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SLC22A1

Synonyms: HOCT1, OCT1, oct1_cds

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Orthologs in other species

rat Slc22a1

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    0.0000706
Kidney Nishimura    0.00389
Liver* Nishimura 2.230
Placenta Nishimura    0.0000830
Small Intestine* Nishimura    0.0000241
Kidney Mean across all PMT Samples    0.876
Liver* Mean across all PMT Samples 322.166
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
1-methyl-4-phenylpyridinium (MPP+) 14.6 OCT1-expressing oocytes Zhang, 1997
1-methyl-4-phenylpyridinium (MPP+) 6.38 MDCK-OCT1 Tu, 2013
1-methyl-4-phenylpyridinium (MPP+) 35 HEK293-OCT1 Boxberger, 2014
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) 2.32 HEK293-OCT1 Ahlin, 2008
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) 9.21 HEK293-OCT1 Ahlin, 2010
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) 21.1 HEK293-OCT1 Chen, 2017
Acyclovir 151.2 S2-OCT1 Takeda, 2002
Amisulpride 31 HEK293-OCT1 Dos, 2014
Atropine 5.9 HEK293-OCT1 Chen, 2017
Berberine 14.8 MDCK-OCT1 Nies, 2008
Butylscopolamine 23 HEK293-OCT1 Chen, 2017
Cycloguanil 18.3 HEK293-OCT1 Matthaei, 2019
DAPI 8.94 MDCKII-OCT1 Yasujima, 2011
Ethambutol 526 HEK293-OCT1 Parvez, 2018
Ethidium 0.8 CHO-OCT1 Lee, 2009
Fenoterol 1.78 HEK293-OCT1 Matthaei, 2016
Furamidine 6.1 CHO-OCT1 Ming, 2009
Ganciclovir 516.2 S2-OCT1 Takeda, 2002
Ipratropium 9 HEK293-OCT1 Hendrickx, 2013
Ipratropium 9 HEK293-OCT1 Hendrickx, 2013
Ipratropium 14 HEK293-OCT1 Chen, 2017
Lamivudine 249 HEK293-OCT1 Jung, 2008
Lamivudine 1250 CHO-OCT1 Minuesa, 2009
Metformin 1470 HEK293-OCT1 Kimura, 2005
Metformin 1060 HEK293-OCT1 Choi, 2007
Metformin 2160 CHO-OCT1 Nies, 2009
Metformin 5450 HEK293-OCT1 Ahlin, 2010
Metformin 5422 Caco-OCT1 Elsby, 2017
Monocrotaline 25 MDCK-OCT1 Tu, 2013
Morphine 3.4 HEK293-OCT1 Tzvetkov, 2013
N-methylpyridinium 21 MDCK II-OCT1 Bachmakov, 2008
O-desmethyltramadol 149 HEK293-OCT1 Tzvetkov, 2011
Oxaliplatin ND MDCK-OCT1 Zhang, 2006
Oxibutynin 8.8 HEK293-OCT1 Wenge, 2011
Pentamidine 36.4 CHO-OCT1 Ming, 2009
Proguanil 8.1 HEK293-OCT1 van, 2017
Proguanil 17.7 HEK293-OCT1 Matthaei, 2019
Prostaglandin E2 0.657 S2-OCT1 Kimura, 2002
Prostaglandin F2-alpha 0.477 S2-OCT1 Kimura, 2002
Prothionamide 806 HEK293-OCT1 Parvez, 2018
Ranitidine 70 OCT1-expressing oocytes Bourdet, 2005
Ranitidine 62.9 HEK293-OCT1 Meyer, 2017
Rhodamine 123 0.54 HEK293-OCT1 Jouan, 2014
Serotonin 197 HEK293-OCT1 Boxberger, 2014
Sulpiride 259.7 HEK293-OCT1 Dos, 2014
Sulpiride 2.6 HEK293-OCT1 Takano, 2017
Sumatriptan 55.4 HEK293-OCT1 Matthaei, 2016
Tetraethylammonium 229 HeLa-OCT1 Zhang, 1998
Tetraethylammonium 566 S2-OCT1 Iwai, 2009
Tetraethylammonium 140 HEK293-OCT1 Hendrickx, 2013
Thiamine 780 HEK293-OCT1 Chen, 2014
Trospium 17 HEK293-OCT1 Wenge, 2011
Trospium 106 HEK293-OCT1 Bexten, 2015
Trospium 15 HEK293-OCT1 Chen, 2017
YM155 22.1 HEK293-OCT1 Minematsu, 2010
Zalcitabine 242 HEK293-OCT1 Jung, 2008

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022


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In Vitro Inhibitors

Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
(-)-Zearalenone 0.62 Tetraethylammonium S2 cells Tachampa, 2008
1-methyl-4-phenylpyridinium (MPP+) 390 Ethidium CHO-OCT1 Lee, 2009
17beta-estradiol 5.73 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hayer-Zillgen, 2002
3,4-methylenedioxymetamphetamine (MDMA) 24.2 N-methylpyridinium HEK293-OCT1 Amphoux, 2006
Abacavir 0.00007 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT1 Minuesa, 2009
Acetylcholine 580 1-methyl-4-phenylpyridinium (MPP+) OCT1-expressing oocytes Lips, 2005
Afatinib 80 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Aflatoxin B1 103 Tetraethylammonium S2 cells Tachampa, 2008
