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Verapamil

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
ABCB1	MDR1, P-gp	2	MDR1-containing proteoliposomes	Borgnia, 1996
SLC22A4	OCTN1	ND	OCTN1-expressing oocytes	Yabuuchi, 1999
SLC22A5	OCTN2	ND	HEK293-OCTN2	Ohashi, 1999
ABCB4	MDR3	ND	Nucleotide trapping assay with Sf9-MDR3 membranes	Smith, 2000
ABCB1	MDR1, P-gp	2	MDR1-expressing Sf9 vesicles	Takahashi, 2005
ABCB1	MDR1, P-gp	4.1	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
ABCB1	MDR1, P-gp	1.9	Sf9 cell membranes	Bircsak, 2013

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	Verapamil	1.2		1-methyl-4-phenylpyridinium (MPP+)	MDCK-OCT1	Grube, 2011
SLC47A1	MATE1	Verapamil	42		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE1	Astorga, 2012
SLC47A2	MATE2K	Verapamil	37.9		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE2K	Astorga, 2012
SLC22A2	OCT2	Verapamil	91.9		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
SLC22A1	OCT1	Verapamil	1.1		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Parvez, 2016
SLC22A2	OCT2	Verapamil	66		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT2	Parvez, 2016
SLC22A2	OCT2	Verapamil	49.7		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
SLC22A2	OCT2	Verapamil	4.6		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
ABCB1	MDR1, P-gp	Verapamil	22.5		Calcein AM	CEM cells	Tiberghien, 1996
ABCB1	MDR1, P-gp	Verapamil	70		Calcein AM	Caco-2 cells	Eneroth, 2001
ABCB1	MDR1, P-gp	Verapamil	28.9		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Verapamil	6.3		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Verapamil	10		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Verapamil	2		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
ABCB1	MDR1, P-gp	Verapamil	4.6		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
ABCB1	MDR1, P-gp	Verapamil	4.6		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2008
ABCC2	MRP2, cMOAT	Verapamil	200		Calcein AM	MRP2-expressing MDCK-II cells	Leyers, 2008
ABCB1	MDR1, P-gp	Verapamil	5.2		Calcein AM	MDR1 expressing A2780/ADR cells	Klinkhammer, 2009
ABCB1	MDR1, P-gp	Verapamil	14		Calcein AM	MDR1 expressing MDCK2 cells	Gannon, 2009
ABCB1	MDR1, P-gp	Verapamil	1.5		Calcein AM	NIH 3T3 cells	Pivcevic, 2006
ABCB1	MDR1, P-gp	Verapamil	0.5		Calcein AM	MDR1 expressing MDCK cells	Pellicani, 2012
ABCB1	MDR1, P-gp	Verapamil	63.9		Calcein AM	MDCK-II cells	Georgantzopoulou, 2014
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Verapamil	>100		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
ABCB1	MDR1, P-gp	Verapamil	17.3		Colchicine	MDCK II-MDR1	Rautio, 2006
ABCB1	MDR1, P-gp	Verapamil	4.2		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Verapamil		15.3	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
ABCB1	MDR1, P-gp	Verapamil	2.1		Digoxin	Caco-2 cells	Choo, 2000
ABCB1	MDR1, P-gp	Verapamil	224		Digoxin	MDR1 expressing LLC-PK1 cells	Kawahara, 2000
ABCB1	MDR1, P-gp	Verapamil		8.11	Digoxin	Caco-2	Tang, 2002
ABCB1	MDR1, P-gp	Verapamil		15.1	Digoxin	MDCK-MDR1	Tang, 2002
ABCB1	MDR1, P-gp	Verapamil		0.88	Digoxin	MDR1-expressing Caco-2 cells	Horie, 2003
ABCB1	MDR1, P-gp	Verapamil	10.7		Digoxin	MDCK II-MDR1	Rautio, 2006
ABCB1	MDR1, P-gp	Verapamil	237		Digoxin	LLC-PK1 cells	Yoshida, 2006
ABCB1	MDR1, P-gp	Verapamil	3.2		Doxorubicin	B16/F10 cells	Bain, 1996
ABCC1	MRP1	Verapamil		13.2	Doxorubicin	2008/P-MRP1	Wong, 2009
SLC22A4	OCTN1	Verapamil		10.8	Ergothioneine	HEK293-OCTN1	Grigat, 2007
ABCC2	MRP2, cMOAT	Verapamil	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Verapamil	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Verapamil	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Verapamil	75.7		Estrone sulfate	HEK-OATP1B1	Tamraz, 2013
SLC22A1	OCT1	Verapamil	12		Ethambutol	HEK293-OCT1	Parvez, 2018
