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Ketoconazole

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.

In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter

Transporter	Synonyms	Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
SLC47A1	MATE1	Ketoconazole	1.33		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE1	Astorga, 2012
SLC47A2	MATE2K	Ketoconazole	9.33		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE2K	Astorga, 2012
SLC22A1	OCT1	Ketoconazole	7.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Ahlin, 2010
SLC22A1	OCT1	Ketoconazole	2.6		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Chen, 2017
ABCB1	MDR1, P-gp	Ketoconazole	36		Calcein AM	Caco-2 cells	Eneroth, 2001
ABCB1	MDR1, P-gp	Ketoconazole		24.9	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
ABCB1	MDR1, P-gp	Ketoconazole	4.8		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Ketoconazole	3.8		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Ketoconazole	6.7		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
ABCB1	MDR1, P-gp	Ketoconazole	5.49		Colchicine	MDCK II-MDR1	Rautio, 2006
ABCB1	MDR1, P-gp	Ketoconazole	5.6		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Ketoconazole	5.6		Daunorubicin	G185 cells	Wang, 2002
SLCO2B1	OATP2B1, OATP-B	Ketoconazole	5.7		Dibromofluorescein	HEK293-OATP2B1	Unger, 2020
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Ketoconazole		11.5	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
ABCB1	MDR1, P-gp	Ketoconazole	1.2		Digoxin	Caco-2 cells	Choo, 2000
ABCB1	MDR1, P-gp	Ketoconazole	1.4		Digoxin	Caco-2 cells	Wandel, 2000
ABCB1	MDR1, P-gp	Ketoconazole	1.34		Digoxin	MDCKII-MDR1	Keogh, 2006
ABCB1	MDR1, P-gp	Ketoconazole	3.07		Digoxin	MDCK II-MDR1	Rautio, 2006
ABCC4	MRP4	Ketoconazole	69		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Ketoconazole	1.8		Estradiol-17beta-glucuronide	HEK-OATP1B1	Vermeer, 2016
ABCC2	MRP2, cMOAT	Ketoconazole	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Ketoconazole	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A8	OAT3	Ketoconazole	0.86		Estrone sulfate	HEK293-OAT3	Vermeer, 2016
SLC22A8	OAT3	Ketoconazole	64		Estrone sulfate	HEK293-OAT3	Tsuruya, 2017
ABCB1	MDR1, P-gp	Ketoconazole	23.4		LDS-751	NIH-3T3-G185 cells	Wang, 2001
SLC22A6	OAT1	Ketoconazole	5.7		PAH	HEK293-OAT1	Vermeer, 2016
SLC22A6	OAT1	Ketoconazole	319		Para-aminohippurate	OAT1-expressing oocytes	Choi, 2011
ABCB1	MDR1, P-gp	Ketoconazole	5.6		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
ABCB1	MDR1, P-gp	Ketoconazole	53.4		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
SLC22A8	OAT3	Ketoconazole	15.77		Rivaroxaban	HEK293-OAT3	Cheong, 2019
SLC10A1	NTCP	Ketoconazole	264		Taurocholate	HeLa-NTCP	Kim, 1999
ABCB11	BSEP	Ketoconazole	3.4		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Ketoconazole	13		Verapamil	Caco-2 cells	Doppenshmitt, 1998
ABCB1	MDR1, P-gp	Ketoconazole		5.27	Vinblastine	MDR1-expressing LLC-PK1 cells	Ekins, 2002
ABCB1	MDR1, P-gp	Ketoconazole	6.34		Vinblastine	MDCK II-MDR1	Rautio, 2006

Clinical Drug-Drug Interactions

No drug-drug interaction information.