Alfuzosin 14.87 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Allethrin 2.6 4',6'-diamidino-2-phenylindole HEK293 cells Chedik, 2017
Alpha-zearalenol 64.4 Tetraethylammonium S2 cells Tachampa, 2008
Amantadine 236 N-methylpyridinium HEK293-OCT1 Amphoux, 2006
Amantadine 18.4 Tetraethylammonium HeLa-OCT1 Bednarczyk, 2003
Amantadine 39.6 YM155 HEK293-OCT1 Minematsu, 2010
Amascrine 5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Amiloride 57 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Amitriptyline 16.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Amitriptyline 6.99 Metformin HEK293-OCT1 Ahlin, 2010
Amitriptyline 4.4 Morphine HEK293-OCT1 Tzvetkov, 2013
Amitriptyline 1.89 Morphine HEK293-OCT1 Zhu, 2018
Amitriptyline 58.1 Rhodamine 123 HEK293-OCT1 Jouan, 2014
Amitriptyline 3.47 Sumatriptan HEK293-OCT1 Matthaei, 2016
Amphetamine 97 Metformin HEK293-OCT1 Wagner, 2017
Artemisinin 4.2 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Hubeny, 2016
Atropine 3 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Chen, 2017
Atropine 12.2 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Atropine 1.2 N-methylpyridinium HEK293-OCT1 Muller, 2005
Baricitinib 22.9 Metformin HEK293-OCT1 Yee, 2021
Bisphenol A 39 Tetraethylammonium HEK293 cells Bruyere, 2017
Bithionol 2.23 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Bosutinib 2.06 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Bucindolol 27 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Bucindolol 15.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Butylscopolamine 28 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Chen, 2017
Butylscopolamine 16 N-methylpyridinium HEK293-OCT1 Muller, 2005
Camostat 20.3 Metformin HEK293-OCT1 Yee, 2021
Camylofine 9.12 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Carbetapentane 1.55 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Carvedilol 1.4 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Carvedilol 3.43 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Cediranib 54 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Chloroquine 12.8 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hubeny, 2016
Chloroquine 10.7 Metformin HEK293-OCT1 Yee, 2021
Chlorpromazine 27 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Chlorpromazine 52.3 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Chlorpromazine 4.3 Tetraethylammonium HeLa-OCT1 Bednarczyk, 2003
Cimetidine >100 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Kido, 2011
Cimetidine 2830 Ethidium CHO-OCT1 Lee, 2009
Cimetidine 275 Metformin Caco-OCT1 Elsby, 2017
Cimetidine 149 YM155 HEK293-OCT1 Minematsu, 2010
Citalopram 18.8 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Citreoviridin A 1.7 Tetraethylammonium S2 cells Tachampa, 2008
Clemastine 4.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Clomipramine 19.3 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Clomipramine 5 Morphine HEK293-OCT1 Tzvetkov, 2013
Clonidine 22.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Clonidine 18.98 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Clonidine 6.5 N-methylpyridinium HEK293-OCT1 Muller, 2005
Clonidine 0.55 Tetraethylammonium HeLa-OCT1 Zhang, 1998
Clonidine 0.71 Tetraethylammonium HeLa-OCT1 Bednarczyk, 2003
Cloperastine 14.89 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Closantel 3 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Clotrimazole 11.97 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Cocaine 85 N-methylpyridinium HEK293-OCT1 Amphoux, 2006
Codeine 11 Morphine HEK293-OCT1 Tzvetkov, 2013
Colchicine 29.7 Metformin HEK293-OCT1 Yee, 2021
Corticosterone 21.7 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hayer-Zillgen, 2002
