampridine	66.8		Metformin^1,3	HEK293-OCT2	Xiao, 2018
Fenamiphos	2.8		Dopamine	HEK293 cells	Chedik, 2019
Fenamiphos	6.9		Rhodamine 123	HEK293 cells	Chedik, 2019
Fenfluramine	10		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Fenitrothion	13.2	16.9	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Flecainide	191		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Flecainide	234		NBD-MTMA	CHO-OCT2	Belzer, 2013
Fluoxetine	56.7		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Fluoxetine	16.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Fluoxetine	18.6		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Fluoxetine	20.1		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Fluoxetine	36		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Flurazepam	60		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Furamidine	182		N-methylpyridinium	CHO-OCT2	Ming, 2009
Gabexate	0.9		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Gliotoxin	117		Tetraethylammonium¹	S2 cells	Tachampa, 2008
Granisetron	4.3		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Grepafloxacin		10.4	Creatinine	S2-OCT2	Imamura, 2011
Haloperidol	32.5	51.6	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Imatinib	4.2		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Imatinib	6.7		Creatinine	HEK293-OCT2	Tanihara, 2009
Imipramine	3.9		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Imipramine	28.9		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Imipramine	4.9		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Imipramine	0.5		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Imipramine	0.77		Metformin^1,3	CHO-OCT2	Belzer, 2013
Imipramine	0.4		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Imipramine	6		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Imipramine	1.4		NBD-MTMA	CHO-OCT2	Belzer, 2013
Imipramine	1.4		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Imipramine	1.3		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Indinavir	142		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Ipratropium	15		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Ipratropium	0.17		NBD-MTMA	CHO-OCT2	Belzer, 2013
Irinotecan	15.6		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Irinotecan	2.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Irinotecan	1.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Irinotecan	3.3		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Irinotecan	3.2		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Irinotecan	4.5		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Ketamine		22.7	N-methylpyridinium	HEK293-OCT2	Amphoux, 2006
Lansoprazole	9.5		Metformin^1,3	HEK293-OCT2	Nies, 2011
Lansoprazole	3.28		Metformin^1,3	HEK293-OCT2	Hacker, 2015
Lansoprazole	13		Para-Aminosalicylic acid (PAS)	HEK293-OCT2	Parvez, 2017
Leucomycin	182		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Levomethadone	60		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Lidocaine	104.6	86.8	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Linagliptin	80		Metformin^1,3	HEK293-OCT2	Ishiguro, 2013
Malathion	71.1		Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Mefloquine	204		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Memantine		7.3	N-methylpyridinium	HEK293-OCT2	Amphoux, 2006
Mepiperphenidol	4.8		Tetraethylammonium¹	OCT2-expressing oocytes	Gorboulev, 1997
Mepiperphenidol		4.8	Tetraethylammonium¹	OCT2-expressing oocytes	Gorboulev, 1997
Metformin^1,3	566		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Metformin^1,3	223		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Metformin^1,3	521		N-methylpyridinium	OCT2-expressing oocytes	Bourdet, 2005
Metformin^1,3		289	N-methylpyridinium	HEK293-OCT2	Umehara, 2007
Metformin^1,3	398		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Metformin^1,3	1180		NBD-MTMA	CHO-OCT2	Belzer, 2013
Metformin^1,3	125.6		Para-Aminosalicylic acid (PAS)	HEK293-OCT2	Parvez, 2017
Metformin^1,3		1380	Tetraethylammonium¹	HEK293-OCT2	Umehara, 2007
Methamphetamine	15		Metformin^1,3	HEK293-OCT2	Wagner, 2017
