TABLE 9 Drugs that have been shown to inhibit human organic cation transporters and have not been tested for transport or could not be identified as substrate (only drugs for which an IC50 value <20 µM was determined for at least one OCT are indicated)
Charge of major microspecies at pH 7.4 was calculated with program MarvinSketch of ChemAxon. Abacavir: Minuesa et al., 2009, abemaciclib: Chappell et al., 2019, adapalene: Kido et al., 2011, alfuzosin: Chen et al., 2017a, amitriptyline: Sata et al., 2005; Ahlin et al., 2008; Zolk et al., 2009b; Belzer et al., 2013; Tzvetkov et al., 2013; Jouan et al., 2014; Hacker et al., 2015; Matthaei et al., 2016; Sandoval et al., 2018; Zhu et al., 2018, amadiaquine: van der Velden et al., 2017, D- amphetamine: Amphoux et al., 2006, amsacrine: Ahlin et al., 2008, artemisin: Hubeny et al., 2016, atomoxetine: Sandoval et al., 2018, azidothymidine: Minuesa et al., 2009, beclomethasone: Lips et al., 2005, benzethonium: Kido et al., 2011, benztropine: Sandoval et al., 2018, bithionol: Kido et al., 2011; Wittwer et al., 2013; Chen et al., 2017a, bosutinib: Johnston et al., 2014, bucindolol: Ahlin et al., 2008, 2011, budesonide: Lips et al., 2005, buflomedil: Kido et al., 2011; Hendrickx et al., 2013, buspirone: Wittwer et al., 2013, Sandoval et al., 2018, bisoprolol: Bachmakov et al., 2009, camylofine: Chen et al., 2017a, carbetapentane: Chen et al., 2017a, carvedilol: Bachmakov et al., 2009; Zolk et al., 2009b; Grube et al., 2011; Belzer et al., 2013; Yin et al., 2016; Chen et al., 2017a, clemastine: Ahlin et al., 2008, clomacran: Kido et al., 2011, chlorhexidine: Wittwer et al., 2013, cediranib: Johnston et al., 2014, chlorphenesin: Kido et al., 2011, chlorpromazine: Bednarczyk et al., 2003; Ahlin et al., 2008, 2011; Zolk et al., 2009a; Belzer et al., 2013, citalopram: Ahlin et al., 2008; Koepsell et al., unpublished data, clomipramine: Ahlin et al., 2008; Hendrickx et al., 2013, clonidine: Zhang et al., 1998; Wu et al., 2000; Müller et al., 2005; Suhre et al., 2005; Ahlin et al., 2008; Zolk et al., 2009a; Astorga et al., 2012; Belzer et al., 2013; Hendrickx et al., 2013; Tzvetkov et al., 2013; Chen et al., 2017a, closantel: Chen et al., 2017a, clotrimazole: Chen et al., 2017a, clozapine: Hendrickx et al., 2013; Wang et al., 2019, codeine: Tzvetkov et al., 2013, darunavir: Moss et al., 2015, dasatinib: Minematsu and Giacomini, 2011, des-fluoro(6)-quinolone: Okuda et al., 2006; Imamura et al., 2011; dextromethorphan: Chen et al., 2017a, dichlorophene: Chen et al., 2017a, desipramine: Gorboulev et al., 1997; Zhang et al., 1998; Wu et al., 2000; Ahlin et al., 2008, 2011; Tsuda et al., 2009b; Zolk et al., 2009b; Chen et al., 2017a, desloratadine: Zolk et al., 2009b, dicyclomine: Kido et al., 2011, dipyramidole: Kido et al., 2011, dobutamine: Chen et al., 2017a, dolutegravir: Reese et al., 2013; Lepist et al., 2014, domperidone: Wittwer et al., 2013, donepezil: Martínez-Guerrero et al., 2016; Matthaei et al., 2016, desloratadine: Zolk et al., 2009b, dihydroergotamine: Wittwer et al., 2013, doxazosin: Ahlin et al., 2011, doxepin: Zolk et al., 2009b; Belzer et al., 2013; Hacker et al., 2015; Chen et al., 2017a, eletriptan: Matthaei et al., 2016, epinastine: Wittwer et al., 2013, erlotinib: Minematsu and Giacomini, 2011; Chen et al., 2017a, esmolol: Martínez-Guerrero et al., 2016, ethinylestradiol: Wittwer et al., 2013, ethylacridinium: Belzer et al., 2013, exemestane: Kido et al., 2011, fenfluramine: Zolk et al., 2009a, flecainide: Umehara et al., 2008; Zolk et al., 2009b; Grube et al., 2011; Belzer et al., 2013, flurazepam: Zolk et al., 2009a,b, gabexate: Kido et al., 2011; Wittwer et al., 2013, gefitinib: Galetti et al., 2010; Minematsu and Giacomini, 2011, gentian violet: Kido et al., 2011, granisetron: Wittwer