General Information of DTP (ID: DTI7UX6)

DTP Name Breast cancer resistance protein (ABCG2) DTP Info
Gene Name BCRP

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
127 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Abacavir DMMN36E Human immunodeficiency virus infection 1C62 Approved [1]
Aciclovir DMYLOVR Genital herpes 1A94 Approved [2]
Adefovir DMM278X N. A. N. A. Approved [3]
Alfuzosin DMZVMKF Benign prostatic hyperplasia GA90 Approved [4]
Apixaban DM89JLN Thrombosis DB61-GB90 Approved [5]
ARRY-162 DM1P6FR Melanoma 2C30 Approved [6]
Baricitinib DM4ONW5 Rheumatoid arthritis FA20 Approved [7]
BIBW 2992 DMTKD7Q Non-small-cell lung cancer 2C25.Y Approved [8]
Bicalutamide DMZMSPF Prostate cancer 2C82.0 Approved [9]
Brigatinib DM7W94S Anaplastic large cell lymphoma 2A90.A Approved [10]
Bupropion DM5PCS7 Depression 6A70-6A7Z Approved [11]
Canagliflozin DMFRM1I Non-insulin dependent diabetes 5A11 Approved [12]
Cephalothin Sodium DM51Z9E Bacterial infection 1A00-1C4Z Approved [13]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [14]
Chlorothiazide DMLHESP Chronic heart failure BD1Z Approved [15]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [16]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [14]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [17]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [18]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [19]
Cladribine DM3JDRP Hairy cell leukaemia 2A82.2 Approved [20]
Clofarabine DMCVJ86 Acute lymphoblastic leukaemia 2A85 Approved [20]
Dabrafenib DMX6OE3 Melanoma 2C30 Approved [21]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [22]
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [23]
Daunorubicin DMQUSBT Acute monocytic leukemia Approved [24]
Dehydroepiandrosterone sulfate DM4Q80H N. A. N. A. Approved [25]
Delavirdine DM3NF5G Human immunodeficiency virus infection 1C62 Approved [14]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [13]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [26]
Dipyridamole DMXY30O Atrial fibrillation BC81.3 Approved [27]
Dirithromycin DM0D9YJ Bacterial infection 1A00-1C4Z Approved [13]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [28]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [29]
Eltrombopag DMOGFIX Thrombocytopenia 3B64 Approved [30]
Empagliflozin DMRF9YK Type-1 diabetes 5A10 Approved [31]
Entacapone DMLBVKQ Parkinson disease 8A00.0 Approved [32]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [33]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [14]
Erlotinib DMCMBHA Adrenal gland neoplasm Approved [34]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [27]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [35]
Estrone sulfate DMVBIZL Atrophic vaginitis GA30.2 Approved [36]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [37]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [38]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [39]
Fluvastatin DM4MDJY Arteriosclerosis BD40 Approved [40]
Folic Acid DMEMBJC Colorectal carcinoma Approved [41]
Ganciclovir DM1MBYQ Cytomegalovirus infection 1D82 Approved [42]
Gefitinib DM15F0X Colon adenocarcinoma Approved [14]
Glibenclamide DM8JXPZ Diabetic complication 5A2Y Approved [43]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [44]
Grepafloxacin DMGLX0T Chronic bronchitis CA20.1 Approved [45]
Hesperetin DMKER83 High blood cholesterol level 5C80.00 Approved [46]
Hydroxychloroquine DMSIVND Chronic renal failure GB61.Z Approved [47]
Idarubicin DMM0XGL Acute myelogenous leukaemia 2A41 Approved [48]