Mexiletine	50.4		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Mexiletine	19.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Mexiletine	21.5		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Mexiletine	55		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Mexiletine	30.5		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Mexiletine	28.5		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Mianserin	17.7		Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Mitoxantrone	73.3		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
MK-801		21.5	N-methylpyridinium	HEK293-OCT2	Amphoux, 2006
Monocrotaline	1852.6		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Chen, 2019
N-butyl-N-methylpyrrolidinium chloride (BmPy-Cl)	0.48		Tetraethylammonium¹	CHO-OCT2	Cheng, 2011
N-butylpyridinium chloride (NBuPy-Cl)	2.29		Tetraethylammonium¹	CHO-OCT2	Cheng, 2011
N-methylpyridinium		2.4	Tetraethylammonium¹	OCT2-expressing oocytes	Gorboulev, 1997
N-methylpyridinium	4.42		YM155	HEK293-OCT2	Minematsu, 2010
Naloxone	235.7		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Naloxone	20.3		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Naloxone	29.5		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Naloxone	55.1		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Naloxone	67.3		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
NBD-MTMA	46		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Nicotine	52.8	57.7	Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Nifekalant	10.3		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Olaparib	19.9		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	McCormick, 2017
Omeprazole	6.7		Metformin^1,3	HEK293-OCT2	Nies, 2011
Omeprazole	5.53		Para-Aminosalicylic acid (PAS)	HEK293-OCT2	Parvez, 2017
Ondansetron	1.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Ondansetron		85	Metformin^1,3	HEK293-OCT2	Li, 2013
P-hydroxymethamphetamine (P-OHMA)	83.8		Metformin^1,3	HEK293-OCT2	Wagner, 2017
Pantoprazole	1.5		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Pantoprazole	2.8		Metformin^1,3	HEK293-OCT2	Nies, 2011
Pantoprazole	0.56		Metformin^1,3	HEK293-OCT2	Hacker, 2015
Para-Aminosalicylic acid (PAS)	94.2		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Parvez, 2016
Para-Aminosalicylic acid (PAS)	85.8		Metformin^1,3	HEK293-OCT2	Parvez, 2016
Pazopanib	3.5		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Sauzay, 2016
Pentamidine	1.2		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Pentamidine	10.6		N-methylpyridinium	CHO-OCT2	Ming, 2009
Phenanthriplatin	2		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Hucke, 2018
Phencyclidine		24.9	N-methylpyridinium	HEK293-OCT2	Amphoux, 2006
Phenformin		54	N-methylpyridinium	HEK293-OCT2	Umehara, 2007
Phenformin		111	Tetraethylammonium¹	HEK293-OCT2	Umehara, 2007
Phenoxybenzamine	4.9		N-methylpyridinium	HEK293-OCT2	Hayer-Zillgen, 2002
Phosmet	3.6		Dopamine	HEK293 cells	Chedik, 2019
Phosmet	7.9		Rhodamine 123	HEK293 cells	Chedik, 2019
Pilocarpine	109.3		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Pilocarpine	55.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Pilocarpine	34.5		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Pilocarpine	48.2		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Pilocarpine	61.9		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Pilsicainide	ND		Tetraethylammonium¹	OCT2-expressing oocytes	Tsuruoka, 2006
Prazosin	13.6		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Prazosin	80.4		YM155	HEK293-OCT2	Minematsu, 2010
Procainamide		50	Tetraethylammonium¹	OCT2-expressing oocytes	Gorboulev, 1997
Procainamide	91.9		YM155	HEK293-OCT2	Minematsu, 2010
Proguanil	13		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	van, 2017
Propafenone	25		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Propafenone	3.6		NBD-MTMA	CHO-OCT2	Belzer, 2013
Propamocarb	38.1		4-DiASP	HEK293 cells	Gueniche, 2020
Propranolol	71.6		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Propranolol	229		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Propranolol	67.2		NBD-MTMA	CHO-OCT2	Belzer, 2013