Corticosterone 8.89 YM155 HEK293-OCT1 Minematsu, 2010
Cyclopiazonic acid 6.63 Tetraethylammonium S2 cells Tachampa, 2008
D-amphetamine 202 N-methylpyridinium HEK293-OCT1 Amphoux, 2006
D-tetrahydropalmatine 13.9 Monocrotaline MDCK-OCT1 Tu, 2013
Darunavir 6 Metformin HEK293-OCT1 Yee, 2021
Darunavir 16 Tetraethylammonium KCL22-OCT1 Moss, 2015
Dasatinib 1.07 Metformin HEK293-OCT1 Minematsu, 2011
Decynium-22 0.98 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hayer-Zillgen, 2002
Decynium-22 2.73 Tetraethylammonium HeLa-OCT1 Zhang, 1998
Decynium-22 21.9 Tetraethylammonium OCT1-expressing oocytes Okuda, 1999
Desipramine 56.8 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Desipramine 43.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Desipramine 9.18 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Dextromethorphan 10.45 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Dichlorophene 8.41 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Diltiazem 15.8 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Umehara, 2008
Diltiazem 1.7 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Diltiazem 12.4 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Diphenhydramine 3.4 N-methylpyridinium HEK293-OCT1 Muller, 2005
Diphenhydramine 4.1 Serotonin HEK293-OCT1 Boxberger, 2014
Dipyridamole 81 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Kido, 2011
Disopyramide 81.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Disopyramide >100 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Kido, 2011
Dobutamine 4.17 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Domperidone 32.8 Sumatriptan HEK293-OCT1 Matthaei, 2016
Doxazosin 14.8 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Doxepin 11.19 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Efavirenz 7.4 Tetraethylammonium KCL22-OCT1 Moss, 2015
Eletriptan 6.8 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Matthaei, 2016
Emtricitabine 0.00002 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT1 Minuesa, 2009
Erlotinib 86 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Erlotinib 16.24 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Erlotinib 0.356 Metformin HEK293-OCT1 Minematsu, 2011
Ethambutol >100 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Parvez, 2016
Ethopropazine 20.46 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Etilefrine 447 N-methylpyridinium HEK293-OCT1 Muller, 2005
Famotidine >300 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Famotidine 28 N-methylpyridinium OCT1-expressing oocytes Bourdet, 2005
Fenamiphos 27.5 4',6'-diamidino-2-phenylindole HEK293 cells Chedik, 2019
Fenamiphos 9.2 Dopamine HEK293 cells Chedik, 2019
Flecainide 41.5 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Umehara, 2008
Flecainide 2.5 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Fluoxetine 6 Morphine HEK293-OCT1 Tzvetkov, 2013
Fluoxetine 9.1 Morphine HEK293-OCT1 Zhu, 2018
Fluoxetine 6.2 Serotonin HEK293-OCT1 Boxberger, 2014
Foretinib 74 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Furamidine 7.4 N-methylpyridinium CHO-OCT1 Ming, 2009
Gefitinib 57 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Gefitinib 1.07 Metformin HEK293-OCT1 Minematsu, 2011
Glyburide 199 Metformin HEK293-OCT1 Ahlin, 2010
Griseofulvin 7.3 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Guanabenz 4.85 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Homatropine 4 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Chen, 2017
Hydroxychloroquine 20 Metformin HEK293-OCT1 Yee, 2021
Imatinib 107 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Imatinib 5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Schmidt-Lauber, 2012
Imatinib 1.47 Metformin HEK293-OCT1 Minematsu, 2011
