Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM7A8TW)

Drug Name
Ezetimibe Drug Info
Synonyms
Ezedoc; Ezetimib; Ezetrol; Zetia; Zient; Essex brand of ezetimibe; MSD brand of ezetimibe; Merck brand of ezetimibe; SCH58235; Sch 58235; Ezetimibe [USAN:INN]; Inegy (TN); MK-0653; SCH-58235; Schering-Plough brand of ezetimibe; Vytorin (TN); Zetia (TN); Zetia , Ezetrol, Ezetimibe; Ezetimibe (JAN/USAN/INN); (-)-Sch 58235; (1-(4-fluorophenyl)-(3R)-(3-(4-fluorophenyl)-(3S)-hydroxypropyl)-(4S)-(4-hydroxyphenyl)-2-azetidinone); (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one; (3R,4S)-1-(p-Fluorophenyl)-3-((3S)-3-(p-fluorophenyl)-3-hydroxypropyl)-4-(p-hydroxyphenyl)-2-azetidinone; 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-(4-hydroxyphenyl)-2-azetidione; 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone
Indication
Disease Entry ICD 11 Status REF
Atherosclerosis BD40 Approved [1]
Hypercholesterolaemia 5C80.0 Approved [2]
Hyperlipidemia 5C80.Z Approved [1]
Hyperlipidemia, familial combined, LPL related Approved [1]
Non-alcoholic fatty liver disease DB92 Approved [1]
Type-1/2 diabetes 5A10-5A11 Approved [1]
Therapeutic Class
Anticholesteremic Agents
Cross-matching ID
PubChem CID
150311
ChEBI ID
CHEMBL49040
CAS Number
CAS 163222-33-1
TTD Drug ID
DM7A8TW
VARIDT Drug ID
DR00140
INTEDE Drug ID
DR0677
ACDINA Drug ID
D00262

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Investigative Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Download the Complete Related Drug List
Drug(s) Targeting Niemann-Pick C1-like protein 1 (NPC1L1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ezetimibe-glucuronide DM5V3S7 Discovery agent N.A. Investigative [14]
Drug(s) Transported By Multidrug resistance-associated protein 2 (ABCC2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [15]
Methotrexate DM2TEOL Anterior urethra cancer Approved [16]
Folic Acid DMEMBJC Colorectal carcinoma Approved [17]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [18]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [19]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [20]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [21]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [22]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [23]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [24]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [25]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [26]
Methotrexate DM2TEOL Anterior urethra cancer Approved [27]
Folic Acid DMEMBJC Colorectal carcinoma Approved [28]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [27]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [27]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [29]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [27]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [30]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [31]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Breast cancer resistance protein (ABCG2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [32]
Methotrexate DM2TEOL Anterior urethra cancer Approved [33]
Folic Acid DMEMBJC Colorectal carcinoma Approved [34]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [35]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [36]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [37]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [38]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [37]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [39]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [40]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Organic anion transporting polypeptide 1B1 (SLCO1B1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [41]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [42]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [43]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [44]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [43]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [45]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [46]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [47]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [48]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [45]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Multidrug resistance-associated protein 3 (ABCC3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [49]
Folic Acid DMEMBJC Colorectal carcinoma Approved [50]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [51]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [52]
Glibenclamide DM8JXPZ Diabetic complication 5A2Y Approved [53]
Morphine DMRMS0L Advanced cancer 2A00-2F9Z Approved [54]
Cefadroxil DMMC345 Bacterial infection 1A00-1C4Z Approved [55]
Teniposide DMLW57T Acute lymphoblastic leukaemia 2A85 Approved [56]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [57]
Efavirenz DMC0GSJ Human immunodeficiency virus infection 1C62 Approved [58]
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Drug(s) Transported By Bile salt export pump (ABCB11)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [59]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [4]
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [4]
Taurocholic Acid DM2LZ8F Type-2 diabetes 5A11 Phase 1/2 [60]
Sodium taurocholate DM3GO0J Type-2 diabetes 5A11 Phase 1/2 [59]
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [94]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [4]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [95]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [94]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [4]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [96]
Gefitinib DM15F0X Colon adenocarcinoma Approved [94]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [97]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [94]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [98]
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Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [61]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [62]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [63]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [64]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [65]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [66]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [67]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [68]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [62]
