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

Quinidine

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

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

Transporter	Synonyms	Km (μM)	Cell System	Reference
SLC22A4	OCTN1	ND	OCTN1-expressing oocytes	Yabuuchi, 1999
SLC22A5	OCTN2	ND	HEK293-OCTN2	Ohashi, 1999
ABCB1	MDR1, P-gp	18.2	MDR1-expressing insect vesicles	Smith, 2001

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
SLC22A1	OCT1	Quinidine	16.8		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Umehara, 2008
SLC47A1	MATE1	Quinidine	1.57		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE1	Astorga, 2012
SLC47A2	MATE2K	Quinidine	1.47		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE2K	Astorga, 2012
SLC22A2	OCT2	Quinidine	91.6		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
SLC22A2	OCT2	Quinidine	92.6		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Severance, 2017
SLC22A2	OCT2	Quinidine	91.1		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
SLC22A1	OCT1	Quinidine	340		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Ahlin, 2010
SLC47A1	MATE1	Quinidine	11.2		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
SLC22A2	OCT2	Quinidine	6.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
ABCB1	MDR1, P-gp	Quinidine	30.5		Calcein AM	CEM cells	Tiberghien, 1996
ABCB1	MDR1, P-gp	Quinidine	157		Calcein AM	Caco-2 cells	Eneroth, 2001
ABCB1	MDR1, P-gp	Quinidine	5.6		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Quinidine	13		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Quinidine	10		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
ABCB1	MDR1, P-gp	Quinidine	51.7		Colchicine	MDCK II-MDR1	Rautio, 2006
ABCB1	MDR1, P-gp	Quinidine	18.8		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Quinidine	2.2		Digoxin	Caco-2 cells	Choo, 2000
ABCB1	MDR1, P-gp	Quinidine		3.23	Digoxin	Caco-2	Tang, 2002
ABCB1	MDR1, P-gp	Quinidine		8.59	Digoxin	MDCK-MDR1	Tang, 2002
ABCB1	MDR1, P-gp	Quinidine	9.52		Digoxin	MDR1 transfected LLC-PK1	Kakumoto, 2002
ABCB1	MDR1, P-gp	Quinidine		0.43	Digoxin	MDR1-expressing Caco-2 cells	Horie, 2003
ABCB1	MDR1, P-gp	Quinidine	9.4		Digoxin	MDCKII-MDR1	Keogh, 2006
ABCB1	MDR1, P-gp	Quinidine	14.9		Digoxin	MDCK II-MDR1	Rautio, 2006
ABCC4	MRP4	Quinidine	45.8		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	Quinidine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Quinidine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A5	OCTN2	Quinidine	239		L-carnitine	HEK293-hOCTN2	Kobayashi, 2007
ABCB1	MDR1, P-gp	Quinidine	1		LDS-751	NIH-3T3-G185 cells	Wang, 2001
SLC22A2	OCT2	Quinidine	6.4		Metformin	CHO-OCT2	Belzer, 2013
SLC22A2	OCT2	Quinidine	18.6		Metformin	CHO-OCT2	Sandoval, 2018
SLC22A1	OCT1	Quinidine	3.58		Monocrotaline	MDCK-OCT1	Tu, 2013
SLC22A1	OCT1	Quinidine	6.7		N-methylpyridinium	OCT1-expressing oocytes	Bourdet, 2005
SLC22A2	OCT2	Quinidine	8.7		N-methylpyridinium	OCT2-expressing oocytes	Bourdet, 2005
SLC22A3	OCT3	Quinidine	18.3		N-methylpyridinium	OCT3-expressing oocytes	Bourdet, 2005
SLC22A1	OCT1	Quinidine	5.7		N-methylpyridinium	CHO-OCT1	Ming, 2009
SLC22A2	OCT2	Quinidine	13.3		N-methylpyridinium	CHO-OCT2	Ming, 2009
SLC22A3	OCT3	Quinidine	22.7		N-methylpyridinium	CHO-OCT3	Ming, 2009
SLC22A2	OCT2	Quinidine	87		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
SLC22A2	OCT2	Quinidine	29.6		NBD-MTMA	CHO-OCT2	Belzer, 2013
SLC22A2	OCT2	Quinidine	18.7		NBD-MTMA	CHO-OCT2	Sandoval, 2018
ABCB1	MDR1, P-gp	Quinidine		1.5	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
SLC22A2	OCT2	Quinidine	10.7		Para-Aminosalicylic acid (PAS)	HEK293-OCT2	Parvez, 2017
ABCB1	MDR1, P-gp	Quinidine	33.9		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Quinidine	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A1	OCT1	Quinidine		17.5	Tetraethylammonium	HeLa-OCT1	Zhang, 1998
SLC22A4	OCTN1	Quinidine	<1000		Tetraethylammonium	HEK293-OCTN1	Yabuuchi, 1999
SLC22A1	OCT1	Quinidine	5.4		Tetraethylammonium	HeLa-OCT1	Bednarczyk, 2003
SLC22A4	OCTN1	Quinidine		68.38	Tetraethylammonium	HEK293-hOCTN1	Peltekova, 2004
SLC47A1	MATE1	Quinidine		29.2	Tetraethylammonium	HEK293-MATE1	Tsuda, 2009
SLC47A2	MATE2K	Quinidine		23.1	Tetraethylammonium	HEK293-MATE2	Tsuda, 2009
SLC22A2	OCT2	Quinidine	23.6		Tetraethylammonium	CHO-OCT2	Sandoval, 2018
ABCB1	MDR1, P-gp	Quinidine	340		Verapamil	Caco-2 cells	Doppenshmitt, 1998
ABCB1	MDR1, P-gp	Quinidine	22.9		Vinblastine	MDCK II-MDR1	Rautio, 2006
ABCB1	MDR1, P-gp	Quinidine	1.8		Ximelagatran	Caco-2 cells	Eriksson, 2006
SLC22A1	OCT1	Quinidine	7.11		YM155	HEK293-OCT1	Minematsu, 2010
SLC22A2	OCT2	Quinidine	11		YM155	HEK293-OCT2	Minematsu, 2010

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	ABCB1	Itraconazole	Quinidine	2.4	1.6	0.5	ND	1.6	yes	Kaukonen, 1997	DDI 1
2	ABCB1	Quinidine	Digoxin	ND	ND	0.7	0.6	ND	ND	Rameis, 1985; Hager, 1979	DDI 2

PK = pharmacokinetic
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
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