Idelalisib DM602WT Chronic lymphocytic leukaemia 2A82.0 Approved [49]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [50]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [51]
Lamivudine DMI347A Chronic HBV infection 1E51.0Z Approved [52]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [53]
Leflunomide DMR8ONJ Arthritis FA20 Approved [54]
Lopinavir DMITQS0 Human immunodeficiency virus infection 1C62 Approved [14]
Menadione DMSJDTY Vitamin K deficiency 5B59 Approved [55]
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [3]
Metformin DM89QE1 Colorectal carcinoma Approved [56]
Methotrexate DM2TEOL Anterior urethra cancer Approved [57]
Mitoxantrone DMM39BF Acute myelogenous leukaemia 2A41 Approved [24]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [58]
Nicardipine DMCDYW7 High blood pressure BA00 Approved [14]
Nifurtimox DMSQLZJ Chagas disease IF53 Approved [59]
Nilotinib DM7HXWT Chronic myelogenous leukaemia 2A20.0 Approved [23]
Nitrofurantoin DM7PQIK Urinary tract infection GC08 Approved [60]
Norfloxacin DMIZ6W2 Acute gonococcal cervicitis Approved [61]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [14]
Olmesartan medoxomil DMWBHRY High blood pressure BA00 Approved [31]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [62]
Paclitaxel DMLB81S Breast carcinoma Approved [28]
Palbociclib DMD7L94 Breast cancer 2C60-2C65 Approved [63]
Pantoprazole DMSVOCZ Gastrinoma 2C10.1 Approved [64]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [65]
Pemetrexed DMMX2E6 Central nervous system lymphoma 2B33.5 Approved [66]
Pirarubicin DMGTW1I Breast cancer 2C60-2C65 Approved [39]
Pitavastatin DMJH792 Hypercholesterolaemia 5C80.0 Approved [27]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [67]
Ponatinib DMYGJQO Acute lymphoblastic leukaemia 2A85 Approved [68]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [69]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [14]
Prazosin DMCD9YG Benign prostatic hyperplasia GA90 Approved [70]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [35]
Pyrimethamine DM5X7VY Malaria 1F40-1F45 Approved [71]
Quercetin DM3NC4M Obesity 5B81 Approved [14]
Rabeprazole DMMZXIW Bacterial infection 1A00-1C4Z Approved [72]
Raltitrexed DMT9K8G Rectal adenocarcinoma 2B92 Approved [73]
Regorafenib DMHSY1I Gastrointestinal stromal tumour 2B5B Approved [31]
Reserpine DM6VM38 Hypertension BA00-BA04 Approved [14]
Riboflavin DM8YMWE Acne vulgaris ED80 Approved [74]
Rifampin DMA8J1G Tuberculosis 1B10-1B1Z Approved [13]
Riluzole DMECBWN Amyotrophic lateral sclerosis 8B60.0 Approved [75]
Riociguat DMXBLMP Chronic thromboembolic pulmonary hypertension Approved [31]
Rivaroxaban DMQMBZ1 Deep vein thrombosis BD71 Approved [76]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [77]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [78]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [79]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [69]
Sofosbuvir DMQI86A Hepatitis C 1E51 Approved [31]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [80]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [81]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [80]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [82]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [83]
Teniposide DMLW57T Acute lymphoblastic leukaemia 2A85 Approved [14]
Tenofovir DM1IS6U Chronic hepatitis B virus infection Approved [31]
Tenofovir alafenamide DMTQF4A Hiv infectious disease Approved [84]
Teriflunomide DMQ2FKJ Hyperlipidaemia 5C80 Approved [47]