Verapamil DMA7PEW Angina pectoris BA40 Approved [69]
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Drug(s) Metabolized By UDP-glucuronosyltransferase 1A1 (UGT1A1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [70]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [71]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [72]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [73]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [74]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [75]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [76]
Metronidazole DMTIVEN Abscess Approved [77]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [78]
Ethanol DMDRQZU Chronic pain MG30 Approved [79]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By UDP-glucuronosyltransferase 2B7 (UGT2B7)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [80]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [81]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [69]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [82]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [83]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [69]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [84]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [85]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [86]
Losartan DM72JXH Diabetic kidney disease GB61.Z Approved [69]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By UDP-glucuronosyltransferase 1A3 (UGT1A3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [87]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [75]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [69]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [88]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [89]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [84]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [85]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [86]
Losartan DM72JXH Diabetic kidney disease GB61.Z Approved [69]
Naproxen DMZ5RGV Bursitis Approved [90]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By UDP-glucuronosyltransferase 2B15 (UGT2B15)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [91]
Lorazepam DM84ZXF Absence epilepsy Approved [92]
Hydroxybenzo[a]pyrene DMFSKYE N. A. N. A. Investigative [93]
Hydroxybenzo(a)pyrene DM9H5EN N. A. N. A. Investigative [93]
BRN-1980310 DMOTU4P N. A. N. A. Investigative [93]
Drug(s) Affected By Phospholipid-transporting ATPase ABCA1 (ABCA1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [99]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [100]
Quercetin DM3NC4M Obesity 5B81 Approved [101]
Fluoxetine DM3PD2C Bipolar depression Approved [102]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [103]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [104]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [105]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [106]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [107]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [108]
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Drug(s) Affected By Sterol regulatory element-binding protein 2 (SREBF2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [109]
Selenium DM25CGV N. A. N. A. Approved [110]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [111]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [103]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [112]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [113]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [114]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [115]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [116]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [115]
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Drug(s) Affected By NPC1-like intracellular cholesterol transporter 1 (NPC1L1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [117]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [118]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [119]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [120]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [121]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [122]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [123]
PMID28870136-Compound-52 DMFDERP N. A. N. A. Patented [124]
bisphenol A DM2ZLD7 Discovery agent N.A. Investigative [125]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Niemann-Pick C1-like protein 1 (NPC1L1) TTPD1CN NPCL1_HUMAN Inhibitor [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Bile salt export pump (ABCB11) DTJ0EW4 ABCBB_HUMAN Substrate [4]
Multidrug resistance-associated protein 3 (ABCC3) DTQ3ZHF MRP3_HUMAN Substrate [5]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [6]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [5]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [7]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [9]
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME DEYGVN4 UD11_HUMAN Substrate [9]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [9]
UDP-glucuronosyltransferase 1A3 (UGT1A3) Main DME DEF2WXN UD13_HUMAN Substrate [10]
UDP-glucuronosyltransferase 2B15 (UGT2B15) Main DME DENZ6B1 UDB15_HUMAN Substrate [9]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [4]
NPC1-like intracellular cholesterol transporter 1 (NPC1L1) OT6GWW1P NPCL1_HUMAN Drug Response [11]
Phospholipid-transporting ATPase ABCA1 (ABCA1) OT94G6BQ ABCA1_HUMAN Gene/Protein Processing [12]
Sterol regulatory element-binding protein 2 (SREBF2) OTBXUNPL SRBP2_HUMAN Gene/Protein Processing [12]
UDP-glucuronosyltransferase 1A1 OTH1C8OJ UD11_HUMAN Biotransformations [13]
UDP-glucuronosyltransferase 1A3 OTUEOER3 UD13_HUMAN Biotransformations [13]
UDP-glucuronosyltransferase 2B15 OTABTFU2 UDB15_HUMAN Biotransformations [13]
UDP-glucuronosyltransferase 2B7 OT2Q71VQ UD2B7_HUMAN Biotransformations [13]

References

1 Ezetimibe FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6816).
3 Update on patented cholesterol absorption inhibitors. Expert Opin Ther Pat. 2009 Aug;19(8):1083-107.
4 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
5 Complex pharmacokinetic behavior of ezetimibe depends on abcc2, abcc3, and abcg2. Drug Metab Dispos. 2009 Aug;37(8):1698-702.
