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Indinavir

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
ABCB1	MDR1, P-gp	0.47	ATPase assay of High Five-MDR1 membranes	Lee, 1998

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
SLC22A1	OCT1	Indinavir	37		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Jung, 2008
SLC22A1	OCT1	Indinavir	208		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Wittwer, 2013
SLC22A3	OCT3	Indinavir	>500		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT3	Wittwer, 2013
SLC22A2	OCT2	Indinavir	142		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
SLC47A1	MATE1	Indinavir	7.8		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
SLC47A2	MATE2K	Indinavir	7.8		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
SLC47A2	MATE2K	Indinavir	>500		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Indinavir	12.2	10.8	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
SLCO1B3	OATP1B3, OATP8	Indinavir	12.3	8.5	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B3	Annaert, 2010
ABCB1	MDR1, P-gp	Indinavir	44		Digoxin	Caco-2 cells	Choo, 2000
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Indinavir	5.84		Estradiol-17beta-glucuronide	HeLa-OATP1B1	Tirona, 2003
SLCO1B3	OATP1B3, OATP8	Indinavir	16		Estradiol-17beta-glucuronide	HEK-OATP1B3	Chiou, 2014
ABCC3	MRP3	Indinavir	83		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	Indinavir	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Indinavir	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO2B1	OATP2B1, OATP-B	Indinavir	3.9	3	Estrone sulfate	Caco-2	Annaert, 2010
SLC47A1	MATE1	Indinavir	1.7		Metformin	HEK293-MATE1	Wittwer, 2013
SLC47A1	MATE1	Indinavir	1.9		Metformin	MDCK2- MATE1	Wittwer, 2013
ABCB11	BSEP	Indinavir	21.2		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A1	OCT1	Indinavir	61.7		Tetraethylammonium	HeLa-OCT1	Zhang, 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/OATPs	Indinavir / Ritonavir	Fexofenadine	4.8	2.5	ND	0.2	0.7	ND	Kharasch, 2009	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