Testosterone DM7HUNW Hot flushes GA30 Approved [85]
Tetracycline DMZA017 Acne vulgaris ED80 Approved [13]
Thioguanine DM7NKEV Acute lymphocytic leukaemia 2B33.3 Approved [3]
Topotecan DMP6G8T Central nervous system neoplasm Approved [86]
Trimetrexate DMDEA85 Toxoplasmosis 1F57 Approved [71]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [87]
Verteporfin DMIY6DB Choroidal neovascularization 9B76 Approved [88]
Vinblastine DM5TVS3 Advanced cancer 2A00-2F9Z Approved [28]
Vincristine DMINOX3 Acute lymphoblastic leukaemia 2A85 Approved [71]
VRX496 DMIO4V5 Acquired immune deficiency syndrome 1C62.3 Approved [14]
YN-968D1 DMMP3Y2 Breast cancer 2C60-2C65 Approved [89]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [14]
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⏷ Show the Full List of 127 Approved Drug(s)
29 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Camptothecin DM6CHNJ Solid tumour/cancer 2A00-2F9Z Phase 3 [90]
Edotecarin DM3ZL7D Gastric adenocarcinoma 2B72 Phase 3 [73]
Exatecan DMCA7FN Solid tumour/cancer 2A00-2F9Z Phase 3 [73]
Karenitecin DMCRGY4 Lung cancer 2C25.0 Phase 3 [73]
Nolatrexed DMOF0CA Solid tumour/cancer 2A00-2F9Z Phase 3 [71]
Resveratrol DM3RWXL Giant cell arteritis 4A44.2 Phase 3 [41]
Synthetic hypericin DMXU4ON Virus infection 1A24-1D9Z Phase 3 [91]
Genistein DM0JETC Menopause symptom GA30.0 Phase 2/3 [92]
9-AMINOCAMPTOTHECIN DMQXYRG Acquired immune deficiency syndrome 1C62.3 Phase 2 [73]
Bisantrene DMW76V0 N. A. N. A. Phase 2 [73]
CKD602 DMW9F1G Solid tumour/cancer 2A00-2F9Z Phase 2 [93]
CP-724714 DMUJ0W7 Lymphoma 2A80-2A86 Phase 2 [94]
DIFLOMOTECAN DM20ATW Solid tumour/cancer 2A00-2F9Z Phase 2 [73]
Flavopiridol DMKSUOI Acute myeloid leukaemia 2A60 Phase 2 [95]
Gimatecan DMSKMET Breast cancer 2C60-2C65 Phase 2 [73]
HPPH DM25PQB N. A. N. A. Phase 2 [96]
LE-SN38 DMW50NF Colorectal cancer 2B91.Z Phase 2 [97]
NSC-645809 DMPJQZG Breast cancer 2C60-2C65 Phase 2 [98]
Ortataxel DM1EK5D Solid tumour/cancer 2A00-2F9Z Phase 2 [14]
Oxfendazole DMSNL51 N. A. N. A. Phase 2 [99]
PEITC DMOMN31 Prostate cancer 2C82.0 Phase 2 [25]
PIRITREXIM DM276N1 Bladder cancer 2C94 Phase 2 [71]
UCN-01 DMUNJZB Non-small-cell lung cancer 2C25.Y Phase 2 [73]
BN-2629 DMA9MP5 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [100]
Taurocholic Acid DM2LZ8F Type-2 diabetes 5A11 Phase 1/2 [16]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [25]
Benzoylphenylurea DMMW4HV N. A. N. A. Phase 1 [101]
Mycophenolic acid glucuronide DM5O4X9 N. A. N. A. Phase 1 [58]
Sphingosine-1-phosphate DMJCQKA Acne vulgaris ED80 Phase 1 [102]
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⏷ Show the Full List of 29 Clinical Trial Drug(s)
7 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Parabis DMDKXYC N. A. N. A. Withdrawn from market [103]
BECATECARIN DMRQV8I Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 3 [104]
Befloxatone DMZIV6D Major depressive disorder 6A70.3 Discontinued in Phase 3 [105]
E-3040 DM35KZG Thrombosis DB61-GB90 Discontinued in Phase 2 [106]
Lurtotecan DMF1RTW Ovarian cancer 2C73 Discontinued in Phase 2 [25]
NB-506 DMGVYXB Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [73]
Rhodamine-123 DMQAK6T Prostate cancer 2C82.0 Discontinued in Phase 1 [107]
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⏷ Show the Full List of 7 Discontinued Drug(s)
9 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Azidothymidine monophosphate DM3FLMR N. A. N. A. Preclinical [106]
Barasertib-hQPA DMTJZIL N. A. N. A. Preclinical [108]
BMS 536924 DMDJH2L N. A. N. A. Preclinical [109]
