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SLCO1A2

Synonyms: OATP, OATP-A, OATP1A2, SLC21A3

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Expression Data

Expression data for other tissues could be found in http://pharmacogenetics.ucsf.edu/gtex/index.html

Asterisk indicates important transporters in the organ as identified in the organ diagram.

Organ	Source	Relative Expression
Brain	Nishimura	`0.0825`
Kidney*	Nishimura	`0.00199`
Liver*	Nishimura	`0.00324`
Placenta	Nishimura	`0.000130`
Small Intestine*	Nishimura	`0.0000198`
Kidney*	Mean across all PMT Samples	BLQ
Liver*	Mean across all PMT Samples	`0.610`

Note that relative expression values should only be compared between entries of the same source.

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In Vitro Substrates

Substrate	Km (μM)	Cell System	Reference
Bromsulphthalein	ND	OATP1A2-expressing oocytes	Kullak-Ublick, 2001
Dehydroepiandrosterone sulfate	ND	OATP1A2-expressing oocytes	Kullak-Ublick, 2001
Estrone sulfate	13.6	HEK293-OATP1A2	Badagnani, 2006
Fexofenadine	6.4	HeLa-OATP1A2	Cvetkovic, 1999
Levofloxacin	136	OATP1A2-expressing oocytes	Maeda, 2007
Methotrexate	457	OATP1A2-expressing oocytes	Badagnani, 2006
Ouabain	5.5	OATP1A2-expressing oocytes	Bossuyt, 1996
Pitavastatin	3.4	OATP1A2-expressing oocytes	Fujino, 2005
Rosuvastatin	2.6	HeLa-OATP1A2	Ho, 2006
Saquinavir	36.4	OATP1A2-expressing oocytes	Su, 2004
Taurocholate	60	OATP1A2-expressing oocytes	Kullak-Ublick, 1995
Tauroursodeoxycholate	19	OATP1A2-expressing oocytes	Kullak-Ublick, 1995
Thyroxine	ND	OATP1A2-expressing oocytes	Fujiwara, 2001

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022

In Vitro Inhibitors

Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
Bromsulphthalein	3.75		Estrone sulfate	COS1-OATP1A2	Lan, 2009
Hesperidin	2.7		Fexofenadine	HeLa-OATP1A2	Bailey, 2007
Naringin	3.6		Fexofenadine	HeLa-OATP1A2	Bailey, 2007
Naringin	343		Talinolol	OATP1A2-expressing oocytes	Shirasaka, 2010
Rifampicin		51	Bromsulphthalein	OATP1A2-expressing oocytes	Vavricka, 2002
Rifamycin SV		11	Bromsulphthalein	OATP1A2-expressing oocytes	Vavricka, 2002
Ritonavir	<10		Fexofenadine	HeLa-OATP1A2	Cvetkovic, 1999
Saquinavir	<10		Fexofenadine	HeLa-OATP1A2	Cvetkovic, 1999
Verapamil	2.6		Fexofenadine	HeLa-OATP1A2	Bailey, 2007

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	Atazanavir / Ritonavir	Rosuvastatin	3.1	7.0	ND	ND	ND	ND	Busti, 2008	DDI 1
2	ABCB1/OATPs	Cyclosporine	Docetaxel	7.3	5.7	ND	ND	ND	ND	Malingre, 2001	DDI 2
3	ABCB1/OATPs	Cyclosporine	Paclitaxel	8.5	2.0	ND	ND	ND	ND	Meerum, 1999	DDI 3
4	ABCG2/OATPs	Cyclosporine	Pitavastatin	4.6	6.6	ND	ND	ND	ND	Livalo Drug Label	DDI 4
5	ABCG2/OATPs	Cyclosporine	Rosuvastatin	5.0	10.6	ND	ND	ND	ND	Simonson, 2004	DDI 5
6	ABCG2/OATPs	Cyclosporine	Rosuvastatin	6.4	18.2	ND	ND	ND	ND	Simonson, 2004	DDI 6
7	ABCB1/OATPs	Erythromycin	Simvastatin	6.2	3.5	ND	ND	NS	ND	Kantola, 1998	DDI 7
8	ABCB1/OATPs	Indinavir / Ritonavir	Fexofenadine	4.8	2.5	ND	0.2	0.7	ND	Kharasch, 2009	DDI 8
9	OATPs	Lopinavir / Ritonavir	Rosuvastatin	2.1	4.7	ND	0.5	NS	yes	Kiser, 2008	DDI 9
10	OATPs	Rifampicin	Glyburide	2.2	1.8	NS	0.5	ND	yes	Zheng, 2009	DDI 10
11	ABCB1/OATPs	Ritonavir	Digoxin	1.9	ND	0.6	0.6	2.6	ND	Ding, 2004	DDI 11
12	ABCB1/OATPs	Ritonavir	Saquinavir	29.9	22.5	ND	ND	ND	ND	la, 2007	DDI 12
13	ABCB1/OATPs	Verapamil	Simvastatin	4.6	2.6	ND	ND	NS	ND	Kantola, 1998	DDI 13

The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
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
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022