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ABCG2

Synonyms: ABC15, ABCP, BCRP, BCRP1, BMDP, CD338, CDw338, EST157481, MGC102821, MRX, MXR, MXR1

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	`0.0224`
Kidney*	Nishimura	`0.00463`
Liver*	Nishimura	`0.0139`
Placenta*	Nishimura	`0.0954`
Small Intestine*	Nishimura	`0.0492`
Kidney*	Mean across all PMT Samples	`0.739`
Liver*	Mean across all PMT Samples	`1.555`

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
(+)-Pantoprazole	5.32	MDCK-transfected cells	Wang, 2012
(-)-Pantoprazole	0.59	MDCK-transfected cells	Wang, 2012
2'-Hydroxyflavone-O-glucuronide	5.4	HeLa-transfected cells	Wei, 2013
3'-Hydroxyflavone-O-glucuronide	5.6	HeLa-transfected cells	Wei, 2013
3'-Hydroxyflavone-O-glucuronide	9.7	HeLa-transfected cells	Wei, 2013
3,2'-Dihydroxyflavone-O-glucuronide	35.9	HeLa-transfected cells	Wei, 2013
3,3'-Dihydroxyflavone-O-glucuronide	45.2	HeLa-transfected cells	Wei, 2013
3,4'-Dihydroxyflavone-O-glucuronide	35.9	HeLa-transfected cells	Wei, 2013
3,5-Dihydroxyflavone-O-glucuronide	12.8	HeLa-transfected cells	Wei, 2013
3,6-Dihydroxyflavone-O-glucuronide	31.9	HeLa-transfected cells	Wei, 2013
3,7-Dihydroxyflavone-O-glucuronide	3.5	HeLa-transfected cells	Wei, 2013
4-Hydroxyflavone-O-glucuronide	17.5	HeLa-transfected cells	Wei, 2013
4-methylumbelliferone sulfate	12.9	BCRP-expressing vesicles from mouse lymphoma (P388) cells	Suzuki, 2003
5-Hydroxyflavone-O-glucuronide	48.5	HeLa-transfected cells	Wei, 2013
6-Hydroxyflavone-O-glucuronide	26.8	HeLa-transfected cells	Wei, 2013
7-Hydroxyflavone-O-glucuronide	9	HeLa-transfected cells	Wei, 2013
Bupropion	3	Membrane vesicles	Hemauer, 2010
Daunorubicin	2.5	ATP hydrolysis assay of BCRP-expressing Sf9 vesicles	Ozvegy, 2001
Doxorubicin	5	ATP hydrolysis assay of BCRP-expressing Sf9 vesicles	Ozvegy, 2001
Edaravone sulfate	16.5	Membrane vesicles	Mizuno, 2007
Estradiol-17beta-glucuronide	44.2	BCRP-expressing HEK293 vesicles	Chen, 2003
Estrone sulfate¹	16.6	BCRP-expressing vesicles from mouse lymphoma (P388) cells	Suzuki, 2003
Estrone sulfate¹	6.8	BCRP-expressing K562 vesicles	Imai, 2003
Ethinyl estradiol sulfate	2.9	Membrane vesicles	Han, 2010
Gemifloxacin	145.69	MDCK-transfected cells	Jin, 2013
Glibenclamide	13.07	MDCK-transfected cells	Pollex, 2010
Hematoporphyrin	17.8	BCRP-expressing Sf9 vesicles	Tamura, 2006
Imatinib	ND	Intracellular accumulation in BCRP-expressing HEK293 cells inhbited with Ko-143	Burger, 2004
Lamivudine	216.5	MDCK-transfected cells	Kim, 2007
Methotrexate	1340	BCRP-expressing HEK293 vesicles	Chen, 2003
Methotrexate	681	BCRP-expressing MCF7/MX vesicles	Volk, 2003
Methotrexate	681	MDCK-transfected cells	Xia, 2007
Methotrexate	1410	BCRP-expressing HEK293 vesicles	Tiwari, 2009
Mitoxantrone	7	ATP hydrolysis assay of BCRP-expressing Sf9 vesicles	Ozvegy, 2001
Nitrofurantoin	69.4	Caco-2 cells	Wright, 2011
Pemetrexed	390	Membrane vesicles	Li, 2011
Pitavastatin	5.73	BCRP-expressing HEK293 vesicles	Hirano, 2005
Rosuvastatin³	10.1	MDCK II-BCRP	Deng, 2008
Rosuvastatin³	2.02	BCRP-expressing HEK293 vesicles	Kitamura, 2008
Sildenafil	22.4	MDCK-transfected cells	Choi, 2012
SN-38	4	BCRP-expressing PC-6/SN2-5H vesicles	Nakatomi, 2001
SN-38 glucuronide	26	BCRP-expressing PC-6/SN2-5H vesicles	Nakatomi, 2001
Sulfasalazine^1,2,3	0.7	Caco-2 cells	Wang, 2008
Sulfasalazine^1,2,3	0.7	BCRP-expressing Sf9 vesicles	Jani, 2009
Sulfasalazine^1,2,3	0.4	Sf9 cell membranes	Bircsak, 2013
Tandutinib	4	Caco-2 cells	Yang, 2010
Topotecan	213	MDCK II-BCRP	Li, 2008
Vardenafil	14.3	MDCK-transfected cells	Choi, 2012