Enrofloxacin DMK6WIO N. A. N. A. Preclinical [110]
Homocamptothecin DMBQDA3 N. A. N. A. Preclinical [111]
N-desethyl sunitinib DM5ATJ0 N. A. N. A. Preclinical [112]
Pancratistatin DM3YUGA N. A. N. A. Preclinical [113]
Puromycin DMDKLB5 N. A. N. A. Preclinical [25]
Scutellarin DMJT1E5 N. A. N. A. Preclinical [114]
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⏷ Show the Full List of 9 Preclinical Drug(s)
14 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Butanoic Acid DMTAJP7 Discovery agent N.A. Investigative [115]
Cholesterol DMR3J6S Discovery agent N.A. Investigative [35]
Chrysin DM7V2LG Discovery agent N.A. Investigative [14]
COUMESTROL DM40TBU Discovery agent N.A. Investigative [116]
daidzein DMRFTJX Discovery agent N.A. Investigative [116]
glycocholic acid DM0SXNM Discovery agent N.A. Investigative [16]
Hematoporphyrin DMVK36Q N. A. N. A. Investigative [117]
JNJ-7706621 DMHTYBS Discovery agent N.A. Investigative [118]
Mepacrine DMU8L7C Discovery agent N.A. Investigative [13]
phosphatidylserine DM76TSG Discovery agent N.A. Investigative [119]
Protoporphyrin IX DMWYE7A Discovery agent N.A. Investigative [73]
Tyrphostin ag-1478 DM87ZIH Discovery agent N.A. Investigative [19]
uric acid DMA1MKT Discovery agent N.A. Investigative [120]
[3H]estradiol-17beta-glucuronide DM3KJ45 Discovery agent N.A. Investigative [121]
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⏷ Show the Full List of 14 Investigative Drug(s)
Molecule Interaction Atlas

References

1 QSAR analysis and molecular modeling of ABCG2-specific inhibitors. Adv Drug Deliv Rev. 2009 Jan 31;61(1):34-46.
2 Acyclovir is a substrate for the human breast cancer resistance protein (BCRP/ABCG2): implications for renal tubular transport and acyclovir-induced nephrotoxicity. Can J Physiol Pharmacol. 2011 Sep;89(9):675-80.
3 ABC transporters and their role in nucleoside and nucleotide drug resistance. Biochem Pharmacol. 2012 Apr 15;83(8):1073-83.
4 In vitro and in vivo evidence for the importance of breast cancer resistance protein transporters (BCRP/MXR/ABCP/ABCG2). Handb Exp Pharmacol. 2011;(201):325-71.
5 Characterization of efflux transporters involved in distribution and disposition of apixaban. Drug Metab Dispos. 2013 Apr;41(4):827-35.
6 The impact of P-glycoprotein and breast cancer resistance protein on the brain pharmacokinetics and pharmacodynamics of a panel of MEK inhibitors. Int J Cancer. 2018 Jan 15;142(2):381-391.
7 Differential Influence of the Antiretroviral Pharmacokinetic Enhancers Ritonavir and Cobicistat on Intestinal P-Glycoprotein Transport and the Pharmacokinetic/Pharmacodynamic Disposition of Dabigatran. Antimicrob Agents Chemother. 2017 Oct 24;61(11). pii: e01201-17.
8 Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation. Pharmacol Res. 2017 Jun;120:43-50.
9 Effects of the ABCG2 and ABCB1 drug transporter polymorphisms on the pharmacokinetics of bicalutamide in humans. Clin Chim Acta. 2015 Jan 1;438:7-11.
10 NDA/BLA Multidisciplinary Review and Evaluation of ALUNBRIG (brigatinib) From FDA.
11 Role of transporter-mediated efflux in the placental biodisposition of bupropion and its metabolite, OH-bupropion. Biochem Pharmacol. 2010 Oct 1;80(7):1080-6.
12 In vitro and physiologically-based pharmacokinetic based assessment of drug-drug interaction potential of canagliflozin. Br J Clin Pharmacol. 2017 May;83(5):1082-1096.
13 Arginine-482 is not essential for transport of antibiotics, primary bile acids and unconjugated sterols by the human breast cancer resistance protein (ABCG2). Biochem J. 2005 Jan 15;385(Pt 2):419-26.