et al., 2013, griseofulvin: Chen et al., 2017a, guanabenz: Kido et al., 2011; Chen et al., 2017a, guanfacine: Astorga et al., 2012, imipramine: Wu et al., 2000; Ahlin et al., 2008; Tsuda et al., 2009b; Zolk et al., 2009b; Kido et al., 2011; Belzer et al., 2013; Hendrickx et al., 2013; Tzvetkov et al., 2013; Sandoval et al., 2018; Zhu et al., 2018, imiquimod: Astorga et al., 2012, indinavir: Zhang et al., 2000; Jung et al., 2008; Wittwer et al., 2013, irinotecan: Tzvetkov et al., 2013; Wittwer et al., 2013; Sandoval et al., 2018; Zhu et al., 2018, jatrorrhizine: Sun et al., 2019, ketoconazole: Ahlin et al., 2011; Astorga et al., 2012; Chen et al., 2017a, ketotifen: Martínez-Guerrero et al., 2016, lansoprazole: Nies et al., 2011a; Hacker et al., 2015, leukomycin: Wittwer et al., 2013, mebeverine: Kido et al., 2011, 3,4-methylenedioxymethamphetamine: Amphoux et al., 2006, mexiletine: Zolk et al., 2009b; Sandoval et al., 2018, mefloquine: Hubeny et al., 2016, midazolam: Zhang et al., 1998, mitoxantrone: Meyer zu Schwabedissen et al., 2010; Wittwer et al., 2013, nelfinavir: Zhang et al., 2000; Jung et al., 2008, nifekalant: Wittwer et al., 2013, nilotinib: Minematsu and Giacomini, 2011, ondansetron: Kido et al., 2011; Tzvetkov et al., 2012, 2013; Wittwer et al., 2013; Lechner et al., 2016; Zhu et al., 2018, oxaliplatin: Yonezawa et al., 2006; Yokoo et al., 2007, 2008; Ahlin et al., 2008, 2011; Jong et al., 2011; Sprowl et al., 2013, olanzapine: Kido et al., 2011, omeprazole: Nies et al., 2011a; Martínez-Guerrero et al., 2016, orphenadrine: Ahlin et al., 2008; Kido et al., 2011, pantoprazole: Nies et al., 2011a; Wittwer et al., 2013; Hacker et al., 2015, phenoxybenzamine: Hayer-Zillgen et al., 2002; Ahlin et al., 2008, phentoloamine: Astorga et al., 2012, phenyltoloxamine: Kido et al., 2011, phenytoin: Hasannejad et al., 2004, prochlorperazine: Ahlin et al., 2008; Hendrickx et al., 2013; Martínez-Guerrero et al., 2016, procyclidine: Kido et al., 2011, proguanil: Astorga et al., 2012; van der Velden et al., 2017, promazine: Ahlin et al., 2008, propafenone: Ahlin et al., 2008, 2011; Zolk et al., 2009b; Grube et al., 2011; Belzer et al., 2013; Hendrickx et al., 2013; Chen et al., 2017a, propantheline bromide: Kido et al., 2011, pyrimethamine: Matsushima et al., 2009; Tsuda et al., 2009b; Astorga et al., 2012; Hubeny et al., 2016; Lechner et al., 2016; Yin et al., 2016; Chen et al., 2017a; van der Velden et al., 2017, quetiapine: Wang et al., 2019, rabeprazole: Kido et al., 2011; Nies et al., 2011a, repaglinide: Ahlin et al., 2008; Bachmakov et al., 2008, rapamycin: Meyer zu Schwabedissen et al., 2010, rimantadine: Wittwer et al., 2013, ritonavir: Zhang et al., 2000; Jung et al., 2008; Meyer zu Schwabedissen et al., 2010; Wittwer et al., 2013; Lepist et al., 2014; Kikuchi et al., 2019, rosiglitazone: Bachmakov et al., 2008, saquinavir: Zhang et al., 2000; Jung et al., 2008, scopolamine: Hendrickx et al., 2013; Chen et al., 2017b, sitagliptin: Hacker et al., 2015, sparteine: Kido et al., 2011, spironolactone: Grube et al., 2006, 2011; Ahlin et al., 2011; Hacker et al., 2015, sulconazole: Kido et al., 2011, sunitinib: Minematsu and Giacomini, 2011; Chen et al., 2017a, tacrine: Kido et al., 2011; Astorga et al., 2012; Chen et al., 2017a; Sandoval et al., 2018; tenatoprazole: Nies et al., 2011a, tenofovir disoproxil: Minuesa et al., 2009; Shen et al., 2017, irtetrachlorosalicylanilide: Kido et al., 2011, tolterodine: Kido et al., 2011, tramadol: Astorga et al., 2012, trimipramine: Ahlin et al., 2008; Hacker et al., 2015, tripilenamine: Sandoval et al., 2018, tubocurarine: Wittwer et al., 2013, valspodar: Lechner et al., 2016, vecuronium: Wittwer et al., 2013, zafirlukast: Wittwer et al., 2013, ziprasidone: Wang et al., 2019, zolpidem: Hacker et al., 2015.