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Valspodar

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)	Ki (μM)	Substrate used	Cell System	Reference
ABCB1	MDR1, P-gp	Valspodar	0.41		Calcein AM	CEM cells	Tiberghien, 1996
ABCB1	MDR1, P-gp	Valspodar		1.3	Calcein AM	CEM/VBL 100	Wigler, 1999
ABCB1	MDR1, P-gp	Valspodar	3.2		Calcein AM	MDCK-II cells	Georgantzopoulou, 2014
ABCB1	MDR1, P-gp	Valspodar	0.5		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
ABCB1	MDR1, P-gp	Valspodar	0.11		Digoxin	Caco-2 cells	Choo, 2000
ABCB1	MDR1, P-gp	Valspodar	0.11		Digoxin	Caco-2 cells	Wandel, 2000
ABCC1	MRP1	Valspodar	27		Leukotriene C4	MRP1-expressing HeLa vesicles	Leier, 1994
ABCC2	MRP2, cMOAT	Valspodar		28.9	Leukotriene C4	MRP2-expressing LLC-PK1 vesicles	Chen, 1999
ABCB4	MDR3	Valspodar	ND		Not applicable	nucleotide trapping with MDR3-expressing Sf9 membranes	Smith, 2000

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	Valspodar	Digoxin	3.0	2.4	0.2	0.3	ND	no	Kovarik, 1999	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