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
17beta-estradiol	4.8		Not applicable	Steroid Sensitivity of K562-BCRP	Imai, 2002
17beta-estradiol-3-sulfate	14		Estrone sulfate¹	BCRP-expressing vesicles from mouse lymphoma (P388) cells	Suzuki, 2003
Abacavir	385		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Afatinib	0.75		Estrone sulfate¹	polarized Caco-2 monolayer	Afatinib NDA application
Allethrin	42.5		Hoechst 33342	HEK293 cells	Chedik, 2017
Allura red	13.3		Lucifer yellow	Sf9 cell membrane vesicles	Sjostedt, 2017
Amaranth dye	2.72		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Ammonium glycyrrhizate flavoring agent	1.15		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Amprenavir	181		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Aripiprazole	3.5		Methotrexate	BCRP membrane vesicles	Nagasaka, 2012
Atazanavir	69.1		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Atorvastatin		14.3	Estrone sulfate¹	BCRP-expressing HEK293 vesicles	Hirano, 2005
Atorvastatin	0.6		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Axitinib	4.4		Topotecan	polarized MDCKII-BCRP	Reyner, 2013
Baricitinib	50		Multiple	BCRP membrane vesicles	Baricitinib NDA application
Brlliant black	6.06		Lucifer yellow	Sf9 cell membrane vesicles	Sjostedt, 2017
Carmoisine	5.38		Lucifer yellow	Sf9 cell membrane vesicles	Sjostedt, 2017
Cerivastatin		18.1	Estrone sulfate¹	BCRP-expressing HEK293 vesicles	Hirano, 2005
Chlorpropham	53.2		Hoechst 33342	HEK293 cells	Gueniche, 2020
Clopidogrel	63		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Curcumin⁴	1.6	0.7	Sulfasalazine^1,2,3	BCRP membrane vesicles	Kusuhara, 2012
Cyclosporine⁴	1.4		Basal activity	High Five insect cell crude membranes	Pawarode, 2007
Cyclosporine⁴	13.4	6.7	Estrone sulfate¹	BCRP membrane vesicles	Xia, 2007
Cyclosporine⁴		7.8	Methotrexate	BCRP membrane vesicles	Xia, 2007
Cyclosporine⁴	3.7		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Darunavir	75		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Daunomycin	59		Estrone sulfate¹	BCRP-expressing vesicles from mouse lymphoma (P388) cells	Suzuki, 2003
D&C Brown No. 1	12		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
D&C Green No. 5	2.47		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
D&C Orange No. 4	4.77		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
D&C Red No. 4	2.47		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
D&C Red No. 27	2.35		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
D&C Red No. 28	1.04		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
D&C Red No. 33	34.2		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
D&C Red No. 6	12.3		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Dehydroaripiprazole	0.52		Methotrexate	BCRP membrane vesicles	Nagasaka, 2012
Dehydroepiandrosterone sulfate	55		Estrone sulfate¹	BCRP-expressing vesicles from mouse lymphoma (P388) cells	Suzuki, 2003
Delavirdine	18.7		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Diclofenac	19.8		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Docusate sodium surfactant	25.4		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Efavirenz	20.6		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Elacridar	0.31		Sunitinib	polarized MDCKII-BCRP	Tang, 2012
Elacridar (GF120918)²	0.31		Mitoxantrone	HEK293-BCRP	Ahmed-Belkacem, 2005
Eltrombopag⁴	2.1		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Endosulfan	6.9		Sulfasalazine^1,2,3	Sf9 cell membranes	Bircsak, 2013