6 Intestinal expression of P-glycoprotein (ABCB1), multidrug resistance associated protein 2 (ABCC2), and uridine diphosphate-glucuronosyltransferase 1A1 predicts the disposition and modulates the effects of the cholesterol absorption inhibitor ezetimibe in humans. Clin Pharmacol Ther. 2006 Mar;79(3):206-17.
7 A LC-MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1. J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Jan 2;830(1):143-50.
8 Pharmacokinetic and pharmacodynamic interactions between the immunosuppressant sirolimus and the lipid-lowering drug ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2010 Jun;87(6):663-7.
9 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
10 Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2011 Apr;89(4):524-8.
11 Compound heterozygosity for two non-synonymous polymorphisms in NPC1L1 in a non-responder to ezetimibe. Clin Genet. 2005 Feb;67(2):175-7. doi: 10.1111/j.1399-0004.2004.00388.x.
12 Carotenoid transport is decreased and expression of the lipid transporters SR-BI, NPC1L1, and ABCA1 is downregulated in Caco-2 cells treated with ezetimibe. J Nutr. 2005 Oct;135(10):2305-12. doi: 10.1093/jn/135.10.2305.
13 Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of ezetimibe (Zetia). Drug Metab Dispos. 2004 Mar;32(3):314-20.
14 Spiroimidazolidinone NPC1L1 inhibitors. 1: Discovery by 3D-similarity-based virtual screening. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2965-8.
15 Involvement of the drug transporters p glycoprotein and multidrug resistance-associated protein Mrp2 in telithromycin transport. Antimicrob Agents Chemother. 2006 Jan;50(1):80-7.
16 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
17 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
18 Enhancing chemosensitivity in oral squamous cell carcinoma by lentivirus vector-mediated RNA interference targeting EGFR and MRP2. Oncol Lett. 2016 Sep;12(3):2107-2114.
19 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
20 Lentivirus-mediated RNAi silencing targeting ABCC2 increasing the sensitivity of a human nasopharyngeal carcinoma cell line against cisplatin. J Transl Med. 2008 Oct 4;6:55.
21 Effect of acetaminophen on expression and activity of rat liver multidrug resistance-associated protein 2 and P-glycoprotein. Biochem Pharmacol. 2004 Aug 15;68(4):791-8.
22 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7.
23 Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anion transporter (cMOAT). Drug Metab Dispos. 2002 Apr;30(4):457-63.
24 Multidrug Resistance-Associated Protein 2 (MRP2) Mediated Transport of Oxaliplatin-Derived Platinum in Membrane Vesicles. PLoS One. 2015 Jul 1;10(7):e0130727.
25 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
26 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
27 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.
28 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
29 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
30 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
31 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
32 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
33 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
34 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.
35 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
36 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
37 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
38 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.
39 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
40 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
41 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
42 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
43 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
44 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
45 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
46 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
47 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
48 FDA Drug Development and Drug Interactions
49 Multidrug resistance protein (MRP) 1 and MRP3 attenuate cytotoxic and transactivating effects of the cyclopentenone prostaglandin, 15-deoxy-Delta(12,14)prostaglandin J2 in MCF7 breast cancer cells. Biochemistry. 2003 May 13;42(18):5429-37.
50 Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32.
51 ATP-binding cassette C transporters in human pancreatic carcinoma cell lines. Upregulation in 5-fluorouracil-resistant cells. Pancreatology. 2009;9(1-2):136-44.
52 Functional reconstitution of human ABCC3 into proteoliposomes reveals a transport mechanism with positive cooperativity. Biochemistry. 2009 May 26;48(20):4423-30.
53 Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102.
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