Pyridine	790		Tetraethylammonium¹	CHO-OCT2	Cheng, 2011
Pyrimethamine	23.6		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Shen, 2013
Pyrimethamine	1.6		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	van, 2017
Pyrimethamine	4.8		Metformin^1,3	HEK293-OCT2	Shen, 2013
Quinidine	91.6		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Quinidine	92.6		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Quinidine	91.1		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Quinidine	6.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Quinidine	6.4		Metformin^1,3	CHO-OCT2	Belzer, 2013
Quinidine	18.6		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Quinidine	8.7		N-methylpyridinium	OCT2-expressing oocytes	Bourdet, 2005
Quinidine	13.3		N-methylpyridinium	CHO-OCT2	Ming, 2009
Quinidine	87		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Quinidine	29.6		NBD-MTMA	CHO-OCT2	Belzer, 2013
Quinidine	18.7		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Quinidine	10.7		Para-Aminosalicylic acid (PAS)	HEK293-OCT2	Parvez, 2017
Quinidine	23.6		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Quinidine	11		YM155	HEK293-OCT2	Minematsu, 2010
Quinine	3.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	van, 2017
Quinine	23		N-methylpyridinium	HEK293-OCT2	Muller, 2005
Quinine		3.4	Tetraethylammonium¹	OCT2-expressing oocytes	Gorboulev, 1997
Rabeprazole	5.7		Metformin^1,3	HEK293-OCT2	Nies, 2011
Ranitidine		79	Cimetidine²	HEK293-OCT2	Tahara, 2005
Ranitidine		30.5	Famotidine	HEK293-OCT2	Tahara, 2005
Ranitidine	76		N-methylpyridinium	OCT2-expressing oocytes	Bourdet, 2005
Ranitidine	1617		N-methylpyridinium	HEK293-OCT2	Muller, 2005
Ranitidine	482		Trospium	HEK293-OCT2	Abebe, 2020
Rimantadine	4.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Ritonavir	24.8		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Rucaparib	31		Metformin^1,3	CHO-OCT2	Liao, 2020
Sibutramine	29		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Sitagliptin	7.41		Metformin^1,3	HEK293-OCT2	Hacker, 2015
Spironolactone	1.29		Metformin^1,3	HEK293-OCT2	Hacker, 2015
Tacrine	2.3		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Tacrine	0.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Tacrine	0.6		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Tacrine	1		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Tacrine	0.9		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Tamoxifen	87		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Telaprevir	6.4		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Kunze, 2012
Tenatoprazole	20.3		Metformin^1,3	HEK293-OCT2	Nies, 2011
Testosterone	3		Not applicable	N/A	Koepsell, 2007
Tetraethylammonium¹	77		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Tetraethylammonium¹	222		N-methylpyridinium	OCT2-expressing oocytes	Bourdet, 2005
Tetraethylammonium¹	189.2		N-methylpyridinium	CHO-OCT2	Ming, 2009
Tetraethylammonium¹	110		NBD-MTMA	CHO-OCT2	Belzer, 2013
Tetramethrin	11.2		Rhodamine 123	HEK293 cells	Chedik, 2017
Tetramethylammonium	301		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Tetrapentylammonium		1.5	Tetraethylammonium¹	OCT2-expressing oocytes	Gorboulev, 1997
Topotecan	61		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Tramadol	140.1		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
Triazolam	65.5		Tetraethylammonium¹	S2-OCT2	Chiba, 2013
Triethylmethylammonium	125		NBD-MTMA	CHO-OCT2	Belzer, 2013
Trimethoprim	775		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Trimethoprim	199.2		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Trimethoprim	14.1		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Trimethoprim	19.8		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Trimethoprim	1318		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Trimethoprim	113		NBD-MTMA	CHO-OCT2	Belzer, 2013
Trimethoprim	43		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Trimethoprim	50.2		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Trimipramine	0.44		Metformin^1,3	HEK293-OCT2	Hacker, 2015