Erlotinib	0.13	0.15	Estrone sulfate¹	BCRP-expressing K562 vesicles	Noguchi, 2009
EXT Yellow No. 7	15.2		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Ezetimibe	2.9		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
FD&C Blue No. 1	1.97		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
FD&C Red No. 3	0.56		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
FD&C Red No. 40	4.42		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
FD&C Yellow No. 5	5.61		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
FD&C Yellow No. 6	14.1		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Fenofibrate	170		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Fluvastatin		5.43	Estrone sulfate¹	BCRP-expressing HEK293 vesicles	Hirano, 2005
Fluvastatin	1.1		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Fostamatinib	0.05		Estrone sulfate¹	BCRP membrane vesicles	Elsby, 2016
Fumitremorgin C²	0.25	0.55	Estrone sulfate¹	BCRP-expressing K562 vesicles	Noguchi, 2009
Fumitremorgin C²	0.47		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Gefitinib	1.01		Topotecan	Transfected K562-BCRP	Yanase, 2004
Guinea green b	2.99		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Hoechst 33342	3.1		Sulfasalazine^1,2,3	Sf9 cell membranes	Bircsak, 2013
Indigotindisulfonate sodium	27.8		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Ivermectin	2.8	1.4	Estrone sulfate¹	BCRP membrane vesicles	Jani, 2011
Ko143²	0.013		Estrone sulfate¹	BCRP membrane vesicles	Xia, 2007
Ko143²	0.01		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Ko143²	0.4		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Lansoprazole	14.4		Methotrexate	BCRP membrane vesicles	Suzuki, 2009
Lapatinib	0.025		Cimetidine	polarized MDCKII-BCRP	Lee, 2015
Leflunomide	1.86		Methotrexate	BCRP membrane vesicles	Kis, 2009
Light green CF yellowish	1		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Lopinavir	7.66		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Lopinavir	8.7		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Losartan	4.8		Cholecystokinin octapeptide	BCRP membrane vesicles	Yee, 2021
Naphthol blue black	4.34		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Nelfinavir	13.5		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Neohesperidin dihydrochalcone	0.86		Lucifer yellow	Sf9 cell membrane vesicles	Sjostedt, 2017
Nifedipine	10.7		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Nilotinib		0.69	Methotrexate	BCRP-expressing HEK293 vesicles	Tiwari, 2009
Novobiocin²	1.4		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Omeprazole	17		Methotrexate	BCRP membrane vesicles	Suzuki, 2009
o,p'-DDT	10.4		Sulfasalazine^1,2,3	Sf9 cell membranes	Bircsak, 2013
Pantoprazole	5.5		Methotrexate	BCRP membrane vesicles	Suzuki, 2009
Pantoprazole	9.6		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Permethrin	7		Sulfasalazine^1,2,3	Sf9 cell membranes	Bircsak, 2013
Pitavastatin		2.92	Estrone sulfate¹	BCRP-expressing HEK293 vesicles	Hirano, 2005
Ponceau 3R	7.12		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Ponceau xylidine	2.12		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
p,p'-DDD	3		Sulfasalazine^1,2,3	Sf9 cell membranes	Bircsak, 2013
p,p'-DDE	4		Sulfasalazine^1,2,3	Sf9 cell membranes	Bircsak, 2013
p,p'-DDT	5		Sulfasalazine^1,2,3	Sf9 cell membranes	Bircsak, 2013
Prazosin¹	10		Methotrexate	BCRP membrane vesicles	Saito, 2006
Quercetin	0.6		Methotrexate	BCRP membrane vesicles	Saito, 2006
Quizartinib (AC220)	0.5		Pheophorbide A	Transfected K562-BCRP	Bhullar, 2013
Rabeprazole	8.5		Methotrexate	BCRP membrane vesicles	Suzuki, 2009
