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Repaglinide

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
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	1.36	HEK-OATP1B1	Izumi, 2015

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	Repaglinide	9.2	4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Ahlin, 2008
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Repaglinide	2.2	Bromsulphthalein	HEK293-OATP1B1	Bachmakov, 2008
SLCO1B3	OATP1B3, OATP8	Repaglinide	5.6	Bromsulphthalein	HEK293-OATP1B3	Bachmakov, 2008
SLCO2B1	OATP2B1, OATP-B	Repaglinide	5.2	Bromsulphthalein	HEK293-OATP2B1	Bachmakov, 2008
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Repaglinide	0.32	Estradiol-17beta-glucuronide	HEK-OATP1B1	Hinton, 2008
ABCC2	MRP2, cMOAT	Repaglinide	72.3	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Repaglinide	16.7	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Repaglinide	53.9	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Repaglinide	1.1	Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
SLC22A1	OCT1	Repaglinide	1.6	Metformin	MDCK II-OCT1	Bachmakov, 2008
SLC22A1	OCT1	Repaglinide	1.8	N-methylpyridinium	MDCK II-OCT1	Bachmakov, 2008
ABCB11	BSEP	Repaglinide	22	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	OATP1B1 (CYP3A4)	Cyclosporine	Repaglinide	2.44	1.72	NS	ND	NS	NS	Kajosaari, 2005	DDI 1
2	OATP1B1 (CYP2C8)	Gemfibrozil	Repaglinide	8.22	2.6	ND	ND	2.27	Yes	Kalliokoski, 2008	DDI 2
3	OATP1B1	Irbesartan	Repaglinide	1.33	1.84	ND	ND	NS	Yes	Pei, 2018	DDI 3

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