Imatinib 10.2 Serotonin HEK293-OCT1 Boxberger, 2014
Imipramine 17.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Imipramine 7.95 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Imipramine 6.2 Morphine HEK293-OCT1 Tzvetkov, 2013
Imipramine 4.03 Morphine HEK293-OCT1 Zhu, 2018
Indinavir 37 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Jung, 2008
Indinavir 208 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Indinavir 61.7 Tetraethylammonium HeLa-OCT1 Zhang, 2000
Ipratropium 17 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Chen, 2017
Irinotecan 20.8 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Irinotecan 1.5 Morphine HEK293-OCT1 Tzvetkov, 2013
Irinotecan 1.4 Morphine HEK293-OCT1 Zhu, 2018
Ketamine 114.5 N-methylpyridinium HEK293-OCT1 Amphoux, 2006
Ketoconazole 7.4 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Ketoconazole 2.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Lamivudine 17 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Jung, 2008
Lansoprazole 35.8 Metformin HEK293-OCT1 Nies, 2011
Lapatinib 96 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Lapatinib >30 Metformin HEK293-OCT1 Minematsu, 2011
Levofloxacin 30.3 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Parvez, 2016
Levofloxacin 22.6 Metformin HEK293-OCT1 Parvez, 2016
Mefloquine 6.6 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Hubeny, 2016
Memantine 27 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Memantine 3.7 N-methylpyridinium HEK293-OCT1 Amphoux, 2006
Metformin 3420 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT1 Nies, 2009
Metformin 1231 N-methylpyridinium OCT1-expressing oocytes Bourdet, 2005
Metformin 493 N-methylpyridinium HEK293-OCT1 Umehara, 2007
Metformin 2820 Tetraethylammonium HEK293-OCT1 Umehara, 2007
Methamphetamine 21.1 Metformin HEK293-OCT1 Wagner, 2017
Methoclopramide 95 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Metoclopramide 15.9 Sumatriptan HEK293-OCT1 Matthaei, 2016
Metoprolol 268 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Umehara, 2008
Metoprolol 52.6 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Midazolam 3.7 Tetraethylammonium HeLa-OCT1 Zhang, 1998
Mitoxantrone 43.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
MK-801 80.5 N-methylpyridinium HEK293-OCT1 Amphoux, 2006
Morphine 4.2 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Tzvetkov, 2013
Morphine 28 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
N-desmethyl imatinib 1.76 Metformin HEK293-OCT1 Minematsu, 2011
N-methylpyridinium 30.4 YM155 HEK293-OCT1 Minematsu, 2010
Naratriptan 25 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Matthaei, 2016
Nelfinavir 7 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Jung, 2008
Nelfinavir 21.8 Tetraethylammonium HeLa-OCT1 Zhang, 2000
Neratinib 77 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Nifedipine 31.1 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Nifekalant >300 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Nilotinib 91 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Nilotinib 2.92 Metformin HEK293-OCT1 Minematsu, 2011
Nitroprusside 43.84 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
O-desmethyl erlotinib 3.62 Metformin HEK293-OCT1 Minematsu, 2011
O-desmethyl gefitinib 2.19 Metformin HEK293-OCT1 Minematsu, 2011
O-methylisoprenaline >100 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hayer-Zillgen, 2002
Omeprazole 15.7 Metformin HEK293-OCT1 Nies, 2011
Ondansetron 63 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Tzvetkov, 2012
Ondansetron >300 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Ondansetron 1.2 Morphine HEK293-OCT1 Tzvetkov, 2013
Ondansetron 0.3 Morphine HEK293-OCT1 Zhu, 2018
