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Simvastatin

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
ABCB1	MDR1, P-gp	Simvastatin	9		Daunorubicin	MDR1 expressing 3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Simvastatin	8.9		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
SLCO2B1	OATP2B1, OATP-B	Simvastatin	9.4		Dibromofluorescein	HEK293-OATP2B1	Unger, 2020
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Simvastatin	3.6		Estradiol-17beta-glucuronide	HEK-OATP1B1	Chen, 2005
ABCC2	MRP2, cMOAT	Simvastatin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Simvastatin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Simvastatin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A8	OAT3	Simvastatin	32.3		Estrone sulfate	S2-OAT3	Takeda, 2004
ABCG2	BCRP, MXR	Simvastatin		18	Estrone sulfate	BCRP-expressing HEK293 vesicles	Hirano, 2005
SLCO2B1	OATP2B1, OATP-B	Simvastatin	84.7		Estrone sulfate	MDCK II-OATP2B1	Grube, 2006
SLC22A5	OCTN2	Simvastatin		12.4	L-carnitine	MDCKII-hOCTN2	Diao, 2010
ABCB1	MDR1, P-gp	Simvastatin	26.1		LDS-751	NIH-3T3-G185 cells	Wang, 2001
SLC22A1	OCT1	Simvastatin	89		Metformin	HEK293-OCT1	Ahlin, 2010
SLC22A6	OAT1	Simvastatin	73.6		Para-aminohippurate	S2-OAT1	Takeda, 2004
SLC22A6	OAT1	Simvastatin	41.5		Para-aminohippurate	OAT1-expressing oocytes	Windass, 2007
ABCB1	MDR1, P-gp	Simvastatin	46		Rhodamine 123	MDR1 expressing 3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Simvastatin	56.8		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Simvastatin	24.7		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, OATP1B3,OATP2B1	Clarithromycin	Simvastatin	9.95	7.14	ND	ND	ND		Jacobson, 2004	DDI 1
2	ABCB1/OATPs	Erythromycin	Simvastatin	6.2	3.5	ND	ND	NS	ND	Kantola, 1998	DDI 2
3	OATP1B1	Gemfibrozil	Simvastatin	2.91	2.12	ND	ND	1.51	ND	Backman, 2000	DDI 3
4	ABCB1/OATPs	Verapamil	Simvastatin	4.6	2.6	ND	ND	NS	ND	Kantola, 1998	DDI 4

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