14 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
15 ABCG2 modulates chlorothiazide permeability--in vitro-characterization of its interactions. Drug Metab Pharmacokinet. 2012;27(3):349-53.
16 Characterization of the role of ABCG2 as a bile acid transporter in liver and placenta. Mol Pharmacol. 2012 Feb;81(2):273-83.
17 Progesterone acts via progesterone receptors A and B to regulate breast cancer resistance protein expression. Mol Pharmacol. 2008 Mar;73(3):613-5.
18 Fluoroquinolone efflux mediated by ABC transporters. J Pharm Sci. 2008 Sep;97(9):3483-93.
19 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
20 Contribution of the drug transporter ABCG2 (breast cancer resistance protein) to resistance against anticancer nucleosides. Mol Cancer Ther. 2008 Sep;7(9):3092-102.
21 Mechanisms limiting distribution of the threonine-protein kinase B-RaF(V600E) inhibitor dabrafenib to the brain: implications for the treatment of melanoma brain metastases. J Pharmacol Exp Ther. 2013 Mar;344(3):655-64.
22 Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. Mol Pharmacol. 2003 Jan;63(1):65-72.
23 Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64.
24 Functional characterization of the human multidrug transporter, ABCG2, expressed in insect cells. Biochem Biophys Res Commun. 2001 Jul 6;285(1):111-7.
25 A prediction model of substrates and non-substrates of breast cancer resistance protein (BCRP) developed by GA-CG-SVM method. Comput Biol Med. 2011 Nov;41(11):1006-13.
26 Transport of diclofenac by breast cancer resistance protein (ABCG2) and stimulation of multidrug resistance protein 2 (ABCC2)-mediated drug transport by diclofenac and benzbromarone. Drug Metab Dispos. 2009 Jan;37(1):129-36.
27 ABCG2: a perspective. Adv Drug Deliv Rev. 2009 Jan 31;61(1):3-13.
28 Ixabepilone, a novel microtubule-targeting agent for breast cancer, is a substrate for P-glycoprotein (P-gp/MDR1/ABCB1) but not breast cancer resistance protein (BCRP/ABCG2). J Pharmacol Exp Ther. 2011 May;337(2):423-32.
29 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
30 Assessment of the pharmacokinetic interaction between eltrombopag and lopinavir-ritonavir in healthy adult subjects. Antimicrob Agents Chemother. 2012 Jun;56(6):2846-51.
31 KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01913)
32 Elucidation of the Impact of P-glycoprotein and Breast Cancer Resistance Protein on the Brain Distribution of Catechol-O-Methyltransferase Inhibitors. Drug Metab Dispos. 2017 Dec;45(12):1282-1291.
33 Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir. Drug Metab Dispos. 2017 Mar;45(3):269-278.
34 Functions of the breast cancer resistance protein (BCRP/ABCG2) in chemotherapy. Adv Drug Deliv Rev. 2009 Jan 31;61(1):26-33.
35 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
36 ABCG2 transports sulfated conjugates of steroids and xenobiotics. J Biol Chem. 2003 Jun 20;278(25):22644-9.
37 Characterization of 3-methoxy flavones for their interaction with ABCG2 as suggested by ATPase activity. Biochim Biophys Acta. 2014 Nov;1838(11):2929-38.
38 Complex pharmacokinetic behavior of ezetimibe depends on abcc2, abcc3, and abcg2. Drug Metab Dispos. 2009 Aug;37(8):1698-702.
39 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
40 Evaluation of the usefulness of breast cancer resistance protein (BCRP) knockout mice and BCRP inhibitor-treated monkeys to estimate the clinical impact of BCRP modulation on the pharmacokinetics of BCRP substrates. Pharm Res. 2015 May;32(5):1634-47.
41 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
42 Side populations of glioblastoma cells are less sensitive to HSV-TK/GCV suicide gene therapy system than the non-side population. In Vitro Cell Dev Biol Anim. 2010 Jun;46(6):497-501.