Orphenadrine 12.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Orphenadrine >100 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Kido, 2011
Oxibutynin 20 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Wenge, 2011
Oxprenolol 87.3 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Umehara, 2008
Pantoprazole >500 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Pantoprazole 30.8 Metformin HEK293-OCT1 Nies, 2011
Para-hydroxymethamphetamine 12 Metformin HEK293-OCT1 Wagner, 2017
Pelitinib 76 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Pentamidine 0.4 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Jung, 2008
Pentamidine 22.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Pentamidine 16.4 N-methylpyridinium CHO-OCT1 Ming, 2009
Phencyclidine 4.4 N-methylpyridinium HEK293-OCT1 Amphoux, 2006
Phenformin 13 N-methylpyridinium HEK293-OCT1 Umehara, 2007
Phenformin 23 Tetraethylammonium HEK293-OCT1 Umehara, 2007
Phenoxybenzamine 2.72 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hayer-Zillgen, 2002
Phenoxybenzamine 15.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Phosmet 10.4 4',6'-diamidino-2-phenylindole HEK293 cells Chedik, 2019
Phosmet 7.1 Dopamine HEK293 cells Chedik, 2019
Piclidenoson 16.5 Metformin HEK293-OCT1 Yee, 2021
Pindolol 39.1 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Umehara, 2008
Pindolol 9.7 Tetraethylammonium HeLa-OCT1 Bednarczyk, 2003
Pioglitazone 185 Metformin HEK293-OCT1 Ahlin, 2010
Prazosin 1.84 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hayer-Zillgen, 2002
Prazosin 9.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Prazosin 50.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Prazosin 1.8 Metformin HEK293-OCT1 Yee, 2021
Prazosin 2.3 Tetraethylammonium KCL22-OCT1 Moss, 2015
Prazosin 1.56 YM155 HEK293-OCT1 Minematsu, 2010
Procainamide 14.5 Tetraethylammonium HeLa-OCT1 Bednarczyk, 2003
Procainamide 51.3 YM155 HEK293-OCT1 Minematsu, 2010
Prochlorperazine 49.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Progesterone 3.05 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hayer-Zillgen, 2002
Promazine 17.2 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Propafenone 1 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Propafenone 14.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Propafenone 15.54 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Propamocarb 48.1 Tetraethylammonium HEK293 cells Gueniche, 2020
Propranolol 113 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Umehara, 2008
Propranolol 1.3 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Propranolol 6.2 Sumatriptan HEK293-OCT1 Matthaei, 2016
Pyrazinamide 36.5 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Parvez, 2016
Pyrazinamide 25.8 Metformin HEK293-OCT1 Parvez, 2016
Pyrimethamine 8.5 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Hubeny, 2016
Pyrimethamine 13.57 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Pyrimethamine 4.46 Metformin Caco-OCT1 Elsby, 2017
Quinidine 16.8 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Umehara, 2008
Quinidine 340 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Quinidine 3.58 Monocrotaline MDCK-OCT1 Tu, 2013
Quinidine 6.7 N-methylpyridinium OCT1-expressing oocytes Bourdet, 2005
Quinidine 5.7 N-methylpyridinium CHO-OCT1 Ming, 2009
Quinidine 17.5 Tetraethylammonium HeLa-OCT1 Zhang, 1998
Quinidine 5.4 Tetraethylammonium HeLa-OCT1 Bednarczyk, 2003
Quinidine 7.11 YM155 HEK293-OCT1 Minematsu, 2010
Quinine 3.5 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Hubeny, 2016
Quinine 51.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Quinine 70 Ethidium CHO-OCT1 Lee, 2009
Quinine 13 N-methylpyridinium HEK293-OCT1 Muller, 2005
Quinine 22.9 Tetraethylammonium HeLa-OCT1 Zhang, 1998
R-(-)-disopyramide 15.4 Tetraethylammonium HeLa-OCT1 Zhang, 1998