Remdesivir	25		Cholecystokinin octapeptide	BCRP membrane vesicles	Yee, 2021
Resmethrin	5.6		Sulfasalazine^1,2,3	Sf9 cell membranes	Bircsak, 2013
Rhodamine B	7.78		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Rilpivirine	1.5		Pheophorbide A	polarized MDCKII-BCRP	Weiss, 2013
Rosuvastatin³		15.4	Estrone sulfate¹	BCRP-expressing HEK293 vesicles	Hirano, 2005
Saquinavir	27.4		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
Sildenafil	3.1		Cholecystokinin octapeptide	BCRP membrane vesicles	Yee, 2021
Simvastatin		18	Estrone sulfate¹	BCRP-expressing HEK293 vesicles	Hirano, 2005
Sirolimus	1.53		Basal activity	High Five insect cell crude membranes	Pawarode, 2007
SN-38	1.6		Estrone sulfate¹	BCRP-expressing vesicles from mouse lymphoma (P388) cells	Suzuki, 2003
Sodium lauryl sulfate surfactant	27.1		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Sucrose monolaurate	57.5		Cholecystokinin octapeptide	BCRP membrane vesicles	Zou, 2020
Sulfasalazine^1,2,3	0.73		Estrone sulfate¹	BCRP-expressing oocytes	Elsby, 2011
Sulfasalazine^1,2,3	0.61		Estrone sulfate¹	BCRP membrane vesicles	Elsby, 2016
Sulfasalazine^1,2,3	2.9		Rosuvastatin³	polarized Caco-2 monolayer	Elsby, 2016
Sunitinib	0.64	0.32	Estrone sulfate¹	BCRP membrane vesicles	Kawahara, 2010
Sunset yellow	10.6		Lucifer yellow	Sf9 cell membrane vesicles	Sjostedt, 2017
Tacrolimus	2.1		Basal activity	High Five insect cell crude membranes	Pawarode, 2007
Tacrolimus	6		Methotrexate	BCRP membrane vesicles	Saito, 2006
Tartrazine	23.5		Lucifer yellow	Sf9 cell membrane vesicles	Sjostedt, 2017
Teriflunomide	0.093		Methotrexate	BCRP membrane vesicles	Kis, 2009
Tetramethrin	72.5		Hoechst 33342	HEK293 cells	Chedik, 2017
Trametinib	1.1		Cimetidine	polarized MDCKII-BCRP	Trametinib NDA application
Vismodegib	2.4		Prazosin¹	polarized MDCKII-BCRP	Vismodegib NDA application

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	Rosuvastatin³	3.1	7.0	ND	ND	ND	ND	Busti, 2008	DDI 1
2	OATP1B1/OATP1B3 (ABCB1/ABCG2)	Atazanavir/ritonavir	Glecaprevir	6.53	4.51	ND	ND	ND	ND	Yu, 2019	DDI 2
3	ABCG2	Curcumin⁴	Sulfasalazine^1,2,3	3.2	3.72	ND	3.24	ND		Kusuhara, 2012	DDI 3
4	ABCB1/ABCG2/OATP1B1/OATP1B3	Cyclosporine⁴	Glecaprevir	5.08	4.51	ND	ND	ND	ND	Yu, 2019	DDI 4
5	ABCG2/OATPs	Cyclosporine⁴	Pitavastatin	4.6	6.6	ND	ND	ND	ND	Livalo Drug Label	DDI 5
6	ABCG2/OATPs	Cyclosporine⁴	Rosuvastatin³	5.0	10.6	ND	ND	ND	ND	Simonson, 2004	DDI 6
7	ABCG2/OATPs	Cyclosporine⁴	Rosuvastatin³	6.4	18.2	ND	ND	ND	ND	Simonson, 2004	DDI 7
8	ABCB1/ABCG2/OATP1B1/OATP1B3	Cyclosporine⁴	Voxilaprevir	9.73	14.29	ND	ND	ND	ND	Yu, 2019	DDI 8
9	ABCG2/OATP1B1/OATP1B3	Darolutamide	Rosuvastatin³	~5	~5	NS	ND	NS	ND	Zurth, 2019	DDI 9
10	ABCB1/ABCG2	Elacridar (GF120918)²	Topotecan	2.4	2.8	ND	ND	NS	ND	Kruijtzer, 2002	DDI 10
11	ABCG2/OATP1B1	Eltrombopag⁴	Rosuvastatin³	1.55	2.03	ND	ND	ND	ND	Allred, 2011	DDI 11
12	ABCG2/OATP	Elvitegravir + Cobicistat	Rosuvastatin³	1.38	1.89	ND	ND	ND		Custodio, 2014	DDI 12
13	ABCG2/OATP1B1	Fostamatinib	Rosuvastatin³	1.96	1.88	ND	ND	ND		Martin, 2016	DDI 13
14	OATs/BCRP	Isavuconazole	Methotrexate	0.97	0.89	ND	ND	ND	ND	Yamazaki, 2017	DDI 14
15	ABCG2	Pantoprazole	Sulfasalazine^1,2,3	1	1	ND	ND	1		Adkison, 2010	DDI 15
16	ABCG2/OATP1B1	Rifampicin	Rosuvastatin³	4.09	9.39	ND	ND	NS	ND	Prueksaritanont, 2014	DDI 16
17	ABCG2/OATP	Tipranavir + Ritonavir	Rosuvastatin³	1.37	2.23	ND	ND	ND		Pham, 2009	DDI 17
18	ABCG2/OATP1B1/OATP1B3	Voxilaprevir	Rosuvastatin³	7.35	17.96	ND	ND	ND	ND	Yu, 2019	DDI 18

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