Details of the Drug

General Information of Drug (ID: DMOGFIX)

Drug Name
Eltrombopag
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], [2]
Idiopathic thrombocytopenic purpura 3B64.10 Phase 3 [1], [3]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 442.5
Topological Polar Surface Area (xlogp) 5.4
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 21 - 32 hours [5]
Chemical Identifiers
Formula
C25H22N4O4
IUPAC Name
3-[3-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]diazenyl]-2-hydroxyphenyl]benzoic acid
Canonical SMILES
CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)N=NC3=CC=CC(=C3O)C4=CC(=CC=C4)C(=O)O)C
InChI
InChI=1S/C25H22N4O4/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33/h4-13,28,30H,1-3H3,(H,32,33)
InChIKey
SVOQIEJWJCQGDQ-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
135449332
ChEBI ID
CHEBI:85010
CAS Number
496775-61-2
DrugBank ID
DB06210
TTD ID
D00PEH
VARIDT ID
DR00908
INTEDE ID
DR0569
ACDINA ID
D00225

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Thrombopoietin receptor (MPL) TTIHYA4 TPOR_HUMAN Agonist [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [6]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 1A1 (UGT1A1)
Main DME 		DEYGVN4 UD11_HUMAN Substrate [8]
Cytochrome P450 1A2 (CYP1A2)
Main DME 		DEJGDUW CP1A2_HUMAN Substrate [9]
Cytochrome P450 2C8 (CYP2C8)
Main DME 		DES5XRU CP2C8_HUMAN Substrate [8]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