43 Glyburide transport across the human placenta. Obstet Gynecol. 2015 Mar;125(3):583-8.
44 Glutathione transport is a unique function of the ATP-binding cassette protein ABCG2. J Biol Chem. 2010 May 28;285(22):16582-7.
45 Involvement of breast cancer resistance protein (ABCG2) in the biliary excretion mechanism of fluoroquinolones. Drug Metab Dispos. 2007 Oct;35(10):1873-9.
46 Interaction of the breast cancer resistance protein with plant polyphenols. Biochem Biophys Res Commun. 2004 Apr 23;317(1):269-75.
47 MDR-ABC transporters: biomarkers in rheumatoid arthritis. Clin Exp Rheumatol. 2013 Sep-Oct;31(5):779-87.
48 Amonafide L-malate is not a substrate for multidrug resistance proteins in secondary acute myeloid leukemia. Leukemia. 2008 Nov;22(11):2110-5.
49 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB09054)
50 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
51 Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan. Cancer Chemother Pharmacol. 2006 Sep;58(3):374-83.
52 The effect of ABCG2 V12M, Q141K and Q126X, known functional variants in vitro, on the disposition of lamivudine. Br J Clin Pharmacol. 2007 Nov;64(5):645-54.
53 The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions. Drug Metab Dispos. 2008 Apr;36(4):695-701.
54 Leflunomide and its metabolite A771726 are high affinity substrates of BCRP: implications for drug resistance. Ann Rheum Dis. 2009 Jul;68(7):1201-7.
55 The naphthoquinones, vitamin K3 and its structural analogue plumbagin, are substrates of the multidrug resistance linked ATP binding cassette drug transporter ABCG2. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3279-86.
56 Role of human placental apical membrane transporters in the efflux of glyburide, rosiglitazone, and metformin. Am J Obstet Gynecol. 2010 Apr;202(4):383.e1-7.
57 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
58 Influence of drug transporters and UGT polymorphisms on pharmacokinetics of phenolic glucuronide metabolite of mycophenolic acid in Japanese renal transplant recipients. Ther Drug Monit. 2008 Oct;30(5):559-64.
59 The transport of nifurtimox, an anti-trypanosomal drug, in an in vitro model of the human blood-brain barrier: evidence for involvement of breast cancer resistance protein. Brain Res. 2012 Feb 3;1436:111-21.
60 The breast cancer resistance protein (BCRP/ABCG2) affects pharmacokinetics, hepatobiliary excretion, and milk secretion of the antibiotic nitrofurantoin. Mol Pharmacol. 2005 May;67(5):1758-64.
61 Breast cancer resistance protein (BCRP/ABCG2) transports fluoroquinolone antibiotics and affects their oral availability, pharmacokinetics, and milk secretion. Drug Metab Dispos. 2006 Apr;34(4):690-5.
62 Effect of ABCG2 on cytotoxicity of platinum drugs: interference of EGFP. Toxicol In Vitro. 2008 Dec;22(8):1846-52.
63 Efflux transporters at the blood-brain barrier limit delivery and efficacy of cyclin-dependent kinase 4/6 inhibitor palbociclib (PD-0332991) in an orthotopic brain tumor model. J Pharmacol Exp Ther. 2015 Nov;355(2):264-71.
64 Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions. Cancer Res. 2004 Aug 15;64(16):5804-11.
65 Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53.
66 pH-Dependent transport of pemetrexed by breast cancer resistance protein. Drug Metab Dispos. 2011 Sep;39(9):1478-85.
67 Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin. Mol Pharmacol. 2005 Sep;68(3):800-7.
68 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB08901)
69 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
70 P-glycoprotein and breast cancer resistance protein expression and function at the blood-brain barrier and blood-cerebrospinal fluid barrier (choroid plexus) in streptozotocin-induced diabetes in rats. Brain Res. 2011 Jan 25;1370:238-45.
71 Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates. Cancer Chemother Pharmacol. 2006 Dec;58(6):826-34.
72 Co-administration of proton pump inhibitors delays elimination of plasma methotrexate in high-dose methotrexate therapy. Br J Clin Pharmacol. 2009 Jan;67(1):44-9.
