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Digoxin

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
ABCB4	MDR3	ND	Nucleotide trapping assay with Sf9-MDR3 membranes	Smith, 2000
SLCO1B3	OATP1B3, OATP8	ND	OATP1B3-expressing oocytes	Kullak-Ublick, 2001
OSTalpha	OSTA	ND	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
OSTbeta	OSTB	ND	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
ABCB1	MDR1, P-gp	177	Caco-2	Troutman, 2003
ABCB1	MDR1, P-gp	73	Caco-2	Collett, 2004
ABCB1	MDR1, P-gp	181	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007

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
ABCB1	MDR1, P-gp	Digoxin	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Digoxin	>50		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Digoxin	>50		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Digoxin	7.9	7	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
SLCO1B3	OATP1B3, OATP8	Digoxin	1	0.7	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B3	Annaert, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Digoxin	63		Estradiol-17beta-glucuronide	HEK-OATP1B1	Gozalpour, 2014
OSTalpha	OSTA	Digoxin	<500		Estrone sulfate	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
OSTbeta	OSTB	Digoxin	<500		Estrone sulfate	OSTalpha-OSTbeta expressing oocytes	Seward, 2003

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	Dronedarone	Digoxin	2.3	1.7	0.5	ND	ND	ND	Dronedarone Drug Label	DDI 1
2	ABCB1	Itraconazole	Digoxin	1.7	NS	0.8	ND	NS	ND	Jalava, 1997	DDI 2
3	ABCB1	Quinidine	Digoxin	ND	ND	0.7	0.6	ND	ND	Rameis, 1985; Hager, 1979	DDI 3
4	ABCB1	Ranolazine	Digoxin	1.6	1.5	ND	ND	ND	ND	Jerling, 2006	DDI 4
5	ABCB1/OATPs	Ritonavir	Digoxin	1.9	ND	0.6	0.6	2.6	ND	Ding, 2004	DDI 5
6	ABCB1	Valspodar	Digoxin	3.0	2.4	0.2	0.3	ND	no	Kovarik, 1999	DDI 6

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