Rabeprazole 3 Metformin HEK293-OCT1 Nies, 2011
Ranitidine 81.91 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Meyer, 2017
Ranitidine 336.59 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Meyer, 2017
Ranitidine 20.93 Metformin HEK293-OCT1 Meyer, 2017
Ranitidine 45.5 Morphine HEK293-OCT1 Meyer, 2017
Ranitidine 33 N-methylpyridinium OCT1-expressing oocytes Bourdet, 2005
Ranitidine 28 N-methylpyridinium HEK293-OCT1 Muller, 2005
Ranitidine 21.7 Tetraethylammonium HeLa-OCT1 Bednarczyk, 2003
Remdesivir 10.1 Metformin HEK293-OCT1 Yee, 2021
Repaglinide 9.2 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Repaglinide 1.6 Metformin MDCK II-OCT1 Bachmakov, 2008
Repaglinide 1.8 N-methylpyridinium MDCK II-OCT1 Bachmakov, 2008
Rhodamine 123 0.37 Tetraethylammonium HEK293-OCT1 Jouan, 2014
Rifabutin 42.7 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Parvez, 2016
Rifabutin 38.7 Metformin HEK293-OCT1 Parvez, 2016
Ritonavir 33.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
Ritonavir 3.8 Metformin HEK293-OCT1 Yee, 2021
Ritonavir 14 N-methylpyridinium HEK293-OCT1 Jung, 2008
Ritonavir 5.18 Tetraethylammonium HeLa-OCT1 Zhang, 2000
Rizatriptan 41 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Matthaei, 2016
Rosiglitazone 6.9 Metformin MDCK II-OCT1 Bachmakov, 2008
Rosiglitazone 30.4 N-methylpyridinium MDCK II-OCT1 Bachmakov, 2008
Ruxolitinib 9.7 Metformin HEK293-OCT1 Yee, 2021
S-(+)-disopyramide 29.9 Tetraethylammonium HeLa-OCT1 Zhang, 1998
Saquinavir 37 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Jung, 2008
Saquinavir 8.26 Tetraethylammonium HeLa-OCT1 Zhang, 2000
Saracatinib 57 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Harrach, 2017
Scopolamine 6.7 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Chen, 2017
Sildenafil 19.8 Metformin HEK293-OCT1 Yee, 2021
Simvastatin 89 Metformin HEK293-OCT1 Ahlin, 2010
SKF550 >0.3 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Hayer-Zillgen, 2002
Sorafenib 99 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Sorafenib >30 Metformin HEK293-OCT1 Minematsu, 2011
Spironolactone 1.2 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Spironolactone 3.08 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2010
Sulpiride 182 Tetraethylammonium HEK293-OCT1 Takano, 2017
Sumatriptan 47 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Matthaei, 2016
Sunitinib 67 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Sunitinib 6.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Sunitinib 0.33 Metformin HEK293-OCT1 Minematsu, 2011
Tacrine 83 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Kido, 2011
Tacrine 21.72 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Talinolol 23.7 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Tenatoprazole 23.3 Metformin HEK293-OCT1 Nies, 2011
Tenofovir 0.0009 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT1 Minuesa, 2009
Tenofovir >10 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Shen, 2017
Terazosine 23.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Tetrabromobisphenol A 37.5 Tetraethylammonium HEK293 cells Bruyere, 2017
Tetraethylammonium 7410 Ethidium CHO-OCT1 Lee, 2009
Tetraethylammonium 158 N-methylpyridinium OCT1-expressing oocytes Dresser, 2000
Tetraethylammonium 216 N-methylpyridinium OCT1-expressing oocytes Bourdet, 2005
Tetraethylammonium 469.7 N-methylpyridinium CHO-OCT1 Ming, 2009
Tetraethylammonium 167 Tetraethylammonium OCT1-expressing oocytes Okuda, 1999
Tetramethrin 4.9 4',6'-diamidino-2-phenylindole HEK293 cells Chedik, 2017
Thiamine 4354 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Tofacitinib 41.4 Metformin HEK293-OCT1 Yee, 2021
Trimethoprim 20 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Jung, 2008
