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

General Information of Drug (ID: DMOGFIX)

Drug Name
Eltrombopag Drug Info
Synonyms
Eltrombopag [INN]; SB 497115; SB497115; SB-497115; [1,1'-Biphenyl]-3-carboxylic acid, 3'-[(2Z)-[1-(3,4-dime; Thylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2'-hydroxy-(9CI); (E)-3\'-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2\'-hydroxybiphenyl-3-carboxylic acid
Indication
Disease Entry ICD 11 Status REF
Thrombocytopenia 3B64 Approved [1]
Idiopathic thrombocytopenic purpura 3B64.10 Phase 3 [1]
Cross-matching ID
PubChem CID
135449332
ChEBI ID
CHEBI:85010
CAS Number
CAS 496775-61-2
TTD Drug ID
DMOGFIX
VARIDT Drug ID
DR00908
INTEDE Drug ID
DR0569
ACDINA Drug ID
D00225

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Thrombopoietin receptor (MPL)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [8]
Lusutrombopag DMH6IKO Thrombocytopenia 3B64 Approved [9]
AS-1670542 DMV05SW Thrombocytopenia 3B64 Approved [10]
LGD-4665 DM9T8A2 Immune thrombocytopenic purpura 3B64.13 Phase 2 [2]
BVI-007 DM43GPX Myocardial infarction BA41-BA43 Phase 1 [10]
NIP-004 DM0PYEQ Thrombocytopenia 3B64 Phase 1 [11]
RhTPO DMCV0BZ Idiopathic thrombocytopenic purpura 3B64.10 Discontinued in Phase 3 [2]
Totrombopag DM6SUDC Thrombocytopenia 3B64 Discontinued in Phase 1 [12]
Promegapoietin DMS4FG0 Bone marrow transplantation QB63.6 Terminated [13]
N. A. N. A. [10]
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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 [14]
Methotrexate DM2TEOL Anterior urethra cancer Approved [15]
Folic Acid DMEMBJC Colorectal carcinoma Approved [16]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [17]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [18]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [19]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [20]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [19]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [21]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [22]
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Drug(s) Transported By Organic anion transporting polypeptide 2B1 (SLCO2B1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [23]
L-Glutamic Acid DM4PUDW Schizophrenia 6A20 Approved [24]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [25]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [26]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [27]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [28]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [29]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [30]
Digoxin DMQCTIH Arrhythmia BC9Z Approved [31]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [32]
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Drug(s) Metabolized By Cytochrome P450 1A2 (CYP1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [33]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [34]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [35]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [36]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [37]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [38]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [39]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [40]
Verapamil DMA7PEW Angina pectoris BA40 Approved [41]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [42]
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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 [43]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [44]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [45]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [46]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [47]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [48]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [49]
Metronidazole DMTIVEN Abscess Approved [50]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [51]
Ethanol DMDRQZU Chronic pain MG30 Approved [52]
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Drug(s) Metabolized By Cytochrome P450 2C8 (CYP2C8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [33]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [53]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [53]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [54]
Verapamil DMA7PEW Angina pectoris BA40 Approved [55]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [56]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [57]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [53]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [58]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [59]
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Drug(s) Affected By Antithrombin-III (SERPINC1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [60]
Prednisone DM2HG4X Acute asthma CA23 Approved [61]
Quercetin DM3NC4M Obesity 5B81 Approved [62]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [63]
Testosterone enanthate DMB6871 N. A. N. A. Approved [64]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [65]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [66]
Aminocaproic Acid DMFGND4 Bleeding disorder GA20-GA21 Approved [61]
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [67]
Warfarin DMJYCVW Atrial fibrillation BC81.3 Approved [68]
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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
Thrombopoietin receptor (MPL) TTIHYA4 TPOR_HUMAN Agonist [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [3]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME DEYGVN4 UD11_HUMAN Substrate [5]
Cytochrome P450 1A2 (CYP1A2) Main DME DEJGDUW CP1A2_HUMAN Substrate [6]
Cytochrome P450 2C8 (CYP2C8) Main DME DES5XRU CP2C8_HUMAN Substrate [5]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Antithrombin-III (SERPINC1) OTDFATG0 ANT3_HUMAN Drug Response [7]

References

1 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: 6961).
2 Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54.
3 Pharmacokinetics and hepatic uptake of eltrombopag, a novel platelet-increasing agent. Drug Metab Dispos. 2011 Jun;39(6):1088-96.
4 Assessment of the pharmacokinetic interaction between eltrombopag and lopinavir-ritonavir in healthy adult subjects. Antimicrob Agents Chemother. 2012 Jun;56(6):2846-51.
5 Eltrombopag-induced acute liver failure in a pediatric patient: a pharmacokinetic and pharmacogenetic analysis. Ther Drug Monit. 2018 Aug;40(4):386-388.
6 Eltrombopag for use in children with immune thrombocytopenia. Blood Adv. 2018 Feb 27;2(4):454-461.
7 Early onset of abdominal venous thrombosis in a newborn with homozygous type II heparin-binding site antithrombin deficiency. Blood Coagul Fibrinolysis. 2017 Apr;28(3):264-266. doi: 10.1097/MBC.0000000000000570.
8 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
9 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
10 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. (Target id: 1722).
11 A novel nonpeptidyl human c-Mpl activator stimulates human megakaryopoiesis and thrombopoiesis. Blood. 2006 Jun 1;107(11):4300-7.
12 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
13 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
14 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
15 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
16 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.
17 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
18 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
19 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
20 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.
21 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
22 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
23 Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60.
24 The Transporter Classification Database (TCDB): recent advances. Nucleic Acids Res. 2016 Jan 4;44(D1):D372-9. (ID: 2.A.60.1.20)
25 Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP. J Pharm Sci. 2017 Sep;106(9):2688-2694.
26 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.
27 Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45.
28 Human platelets express organic anion-transporting peptide 2B1, an uptake transporter for atorvastatin. Drug Metab Dispos. 2009 May;37(5):1129-37.
29 pH-sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1. Mol Pharm. 2011 Aug 1;8(4):1303-13.
30 Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos. 2006 Jul;34(7):1229-36.
31 Drug Interactions in Infectious Diseases.
32 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
33 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
34 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
35 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
36 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
37 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
38 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
39 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
40 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
41 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
42 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
43 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
44 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
45 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
46 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
47 Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
48 Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
49 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
50 Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
51 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
52 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
53 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
54 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
55 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
56 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
57 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
58 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
59 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
60 MS4A3-HSP27 target pathway reveals potential for haematopoietic disorder treatment in alimentary toxic aleukia. Cell Biol Toxicol. 2023 Feb;39(1):201-216. doi: 10.1007/s10565-021-09639-4. Epub 2021 Sep 28.
61 Plasma proteinase inhibitor activity and hemostasis tests in children with nephrotic syndrome. Effect of prednisone alone and prednisone plus epsilon-aminocaproic acid treatment regimens: a preliminary report. Am J Ther. 2001 Mar-Apr;8(2):97-107. doi: 10.1097/00045391-200103000-00004.
62 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
63 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
64 Haemostatic effects of supraphysiological levels of testosterone in normal men. Thromb Haemost. 1995 Aug;74(2):693-7.
65 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
66 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
67 Stress doses of hydrocortisone reduce severe systemic inflammatory response syndrome and improve early outcome in a risk group of patients after cardiac surgery. Crit Care Med. 2003 Apr;31(4):1068-74. doi: 10.1097/01.CCM.0000059646.89546.98.
68 Venous thrombosis, heparin-induced antithrombin III deficiency, and factor VIII. Lancet. 1977 Dec 10;2(8050):1231-2.