73 Pharmacogenomic importance of ABCG2. Pharmacogenomics. 2008 Aug;9(8):1005-9.
74 Multidrug transporter ABCG2/breast cancer resistance protein secretes riboflavin (vitamin B2) into milk. Mol Cell Biol. 2007 Feb;27(4):1247-53.
75 Interactions between riluzole and ABCG2/BCRP transporter. Neurosci Lett. 2009 Mar 6;452(1):12-6.
76 Absence of both MDR1 (ABCB1) and breast cancer resistance protein (ABCG2) transporters significantly alters rivaroxaban disposition and central nervous system entry. Basic Clin Pharmacol Toxicol. 2013 Mar;112(3):164-70.
77 ATP-binding cassette transporters in human heart failure. Naunyn Schmiedebergs Arch Pharmacol. 2008 May;377(3):231-43.
78 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
79 Nicotine and cotinine increases the brain penetration of saquinavir in rat. J Neurochem. 2010 Dec;115(6):1495-507.
80 Double-transduced MDCKII cells to study human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) interplay in drug transport across the blood-brain barrier. Mol Pharm. 2011 Apr 4;8(2):571-82.
81 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
82 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB11760)
83 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
84 Pharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals. J Acquir Immune Defic Syndr. 2018 Aug 1;78(4):465-472.
85 Association of the ABCG2 C421A polymorphism with prostate cancer risk and survival. BJU Int. 2008 Dec;102(11):1694-9.
86 Differential inhibition of murine Bcrp1/Abcg2 and human BCRP/ABCG2 by the mycotoxin fumitremorgin C. Eur J Pharmacol. 2010 Oct 10;644(1-3):41-8.
87 Tyrosine kinase inhibitors and multidrug resistance proteins: interactions and biological consequences. Cancer Chemother Pharmacol. 2010 Jan;65(2):335-46.
88 The tyrosine kinase inhibitor imatinib mesylate enhances the efficacy of photodynamic therapy by inhibiting ABCG2. Clin Cancer Res. 2007 Apr 15;13(8):2463-70.
89 Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters. Cancer Res. 2010 Oct 15;70(20):7981-91.
90 The beta-carboline alkaloid harmine inhibits BCRP and can reverse resistance to the anticancer drugs mitoxantrone and camptothecin in breast cancer cells. Phytother Res. 2010 Jan;24(1):146-9.
91 Drug efflux transporters, MRP1 and BCRP, affect the outcome of hypericin-mediated photodynamic therapy in HT-29 adenocarcinoma cells. Photochem Photobiol Sci. 2009 Dec;8(12):1716-23.
92 Differential selectivity of efflux transporter inhibitors in Caco-2 and MDCK-MDR1 monolayers: a strategy to assess the interaction of a new chemical entity with P-gp, BCRP, and MRP2. J Pharm Sci. 2012 May;101(5):1888-97.
93 Involvement of P-glycoprotein, multidrug resistance protein 2 and breast cancer resistance protein in the transport of belotecan and topotecan in Caco-2 and MDCKII cells. Pharm Res. 2008 Nov;25(11):2601-12.
94 Multi-drug-resistance-reverting agents: 2-aryloxazole and 2-arylthiazole derivatives as potent BCRP or MRP1 inhibitors. ChemMedChem. 2009 Feb;4(2):188-95.
95 The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the MDR-associated ATP-binding cassette transporter ABCG2. Mol Cancer Ther. 2012 Sep;11(9):2033-44.
96 Substrate affinity of photosensitizers derived from chlorophyll-a: the ABCG2 transporter affects the phototoxic response of side population stem cell-like cancer cells to photodynamic therapy. Mol Pharm. 2010 Oct 4;7(5):1789-804.
97 Transport of 7-ethyl-10-hydroxycamptothecin (SN-38) by breast cancer resistance protein ABCG2 in human lung cancer cells. Biochem Biophys Res Commun. 2001 Nov 9;288(4):827-32.