ICD Disease Classification 03 Disease of the blood or blood-forming organs
Disease Class ICD-11: 3B64 Thrombocytopenia
The Studied Tissue Whole blood
The Studied Disease Thrombocytopenia [ICD-11:3B64]
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Thrombopoietin receptor (MPL) DTT MPL 8.96E-01 0.07 0.28
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 1.68E-01 -3.34E-02 -2.12E-01
Breast cancer resistance protein (ABCG2) DTP BCRP 3.02E-01 -3.34E-02 -6.08E-02
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 5.31E-01 7.20E-02 4.31E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 4.83E-01 3.92E-02 2.84E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 4.45E-01 4.11E-01 1.01E+00
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Eltrombopag
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Lusutrombopag DMH6IKO Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [61]
Coadministration of a Drug Treating the Disease Different from Eltrombopag (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Eltrombopag and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [62]
Midostaurin DMI6E0R Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [63]
Arn-509 DMT81LZ Moderate Accelerated clearance of Eltrombopag due to the transporter induction by Arn-509. Acute myeloid leukaemia [2A60] [63]
Gilteritinib DMWQ4MZ Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Gilteritinib. Acute myeloid leukaemia [2A60] [62]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Eltrombopag and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [64]
Ag-221 DMS0ZBI Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [62]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Eltrombopag and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [65]
Tucatinib DMBESUA Moderate Decreased metabolism of Eltrombopag caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [66]
PF-04449913 DMSB068 Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by PF-04449913. Chronic myelomonocytic leukaemia [2A40] [63]
Revefenacin DMMP5SI Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Revefenacin. Chronic obstructive pulmonary disease [CA22] [67]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Eltrombopag and Cannabidiol. Epileptic encephalopathy [8A62] [63]
Simeprevir DMLUA9D Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Simeprevir. Hepatitis virus infection [1E50-1E51] [61]
GS-9857 DMYU6P5 Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by GS-9857. Hepatitis virus infection [1E50-1E51] [68]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Eltrombopag and Brentuximab vedotin. Hodgkin lymphoma [2B30] [69]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Eltrombopag and Teriflunomide. Hyper-lipoproteinaemia [5C80] [70]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Eltrombopag and BMS-201038. Hyper-lipoproteinaemia [5C80] [71]
Berotralstat DMWA2DZ Major Decreased clearance of Eltrombopag due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [72]
Eluxadoline DMYZ0P1 Major Decreased clearance of Eltrombopag due to the transporter inhibition by Eluxadoline. Irritable bowel syndrome [DD91] [63]
PF-06463922 DMKM7EW Moderate Increased metabolism of Eltrombopag caused by PF-06463922 mediated induction of UGT. Lung cancer [2C25] [62]
Capmatinib DMYCXKL Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [73]
Artesunate DMR27C8 Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Artesunate. Malaria [1F40-1F45] [61]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Eltrombopag and Idelalisib. Mature B-cell leukaemia [2A82] [74]
Arry-162 DM1P6FR Moderate Decreased metabolism of Eltrombopag caused by Arry-162 mediated inhibition of UGT. Melanoma [2C30] [62]
Ubrogepant DM749I3 Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Ubrogepant. Migraine [8A80] [75]
Rimegepant DMHOAUG Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Rimegepant. Migraine [8A80] [76]
Lasmiditan DMXLVDT Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Lasmiditan. Migraine [8A80] [77]
Carfilzomib DM48K0X Major Additive thrombogenic effects by the combination of Eltrombopag and Carfilzomib. Multiple myeloma [2A83] [62]
MK-4827 DMLYGH4 Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by MK-4827. Ovarian cancer [2C73] [61]
Darolutamide DMV7YFT Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [78]
Tedizolid DMG2SKR Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Tedizolid. Skin and skin-structure infection [1F28-1G0Z] [63]
Larotrectinib DM26CQR Moderate Decreased clearance of Eltrombopag due to the transporter inhibition by Larotrectinib. Solid tumour/cancer [2A00-2F9Z] [61]
Deferiprone DMS2M7O Moderate Decreased metabolism of Eltrombopag caused by Deferiprone mediated inhibition of UGT. Thalassaemia [3A50] [79]
⏷ Show the Full List of 32 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 2 E00446 2723854 Colorant
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sucralose E00370 71485 Flavoring agent
Sunset yellow FCF E00255 17730 Colorant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferric oxide black E00522 16211978 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Hypromellose E00634 Not Available Coating agent
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Polyvinyl alcohol E00666 Not Available Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Certolake sunset yellow E00351 61817 Colorant
Haematite red E00236 14833 Colorant
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
Xanthan gum E00694 Not Available Bioadhesive material; Emulsifying agent; Gelling agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
⏷ Show the Full List of 20 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Eltrombopag 50 mg tablet 50 mg Oral Tablet Oral
Eltrombopag 12.5 mg tablet 12.5 mg Oral Tablet Oral
Eltrombopag 25 mg tablet 25 mg Oral Tablet Oral
Eltrombopag 75 mg tablet 75 mg Oral Tablet Oral
Eltrombopag 100 mg tablet 100 mg Oral Tablet Oral
Eltrombopag Olamine eq 50mg acid tablet eq 50mg acid Tablet Oral
Eltrombopag Olamine eq 12.5mg acid tablet eq 12.5mg acid Tablet Oral
Eltrombopag Olamine eq 100mg acid tablet eq 100mg acid Tablet Oral
Eltrombopag Olamine eq 25mg acid tablet eq 25mg acid Tablet Oral
Eltrombopag Olamine eq 75mg acid tablet eq 75mg acid Tablet Oral
Eltrombopag Olamine eq 12.5mg acid/packet for suspension eq 12.5mg acid/packet For Suspension Oral
Eltrombopag Olamine eq 25mg acid/packet for suspension eq 25mg acid/packet For Suspension Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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64 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
65 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
66 Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
67 Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
68 Product Information. Vosevi (sofosbuvir/velpatasvir/voxilaprevir). Gilead Sciences, Foster City, CA.
69 Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
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72 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
73 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
74 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
75 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
76 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
77 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
78 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
79 Product Information. Ferriprox (deferiprone). ApoPharma USA Inc, Rockville, MD.