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Pitavastatin

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	3	HEK293-OATP1B1	Hirano, 2004
SLCO1B3	OATP1B3, OATP8	3.25	HEK293-OATP1B3	Hirano, 2004
ABCG2	BCRP, MXR	5.73	BCRP-expressing HEK293 vesicles	Hirano, 2005
SLC22A8	OAT3	3.3	OAT3-expressing oocytes	Fujino, 2005
SLCO1A2	OATP1A2, OATP-A	3.4	OATP1A2-expressing oocytes	Fujino, 2005
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	3.6	OATP1B1-expressing oocytes	Fujino, 2005
SLCO1B3	OATP1B3, OATP8	3.8	OATP1B3-expressing oocytes	Fujino, 2005
SLC10A1	NTCP	15.1	NTCP-expressing oocytes	Fujino, 2005
SLCO2B1	OATP2B1, OATP-B	1.17	HEK293-OATP2B1	Hirano, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	6.7	OATP1B1-expressing oocytes	Deng, 2008
mouse_Slco1a4	Oat, Oatp2, Oatp1a4, Slc21a5	8.27	HEK293 cells	Ose, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	2.48	HEK-OATP1B1	Izumi, 2015
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	0.429	HEK-OATP1B1	Chapy, 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
ABCG2	BCRP, MXR	Pitavastatin		2.92	Estrone sulfate	BCRP-expressing HEK293 vesicles	Hirano, 2005

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	ABCG2/OATPs	Cyclosporine	Pitavastatin	4.6	6.6	ND	ND	ND	ND	Livalo Drug Label	DDI 1
2	OATP1B1, OATP1B3,OATP2B1	Cyclosporine	Pitavastatin	4.60	ND	ND	ND	ND		Gessner, 2019	DDI 2
3	OATP1B1, OATP1B3,OATP2B1	Rifamin	Pitavastatin	5.70	4.36	ND	ND	0.75		Prueksaritanont, 2014	DDI 3
4	OATP1B1	Rifampicin	Pitavastatin	5.28	7.65	ND	0.15	0.51	ND	Chen, 2013	DDI 4
5	OATP1B1	Rifampicin	Pitavastatin	5.41	4.77	ND	ND	NS	ND	Prueksaritanont, 2014	DDI 5

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