98 C421 allele-specific ABCG2 gene amplification confers resistance to the antitumor triazoloacridone C-1305 in human lung cancer cells. Biochem Pharmacol. 2007 Jun 30;74(1):41-53.
99 Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (BCRP/ABCG2). Drug Metab Dispos. 2005 May;33(5):614-8.
100 Optimization of the antitumor activity of sequence-specific pyrrolobenzodiazepine derivatives based on their affinity for ABC transporters. AAPS J. 2010 Dec;12(4):617-27.
101 American Association for Cancer Research.
102 Estradiol induces export of sphingosine 1-phosphate from breast cancer cells via ABCC1 and ABCG2. J Biol Chem. 2010 Apr 2;285(14):10477-86.
103 Human and rat ABC transporter efflux of bisphenol a and bisphenol a glucuronide: interspecies comparison and implications for pharmacokinetic assessment. Toxicol Sci. 2012 Aug;128(2):317-25.
104 Becatecarin (rebeccamycin analog, NSC 655649) is a transport substrate and induces expression of the ATP-binding cassette transporter, ABCG2, in lung carcinoma cells. Cancer Chemother Pharmacol. 2009 Aug;64(3):575-83.
105 Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screening. J Nucl Med. 2011 Mar;52(3):415-23.
106 Role of the breast cancer resistance protein (ABCG2) in drug transport. AAPS J. 2005 May 11;7(1):E118-33.
107 Alectinib (CH5424802) antagonizes ABCB1- and ABCG2-mediated multidrug resistance in vitro, in vivo and ex vivo. Exp Mol Med. 2017 Mar 17;49(3):e303.
108 P-glycoprotein and breast cancer resistance protein in acute myeloid leukaemia cells treated with the aurora-B kinase inhibitor barasertib-hQPA. BMC Cancer. 2011 Jun 16;11:254.
109 Drug efflux by breast cancer resistance protein is a mechanism of resistance to the benzimidazole insulin-like growth factor receptor/insulin receptor inhibitor, BMS-536924. Mol Cancer Ther. 2011 Jan;10(1):117-25.
110 Interaction of enrofloxacin with breast cancer resistance protein (BCRP/ABCG2): influence of flavonoids and role in milk secretion in sheep. J Vet Pharmacol Ther. 2006 Aug;29(4):279-87.
111 ABCG2: determining its relevance in clinical drug resistance. Cancer Metastasis Rev. 2007 Mar;26(1):39-57.
112 P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib. J Pharmacol Exp Ther. 2012 Apr;341(1):164-73.
113 Identification of compounds that correlate with ABCG2 transporter function in the National Cancer Institute Anticancer Drug Screen. Mol Pharmacol. 2009 Nov;76(5):946-56.
114 Mechanistic studies on the absorption and disposition of scutellarin in humans: selective OATP2B1-mediated hepatic uptake is a likely key determinant for its unique pharmacokinetic characteristics. Drug Metab Dispos. 2012 Oct;40(10):2009-20.
115 The short-chain fatty acid butyrate is a substrate of breast cancer resistance protein. Am J Physiol Cell Physiol. 2011 Nov;301(5):C984-94.
116 Effect of breast cancer resistance protein (Bcrp/Abcg2) on the disposition of phytoestrogens. Mol Pharmacol. 2007 Oct;72(4):967-75.
117 Cellular phototoxicity evoked through the inhibition of human ABC transporter ABCG2 by cyclin-dependent kinase inhibitors in vitro. Pharm Res. 2009 Feb;26(2):449-58.
118 Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor. Mol Cancer Ther. 2006 Oct;5(10):2459-67.
119 ABCG2: a potential marker of stem cells and novel target in stem cell and cancer therapy. Life Sci. 2010 Apr 24;86(17-18):631-7.
120 Extra-renal elimination of uric acid via intestinal efflux transporter BCRP/ABCG2. PLoS One. 2012;7(2):e30456.
121 Regulation of the function of the human ABCG2 multidrug transporter by cholesterol and bile acids: effects of mutations in potential substrate and steroid binding sites. Drug Metab Dispos. 2014 Apr;42(4):575-85.