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Famotidine

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	56.1	HEK293-OCT2	Tahara, 2005

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	Famotidine	2.16		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE1	Astorga, 2012
SLC47A2	MATE2K	Famotidine	6.28		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE2K	Astorga, 2012
SLC22A1	OCT1	Famotidine	>300		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Wittwer, 2013
SLC22A3	OCT3	Famotidine	10.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT3	Wittwer, 2013
SLC22A2	OCT2	Famotidine	36.1		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
SLC47A1	MATE1	Famotidine	0.76		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
SLC47A2	MATE2K	Famotidine	36.2		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
ABCC2	MRP2, cMOAT	Famotidine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Famotidine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Famotidine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A1	OCT1	Famotidine	28		N-methylpyridinium	OCT1-expressing oocytes	Bourdet, 2005
SLC22A2	OCT2	Famotidine	114		N-methylpyridinium	OCT2-expressing oocytes	Bourdet, 2005
SLC22A3	OCT3	Famotidine	6.7		N-methylpyridinium	OCT3-expressing oocytes	Bourdet, 2005
ABCB11	BSEP	Famotidine	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC47A1	MATE1	Famotidine		0.6	Tetraethylammonium	HEK293-MATE1	Tsuda, 2009
SLC47A2	MATE2K	Famotidine		9.7	Tetraethylammonium	HEK293-MATE2	Tsuda, 2009

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	OATs	Probenecid	Famotidine	1.8	1.5	0.4	0.1	NS	ND	Inotsume, 1990	DDI 1

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