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Gemfibrozil

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
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Gemfibrozil	156.2	68.05	Atorvastatin	HEK-OATP1B1	Karlgren, 2012
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Gemfibrozil		18.1	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Gemfibrozil		12.5	Estradiol-17beta-glucuronide	HEK293-OATP1B1	Yamazaki, 2005
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Gemfibrozil	7.4		Estradiol-17beta-glucuronide	HEK-OATP1B1	Hinton, 2008
ABCC3	MRP3	Gemfibrozil	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Gemfibrozil	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A8	OAT3	Gemfibrozil	6.8		Pravastatin	S2-OAT3	Nakagomi-Hagihara, 2007
SLC10A1	NTCP	Gemfibrozil	23		Rosuvastatin	HeLa-NTCP	Ho, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Gemfibrozil	25		Rosuvastatin	HeLa-OATP1B1	Ho, 2006
SLCO2B1	OATP2B1, OATP-B	Gemfibrozil	8		Rosuvastatin	HeLa-OATP2B1	Ho, 2006
ABCB11	BSEP	Gemfibrozil	>133		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	Gemfibrozil	Atorvastatin	1.24	1.17	ND	ND	0.84	ND	Backman, 2005	DDI 1
2	OATP1B1	Gemfibrozil	Atorvastatin	1.35	NS	ND	ND	0.74	ND	Whitfield, 2011	DDI 2
3	OATP1B1	Gemfibrozil	Lovastatin	2.79	2.81	ND	ND	ND	ND	Kyrklund, 2001	DDI 3
4	OATP1B1	Gemfibrozil	Pravastatin	2.02	NS	0.57	ND	NS	ND	Kyrklund, 2003	DDI 4
5	OATP1B1 (CYP2C8)	Gemfibrozil	Repaglinide	8.22	2.6	ND	ND	2.27	Yes	Kalliokoski, 2008	DDI 5
6	OATP1B1	Gemfibrozil	Rosuvastatin	1.88	2.21	ND	ND	NS	ND	Schneck, 2004	DDI 6
7	OATP1B1	Gemfibrozil	Simvastatin	2.91	2.12	ND	ND	1.51	ND	Backman, 2000	DDI 7

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