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Pantoprazole

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)	Substrate used	Cell System	Reference
SLC22A1	OCT1	Pantoprazole	>500	4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Wittwer, 2013
SLC22A3	OCT3	Pantoprazole	137	4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT3	Wittwer, 2013
SLC22A2	OCT2	Pantoprazole	1.5	4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
SLC47A1	MATE1	Pantoprazole	43.2	4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
SLC47A2	MATE2K	Pantoprazole	43.2	4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
SLC47A2	MATE2K	Pantoprazole	500	4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
ABCB1	MDR1, P-gp	Pantoprazole	17.9	Digoxin	Caco-2 cells	Pauli-Magnus, 2001
SLC22A1	OCT1	Pantoprazole	30.8	Metformin	HEK293-OCT1	Nies, 2011
SLC22A2	OCT2	Pantoprazole	2.8	Metformin	HEK293-OCT2	Nies, 2011
SLC47A1	MATE1	Pantoprazole	2.8	Metformin	MDCK2- MATE1	Wittwer, 2013
SLC47A1	MATE1	Pantoprazole	2.8	Metformin	HEK293-MATE1	Wittwer, 2013
SLC22A2	OCT2	Pantoprazole	0.56	Metformin	HEK293-OCT2	Hacker, 2015
ABCG2	BCRP, MXR	Pantoprazole	5.5	Methotrexate	BCRP membrane vesicles	Suzuki, 2009
ABCG2	BCRP, MXR	Pantoprazole	9.6	Rosuvastatin	polarized Caco-2 monolayer	Elsby, 2016

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	ABCG2	Pantoprazole	Sulfasalazine	1	1	ND	ND	1		Adkison, 2010	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