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Itraconazole

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
ABCB1	MDR1, P-gp	Itraconazole	2.1	Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Itraconazole	0.2	Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Itraconazole	0.7	Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
ABCB1	MDR1, P-gp	Itraconazole	1.7	Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Itraconazole	1.7	Daunorubicin	G185 cells	Wang, 2002
SLCO2B1	OATP2B1, OATP-B	Itraconazole	24.8	Dibromofluorescein	HEK293-OATP2B1	Unger, 2020
ABCB1	MDR1, P-gp	Itraconazole	0.95	Digoxin	MDCKII-MDR1	Keogh, 2006
ABCB1	MDR1, P-gp	Itraconazole	2	Digoxin	Caco-2 cells	Cook, 2010
ABCC2	MRP2, cMOAT	Itraconazole	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Itraconazole	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Itraconazole	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Itraconazole	2.4	LDS-751	NIH-3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Itraconazole	18	Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013

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	Itraconazole	Digoxin	1.7	NS	0.8	ND	NS	ND	Jalava, 1997	DDI 1
2	ABCB1	Itraconazole	Quinidine	2.4	1.6	0.5	ND	1.6	yes	Kaukonen, 1997	DDI 2

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