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Glyburide

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
SLCO2B1	OATP2B1, OATP-B	6.26	HEK293-OATP2B1	Satoh, 2005
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	1.24	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)	Ki (μM)	Substrate used	Cell System	Reference
ABCC5	MRP5	Glyburide	15		5-fluorodeoxyuridine monophosphate	MRP5-expressing HEK293 vesicles	Pratt, 2005
SLC22A8	OAT3	Glyburide	0.21		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
SLC22A6	OAT1	Glyburide	5.7		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Glyburide	0.26		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
SLCO2B1	OATP2B1, OATP-B	Glyburide	1.9		Dibromofluorescein	HEK293-OATP2B1	Unger, 2020
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Glyburide	2.99		Estradiol-17beta-glucuronide	HEK-OATP1B1	van, 2013
ABCC3	MRP3	Glyburide	33		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Glyburide	10.5		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Glyburide	1.4		Estrone sulfate	HEK-OATP1B1	Tamraz, 2013
ABCB11	BSEP	Glyburide	18.8		Glycocholate	BSEP-expressing Sf9 vesicles	Kis, 2009
SLC22A1	OCT1	Glyburide	199		Metformin	HEK293-OCT1	Ahlin, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Glyburide		0.75	Pitavastatin	HEK293-OATP1B1	Hirano, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Glyburide	1.77		Rosuvastatin	HEK-OATP1B1	van, 2013
ABCB11	BSEP	Glyburide	15.8		Taurochenodeoxycholate	BSEP-expressing Sf9 vesicles	Kis, 2009
ABCB11	BSEP	Glyburide	11.3		Taurocholate	BSEP-expressing Sf9 vesicles	Kis, 2009
ABCB11	BSEP	Glyburide	14.7		Taurocholate	BSEP-expressing Sf9 vesicles	Kis, 2009
ABCB11	BSEP	Glyburide	5		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	OATPs	Rifampicin	Glyburide	2.2	1.8	NS	0.5	ND	yes	Zheng, 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