Tripelennamine	12.1		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Tripelennamine	3.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Tripelennamine	2.1		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Tripelennamine	5.7		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Tripelennamine	5		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Tropicamide	691.5		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Tropicamide	141.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Tropicamide	94.3		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Tropicamide	189		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Tropicamide	205.4		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Trospium chloride	0.07		Metformin^1,3	HEK293-OCT2	Hacker, 2015
Tubocurarine	78.8		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Vandetanib	73.4		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Shen, 2013
Vandetanib	8.8		Metformin^1,3	HEK293-OCT2	Shen, 2013
Vecuronium bromide	3.5		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Veliparib	3913		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Kikuchi, 2013
Verapamil	91.9		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
Verapamil	66		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Parvez, 2016
Verapamil	49.7		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
Verapamil	4.6		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
Verapamil	20		Metformin^1,3	CHO-OCT2	Belzer, 2013
Verapamil	36		Metformin^1,3	HEK293-OCT2	Parvez, 2016
Verapamil	10.3		Metformin^1,3	CHO-OCT2	Sandoval, 2018
Verapamil	85		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
Verapamil	21		NBD-MTMA	CHO-OCT2	Belzer, 2013
Verapamil	9.7		NBD-MTMA	CHO-OCT2	Sandoval, 2018
Verapamil	21.4		Para-Aminosalicylic acid (PAS)	HEK293-OCT2	Parvez, 2017
Verapamil	17.8		Tetraethylammonium¹	CHO-OCT2	Sandoval, 2018
Verapamil	13.4		YM155	HEK293-OCT2	Minematsu, 2010
YM155	15.9		N-methylpyridinium	HEK293-OCT2	Minematsu, 2010
Zafirlukast	9.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
Zolpidem	0.15		Metformin^1,3	HEK293-OCT2	Hacker, 2015

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	OCT2/MATEs	Abemaciclib	Metformin^1,3	1.37	1.22	0.55	ND	NS	yes	Chappell, 2019	DDI 1
2	OCTs/MATE2K	Cefiderocol	Metformin^1,3	1.05	1.09	ND	NR	0.88	ND	Katsube, 2018	DDI 2
3	OCTs/MATEs	Cetirizine	Pilsicainide	1.4	NS	ND	ND	ND	ND	Tsuruoka, 2006	DDI 3
4	OCTs/MATEs	Cimetidine²	Cephalexin	NS	NS	0.8	0.8	NS	ND	van, 1986	DDI 4
5	OCTs/MATEs	Cimetidine²	Dofetilide	1.5	1.3	0.7	0.7	1.3	yes	Abel, 2000	DDI 5
6	OCTs/MATEs	Cimetidine²	Metformin^1,3	1.5	1.7	0.7	ND	ND	ND	Somogyi, 1987	DDI 6
7	OCTs/MATEs	Cimetidine²	Pilsicainide	1.3	NS	0.7	0.7	1.2	ND	Shiga, 2000	DDI 7
8	OCTs/MATEs	Cimetidine²	Pindolol (S-enantiomer)	1.4	1.3	0.7	ND	NS	ND	Somogyi, 1992	DDI 8
9	OCTs/MATEs	Cimetidine²	Procainamide	1.4	NS	0.6	ND	1.3	ND	Somogyi, 1983	DDI 9
10	OCTs/MATEs	Cimetidine²	Ranitidine	1.3	NS	0.7	ND	1.3	ND	van, 1986	DDI 10
11	OCTs/MATEs	Cimetidine²	Varenicline	1.3	ND	0.8	0.8	ND	ND	Feng, 2008	DDI 11
12	OATs/OCTs	Cotrimoxazole (trimethoprim/sulfamethoxazole)	Apricitabine	1.7	1.3	0.6	0.6	1.4	ND	Shiveley, 2008	DDI 12
13	OATs/OCTs	Cotrimoxazole (trimethoprim/sulfamethoxazole)	Zidovudine	NS	ND	0.4	NS	NS	ND	Chatton, 1992	DDI 13
14	OCTs/MATEs	Isavuconazole	Metformin^1,3	1.52	1.22	ND	0.66	1.14	ND	Yamazaki, 2017	DDI 14
15	OCTs/MATEs	Plazomicin	Metformin^1,3	1.04	1.1	0.99	0.97	0.92		Choi, 2019	DDI 15
16	OCTs/MATEs	Ranitidine	Trospium (IV)	1.06	1.10	0.87	1.1	1.00	No	Abebe, 2020	DDI 16
17	OCTs/MATEs	Ranitidine	Trospium (oral)	0.87	0.92	0.99	NR	0.98	No	Abebe, 2020	DDI 17
18	OCTs/MATEs	Test cocktail 1: digoxin, furosemide, metformin, and rosuvastatin	Metformin^1,3	0.99	1.1					Stopfer, 2016	DDI 18
19	OCTs/MATEs	Test cocktail 3: digoxin, metformin, rosuvastatin, and increased furosemide	Metformin^1,3	1.03	1.03					Stopfer, 2016	DDI 19
20	OCTs	Trimethoprim	Zidovudine	NS	ND	0.5	NS	NS	ND	Chatton, 1992	DDI 20

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