SLC22A4	OCTN1	Verapamil	12		Ethambutol	HEK293-hOCTN1	Parvez, 2018
SLC22A5	OCTN2	Verapamil	21.4		Ethambutol	HEK293-hOCTN2	Parvez, 2018
ABCB1	MDR1, P-gp	Verapamil	8.44		Fexofenadine	Caco-2	Petri, 2004
SLCO1A2	OATP1A2, OATP-A	Verapamil	2.6		Fexofenadine	HeLa-OATP1A2	Bailey, 2007
ABCB1	MDR1, P-gp	Verapamil	446.5		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Verapamil	6.6		Hoechst 33342	MDR1 expressing A2780/ADR cells	Muller, 2008
ABCB1	MDR1, P-gp	Verapamil	4.6		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
ABCB1	MDR1, P-gp	Verapamil	1.7		Hoechst 33342	Hela cells	Cortes-Ciriano, 2013
ABCB1	MDR1, P-gp	Verapamil		29	Irinotecan	MDCK II-MDR1	Luo, 2002
ABCB1	MDR1, P-gp	Verapamil	42		JC-1	NIH-3T3-G185 cells	Wang, 2001
SLC22A5	OCTN2	Verapamil	58.8		L-carnitine	HEK293-hOCTN2	Kobayashi, 2007
SLC22A5	OCTN2	Verapamil		5.3	L-carnitine	L6-hOCTN2	Todesco, 2008
SLC22A5	OCTN2	Verapamil		17.6	L-carnitine	MDCKII-hOCTN2	Diao, 2009
SLC22A5	OCTN2	Verapamil	50.9		L-carnitine	MDCKII-hOCTN2	Grube, 2011
ABCB1	MDR1, P-gp	Verapamil	4.7		LDS-751	NIH-3T3-G185 cells	Wang, 2001
SLC22A1	OCT1	Verapamil	0.62		Metformin	HEK293-OCT1	Ahlin, 2010
SLC22A2	OCT2	Verapamil	20		Metformin	CHO-OCT2	Belzer, 2013
SLC22A1	OCT1	Verapamil	0.8		Metformin	HEK293-OCT1	Parvez, 2016
SLC22A2	OCT2	Verapamil	36		Metformin	HEK293-OCT2	Parvez, 2016
SLC22A2	OCT2	Verapamil	10.3		Metformin	CHO-OCT2	Sandoval, 2018
SLC22A1	OCT1	Verapamil	1.6		Morphine	HEK293-OCT1	Tzvetkov, 2013
SLC22A1	OCT1	Verapamil	9.62		Morphine	HEK293-OCT1	Zhu, 2018
ABCB1	MDR1, P-gp	Verapamil	1.8		N-methyl-quinidine	Human "K" cell inverted vesicles	Mazur, 2015
SLC22A2	OCT2	Verapamil	85		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
ABCB4	MDR3	Verapamil	ND		Not applicable	nucleotide trapping with MDR3-expressing Sf9 membranes	Smith, 2000
SLC22A2	OCT2	Verapamil	21		NBD-MTMA	CHO-OCT2	Belzer, 2013
SLC22A2	OCT2	Verapamil	9.7		NBD-MTMA	CHO-OCT2	Sandoval, 2018
ABCB1	MDR1, P-gp	Verapamil		3	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
SLC22A2	OCT2	Verapamil	21.4		Para-Aminosalicylic acid (PAS)	HEK293-OCT2	Parvez, 2017
SLC22A1	OCT1	Verapamil	3.9		Prothionamide	HEK293-OCT1	Parvez, 2018
ABCB1	MDR1, P-gp	Verapamil	4.2		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
ABCB1	MDR1, P-gp	Verapamil	6.5		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Verapamil	9.8		Rhodamine 123	MDR1 expressing MDCK cells	Pick, 2011
SLC22A1	OCT1	Verapamil	33.2		Rhodamine 123	HEK293-OCT1	Jouan, 2014
SLC22A1	OCT1	Verapamil	1.5		Serotonin	HEK293-OCT1	Boxberger, 2014
ABCB11	BSEP	Verapamil	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A4	OCTN1	Verapamil		8.38	Tetraethylammonium	HEK293-hOCTN1	Peltekova, 2004
SLC47A1	MATE1	Verapamil		27.5	Tetraethylammonium	HEK293-MATE1	Tsuda, 2009
SLC47A2	MATE2K	Verapamil		32.1	Tetraethylammonium	HEK293-MATE2	Tsuda, 2009
SLC22A4	OCTN1	Verapamil	11		Tetraethylammonium	MDCKII-hOCTN1	Grube, 2011
SLC22A2	OCT2	Verapamil	17.8		Tetraethylammonium	CHO-OCT2	Sandoval, 2018
ABCB1	MDR1, P-gp	Verapamil	38.2		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Verapamil	1.5		Verapamil	Caco-2 cells	Doppenshmitt, 1998
ABCB1	MDR1, P-gp	Verapamil	33.5		Vinblastine	MDCK II-MDR1	Rautio, 2006
ABCB1	MDR1, P-gp	Verapamil	0.2		Vincristine	MDR1-expressing K562 vesicles	Noguchi, 2009
ABCB1	MDR1, P-gp	Verapamil	1.7		Ximelagatran	Caco-2 cells	Eriksson, 2006
SLC22A2	OCT2	Verapamil	13.4		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	Lovastatin	Verapamil	1.6	1.3	ND	ND	NS	ND	Choi, 2010	DDI 1
2	ABCB1	Verapamil	(R)-fexofenadine	2.9	2.2	ND	0.4	NS	ND	Sakugawa, 2009	DDI 2
3	ABCB1	Verapamil	(S)-fexofenadine	2.2	2.2	ND	0.5	NS	ND	Sakugawa, 2009	DDI 3
4	OCT1/MATEs	Verapamil	Metformin	1.07	1.09	0.98	NR	0.80	Yes	Cho, 2014	DDI 4
5	ABCB1/OATPs	Verapamil	Simvastatin	4.6	2.6	ND	ND	NS	ND	Kantola, 1998	DDI 5

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