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Ranitidine

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
SLC22A2	OCT2	65.2	HEK293-OCT2	Tahara, 2005
SLC22A1	OCT1	70	OCT1-expressing oocytes	Bourdet, 2005
SLC22A1	OCT1	62.9	HEK293-OCT1	Meyer, 2017

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	Ranitidine	5.4		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE1	Astorga, 2012
SLC47A2	MATE2K	Ranitidine	10		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE2K	Astorga, 2012
SLC22A1	OCT1	Ranitidine	81.91		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Meyer, 2017
SLC47A1	MATE1	Ranitidine	8.3		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
SLC22A1	OCT1	Ranitidine	336.59		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Meyer, 2017
ABCB1	MDR1, P-gp	Ranitidine	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Ranitidine	>50		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Ranitidine	>50		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
SLC22A2	OCT2	Ranitidine		79	Cimetidine	HEK293-OCT2	Tahara, 2005
ABCC2	MRP2, cMOAT	Ranitidine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Ranitidine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Ranitidine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A2	OCT2	Ranitidine		30.5	Famotidine	HEK293-OCT2	Tahara, 2005
SLC47A1	MATE1	Ranitidine	18.9		Metformin	HeLa-MATE1	Meyer, 2010
SLC22A1	OCT1	Ranitidine	20.93		Metformin	HEK293-OCT1	Meyer, 2017
SLC22A1	OCT1	Ranitidine	45.5		Morphine	HEK293-OCT1	Meyer, 2017
SLC22A1	OCT1	Ranitidine	33		N-methylpyridinium	OCT1-expressing oocytes	Bourdet, 2005
SLC22A2	OCT2	Ranitidine	76		N-methylpyridinium	OCT2-expressing oocytes	Bourdet, 2005
SLC22A3	OCT3	Ranitidine	290		N-methylpyridinium	OCT3-expressing oocytes	Bourdet, 2005
SLC22A1	OCT1	Ranitidine	28		N-methylpyridinium	HEK293-OCT1	Muller, 2005
SLC22A2	OCT2	Ranitidine	1617		N-methylpyridinium	HEK293-OCT2	Muller, 2005
SLC22A3	OCT3	Ranitidine	372		N-methylpyridinium	CHO-OCT3	Muller, 2005
ABCB11	BSEP	Ranitidine	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A1	OCT1	Ranitidine	21.7		Tetraethylammonium	HeLa-OCT1	Bednarczyk, 2003
SLC47A1	MATE1	Ranitidine		25.4	Tetraethylammonium	HEK293-MATE1	Tsuda, 2009
SLC47A2	MATE2K	Ranitidine		25	Tetraethylammonium	HEK293-MATE2	Tsuda, 2009
SLC47A1	MATE1	Ranitidine	17.5		Tetraethylammonium	HeLa-MATE1	Meyer, 2010
SLC22A2	OCT2	Ranitidine	482		Trospium	HEK293-OCT2	Abebe, 2020

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	OCTs/MATEs	Cimetidine	Ranitidine	1.3	NS	0.7	ND	1.3	ND	van, 1986	DDI 1
2	OCTs/MATEs	Ranitidine	Trospium (IV)	1.06	1.10	0.87	1.1	1.00	No	Abebe, 2020	DDI 2
3	OCTs/MATEs	Ranitidine	Trospium (oral)	0.87	0.92	0.99	NR	0.98	No	Abebe, 2020	DDI 3

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