Trimethoprim 56.8 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Trimethoprim 50.68 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
Trimethoprim 27.7 Metformin Caco-OCT1 Elsby, 2017
Trimipramine 28 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
Tropisetron 8.5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Tzvetkov, 2012
Tropisetron 3.3 Morphine HEK293-OCT1 Tzvetkov, 2013
Trospium 18.1 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Wenge, 2011
Trospium 15 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Chen, 2017
Tubocurarine 62.4 YM155 HEK293-OCT1 Minematsu, 2010
Umifenovir 1.2 Metformin HEK293-OCT1 Yee, 2021
Vandetanib 68 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
Verapamil 1.2 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Grube, 2011
Verapamil 1.1 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Parvez, 2016
Verapamil 12 Ethambutol HEK293-OCT1 Parvez, 2018
Verapamil 0.62 Metformin HEK293-OCT1 Ahlin, 2010
Verapamil 0.8 Metformin HEK293-OCT1 Parvez, 2016
Verapamil 1.6 Morphine HEK293-OCT1 Tzvetkov, 2013
Verapamil 9.62 Morphine HEK293-OCT1 Zhu, 2018
Verapamil 3.9 Prothionamide HEK293-OCT1 Parvez, 2018
Verapamil 33.2 Rhodamine 123 HEK293-OCT1 Jouan, 2014
Verapamil 1.5 Serotonin HEK293-OCT1 Boxberger, 2014
Verapamil (Racemic) 2.9 Tetraethylammonium HeLa-OCT1 Zhang, 1998
Verapamil (Racemic) 1.23 YM155 HEK293-OCT1 Minematsu, 2010
YM155 23.8 N-methylpyridinium HEK293-OCT1 Minematsu, 2010
YM758 40.5 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Umehara, 2008
Zalcitabine 24 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Jung, 2008
Zidovudine 0.0002 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT1 Minuesa, 2009
Zolmitriptan >1000 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Matthaei, 2016

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022


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Clinical Drug-Drug Interactions

DDI Implicated Transporter Interacting Drug Affected Drug AUC Cmax CLR CL/F t1/2 Effect on PD Reference More Details
Clinical PK Impact(fold change)
1 OCTs/MATE2K Cefiderocol Metformin 1.05 1.09 ND NR 0.88 ND Katsube, 2018 DDI 1
2 OCTs/MATEs Cetirizine Pilsicainide 1.4 NS ND ND ND ND Tsuruoka, 2006 DDI 2
3 OCTs/MATEs Cimetidine Cephalexin NS NS 0.8 0.8 NS ND van, 1986 DDI 3
4 OCTs/MATEs Cimetidine Dofetilide 1.5 1.3 0.7 0.7 1.3 yes Abel, 2000 DDI 4
5 OCTs/MATEs Cimetidine Metformin 1.5 1.7 0.7 ND ND ND Somogyi, 1987 DDI 5
6 OCTs/MATEs Cimetidine Pilsicainide 1.3 NS 0.7 0.7 1.2 ND Shiga, 2000 DDI 6
7 OCTs/MATEs Cimetidine Pindolol (S-enantiomer) 1.4 1.3 0.7 ND NS ND Somogyi, 1992 DDI 7
8 OCTs/MATEs Cimetidine Procainamide 1.4 NS 0.6 ND 1.3 ND Somogyi, 1983 DDI 8
9 OCTs/MATEs Cimetidine Ranitidine 1.3 NS 0.7 ND 1.3 ND van, 1986 DDI 9
10 OCTs/MATEs Cimetidine Varenicline 1.3 ND 0.8 0.8 ND ND Feng, 2008 DDI 10
11 OATs/OCTs Cotrimoxazole (trimethoprim/sulfamethoxazole) Apricitabine 1.7 1.3 0.6 0.6 1.4 ND Shiveley, 2008 DDI 11
12 OATs/OCTs Cotrimoxazole (trimethoprim/sulfamethoxazole) Zidovudine NS ND 0.4 NS NS ND Chatton, 1992 DDI 12
13 OCTs/MATEs Isavuconazole Metformin 1.52 1.22 ND 0.66 1.14 ND Yamazaki, 2017 DDI 13
14 OCTs/MATEs Ranitidine Trospium (IV) 1.06 1.10 0.87 1.1 1.00 No Abebe, 2020 DDI 14
15 OCTs/MATEs Ranitidine Trospium (oral) 0.87 0.92 0.99 NR 0.98 No Abebe, 2020 DDI 15
16 OCTs Rifampin Metformin 1.13 1.10 1.16 NR 0.92 Yes Cho, 2011 DDI 16
17 OCT1 St John's wort Metformin 1.03 1.04 0.97 1.01 0.89 Yes Stage, 2015 DDI 17
18 OCTs Trimethoprim Zidovudine NS ND 0.5 NS NS ND Chatton, 1992 DDI 18
19 OCT1/MATEs Verapamil Metformin 1.07 1.09 0.98 NR 0.80 Yes Cho, 2014 DDI 19

The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022


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