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Pravastatin

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	2250	HEK293-OATP2B1	Nozawa, 2004
ABCB11	BSEP	124	BSEP-expressing HEK293 vesicles	Hirano, 2005
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	85.7	HEK293-OATP1B1	Kameyama, 2005
SLC22A8	OAT3	27.2	S2-OAT3	Nakagomi-Hagihara, 2007
SLC22A11	OAT4	257	S2-OAT4	Nakagomi-Hagihara, 2007
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	57.5	OATP1B1-expressing oocytes	Deng, 2008
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	27	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
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Pravastatin	>100		Estradiol-17beta-glucuronide	HEK-OATP1B1	Chen, 2005
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Pravastatin		21.8	Estradiol-17beta-glucuronide	CHO-OATP1B1	Gui, 2009
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Pravastatin	3.6	3.4	Estradiol-17beta-glucuronide	HEK-OATP1B1	Karlgren, 2012
SLCO1B3	OATP1B3, OATP8	Pravastatin	62	57	Estradiol-17beta-glucuronide	HEK293-OATP1B3	Karlgren, 2012
SLC22A8	OAT3	Pravastatin	13.7		Estrone sulfate	S2-OAT3	Takeda, 2004
SLC22A6	OAT1	Pravastatin	408		Para-aminohippurate	S2-OAT1	Takeda, 2004
SLC22A8	OAT3	Pravastatin	76.3		Pemetrexed	HEK-OAT3	Kurata, 2014

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	Pravastatin	2.11	2.28	ND	ND	ND		Jacobson, 2004	DDI 1
2	ABCC2/OATP1B1	Cyclosporine	Pravastatin	9.93	7.78	ND	ND	0.75	ND	Hedman, 2004	DDI 2
3	OATP1B1	Gemfibrozil	Pravastatin	2.02	NS	0.57	ND	NS	ND	Kyrklund, 2003	DDI 3
4	OATP1B1	Rifampicin	Pravastatin	2.27	2.73	ND	0.5	NS	ND	Deng, 2009	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