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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
Liver* Mean across all PMT Samples    1.555
Kidney* Mean across all PMT Samples    0.739
Note that relative expression values should only be compared between entries of the same source.

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In Vitro Substrates

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Substrate Km (μM) Cell System Reference
4-methylumbelliferone sulfate 12.9 BCRP-expressing vesicles from mouse lymphoma (P388) cells Suzuki, 2003
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
Estradiol-17beta-glucuronide 44.2 BCRP-expressing HEK293 vesicles Chen, 2003
Estrone 3-sulfate 6.8 BCRP-expressing K562 vesicles Imai, 2003
Estrone 3-sulfate 16.6 BCRP-expressing vesicles from mouse lymphoma (P388) cells Suzuki, 2003
Hematoporphyrin 17.8 BCRP-expressing Sf9 vesicles Tamura, 2006
Imatinib ND Intracellular accumulation in BCRP-expressing HEK293 cells inhbited with Ko-143 Burger, 2004
Methotrexate 681 BCRP-expressing MCF7/MX vesicles Volk, 2003
Methotrexate 1340 BCRP-expressing HEK293 vesicles Chen, 2003
Methotrexate 1410 BCRP-expressing HEK293 vesicles Tiwari, 2009
Mitoxantrone 7 ATP hydrolysis assay of BCRP-expressing Sf9 vesicles Ozvegy, 2001
Pitavastatin* 5.73 BCRP-expressing HEK293 vesicles Hirano, 2005
Rosuvastatin* 2.02 BCRP-expressing HEK293 vesicles Kitamura, 2008
Rosuvastatin* 10.1 MDCK II-BCRP Deng, 2008
SN-38 4.0 BCRP-expressing PC-6/SN2-5H vesicles Nakatomi, 2001
SN-38 glucuronide 26 BCRP-expressing PC-6/SN2-5H vesicles Nakatomi, 2001
Sulfasalazine 0.7 BCRP-expressing Sf9 vesicles Jani, 2009
Topotecan 213 MDCK II-BCRP Li, 2008

ND = not determined


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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
17beta-estradiol 4.8 Steroid Sensitivity of K562-BCRP Imai, 2002
17beta-estradiol-3-sulfate 14 Estrone 3-sulfate BCRP-expressing vesicles from mouse lymphoma (P388) cells Suzuki, 2003
Abacavir 385 Pheophorbide A MDCK II-BCRP Weiss, 2007
Amprenavir 181 Pheophorbide A MDCK II-BCRP Weiss, 2007
Atazanavir 69.1 Pheophorbide A MDCK II-BCRP Weiss, 2007
Atorvastatin 14.3 Estrone 3-sulfate BCRP-expressing HEK293 vesicles Hirano, 2005
Cerivastatin 18.1 Estrone 3-sulfate BCRP-expressing HEK293 vesicles Hirano, 2005
Daunomycin 59 Estrone 3-sulfate BCRP-expressing vesicles from mouse lymphoma (P388) cells Suzuki, 2003
Dehydroepiandrosterone sulfate 55 Estrone 3-sulfate BCRP-expressing vesicles from mouse lymphoma (P388) cells Suzuki, 2003
Delavirdine 18.7 Pheophorbide A MDCK II-BCRP Weiss, 2007
Efavirenz 20.6 Pheophorbide A MDCK II-BCRP Weiss, 2007
Elacridar (GF120918) 0.31 Mitoxantrone HEK293-BCRP Ahmed-Belkacem, 2005
Erlotinib 0.13 0.15 Estrone 3-sulfate BCRP-expressing K562 vesicles Noguchi, 2009
Fluvastatin 5.43 Estrone 3-sulfate BCRP-expressing HEK293 vesicles Hirano, 2005
Fumitremorgin C 0.25 0.55 Estrone 3-sulfate BCRP-expressing K562 vesicles Noguchi, 2009
Fumitremorgin C 0.47 Pheophorbide A MDCK II-BCRP Weiss, 2007
Ko143 0.01 Pheophorbide A MDCK II-BCRP Weiss, 2007
Lopinavir 7.66 Pheophorbide A MDCK II-BCRP Weiss, 2007
Nelfinavir 13.5 Pheophorbide A MDCK II-BCRP Weiss, 2007
Nilotinib 0.69 Methotrexate BCRP-expressing HEK293 vesicles Tiwari, 2009
Pitavastatin 2.92 Estrone 3-sulfate BCRP-expressing HEK293 vesicles Hirano, 2005
Rosuvastatin 15.4 Estrone 3-sulfate BCRP-expressing HEK293 vesicles Hirano, 2005
Saquinavir 27.4 Pheophorbide A MDCK II-BCRP Weiss, 2007
Simvastatin 18 Estrone 3-sulfate BCRP-expressing HEK293 vesicles Hirano, 2005
SN-38 1.6 Estrone 3-sulfate BCRP-expressing vesicles from mouse lymphoma (P388) cells Suzuki, 2003
Sulfasalazine 0.73 Estrone 3-sulfate BCRP-expressing oocytes Elsby, 2011

ND = not determined


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Clinical Drug-Drug Interactions

DDI Implicated Transporter Interacting Drug Affected Drug AUC Cmax CLR CL/F t1/2 Effect on PD Reference More Details
Clinical PK Impact(fold change)
1 ABCG2/OATPs Atazanavir / Ritonavir Rosuvastatin 3.1 7.0 ND ND ND ND Busti, 2008 DDI 1
2 ABCG2/OATPs Cyclosporine Pitavastatin 4.6 6.6 ND ND ND ND Livalo Drug Label DDI 2
3 ABCG2/OATPs Cyclosporine Rosuvastatin 5.0 10.6 ND ND ND ND Simonson, 2004 DDI 3
4 ABCG2/OATPs Cyclosporine Rosuvastatin 6.4 18.2 ND ND ND ND Simonson, 2004 DDI 4
5 ABCB1/ABCG2 Elacridar (GF120918) Topotecan 2.4 2.8 ND ND NS ND Kruijtzer, 2002 DDI 5

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


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