Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00225)
Name
Eltrombopag
Synonyms    Click to Show/Hide the Synonyms of This API
496775-61-2; Promacta; Revolade; (Z)-3'-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid; SB497115; UNII-S56D65XJ9G; Eltrombopag free base; 3'-[2-[(2Z)-1-(3,4-Dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid; SB-497115; CHEMBL461101; S56D65XJ9G; CHEMBL3186485; CHEBI:85010; Eltrombopag (SB-497115-GR); 496775-61-2 (free base); NCGC00274067-01; (Z)-3'-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,; 1807882-48-9; Eltrombopag [INN]; 3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid; SB 497115; Eltrombopag/; Eltrombopag?; AMG531; HSDB 8212; (ZE)-Eltrombopag; PubChem20546; DSSTox_CID_31542; DSSTox_RID_97427; DSSTox_GSID_57753; SCHEMBL18910; MLS006010024; SCHEMBL164270; SCHEMBL211081; SCHEMBL211082; CHEMBL478463; GTPL6961; DTXSID5057753; EX-A443; BCPP000243; HMS3655B14; HMS3743O17; BCP01884; Tox21_113965; ABP000381; ANW-44916; BDBM50248106; MFCD20926253; MFCD21090400; ZINC11679756; ZINC30690955; AKOS015920246; AKOS026750537; ZINC100015243; ZINC100794657; ZINC252551075; ZINC299848778; BCP9000641; CCG-269152; CS-1565; DB06210; EX-7216; SB19101; VA10799; NCGC00274067-02; 376591-99-0; AK-72820; AS-19180; AS-35176; BR-72820; HY-15306; SMR004701208; CAS-496775-61-2; FT-0660417; SW219608-1; SB-497115-GR;SB497115; A12686; A25156; AB01274808-01; AB01274808_02; 775E612; Q411588; Z2216208634; (1,1'-Biphenyl)-3-carboxylic acid, 3'-((2Z)-(1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene)hydrazino)-2'-hydroxy-; (E)-3'-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid; (Z)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxybiphenyl-3-carboxylic acid; 3'-[(2Z)- [1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid; 3'-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid; 3'-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo4H-pyrazol-4-ylidene]hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid; 3'-{(2z)-2-(1-[3,4-dimethylphenyl]-3-methyl-5-oxo-1,5-dihydro-4h-pyrazol-4-ylidene)diazanyl}-2'-hydroxybiphenyl-3-carboxylic acid; 3'-{(2Z)-2-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]hydrazino}-2'-hydroxybiphenyl-3-carboxylic acid; 3'-{(2Z)-2-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]hydrazinyl}-2'-hydroxy[1,1'-biphenyl]-3-carboxylic acid; 3'-{2-[(4E)-1-(3,4-dimethylphenyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-ylidene]hydrazin-1-yl}-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid; 3'-{N'-[1-(3,4-dimethyl-phenyl)-3-methyl-5-oxo-1,5-dihydropyrazol-4-ylidene]hydrazino}-2'-hydroxybiphenyl-3-carboxylic acid; 3'-{N'-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-pyrazol-4-ylidene]hydrazino}-2'-hydroxybiphenyl-3-carboxylic acid; 3-(3-{2-[(4Z)-1-(3,4-dimethylphenyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-ylidene]hydrazin-1-yl}-2-hydroxyphenyl)benzoic acid; 3-(5-{2-[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-2,3-dihydro-1H-pyrazol-4-yl]hydrazin-1-ylidene}-6-oxocyclohexa-1,3-dien-1-yl)benzoic acid; 3-[3-[2-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazole-4-ylidene]hydrazino]-2-hydroxyphenyl]benzoic acid
Clinical Status
Approved
Disease Indication Thrombocytopenia ICD-11: 3B64 [1]
PubChem CID
135449332
Formula
C25H22N4O4
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
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
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=135449332"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 442.5 Topological Polar Surface Area 115
XlogP 5.4 Complexity 812
Heavy Atom Count 33 Rotatable Bond Count 5
Hydrogen Bond Donor Count 3 Hydrogen Bond Acceptor Count 7
Full List of Drug Formulations (DFMs) Containing This API
          Eltrombopag 12.5 mg tablet Click to Show/Hide the Full List of Formulation(s):          2 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium stearate; Mannitol; Titanium dioxide; Polyethylene glycol 400; Polysorbate 80; Cellulose, microcrystalline; Hypromelloses; Povidones; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium stearate; Mannitol; Ferric oxide red; Ferrosoferric oxide; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hypromelloses; Povidones; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Novartis Pharmaceuticals Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag 25 mg tablet Click to Show/Hide the Full List of Formulation(s):          2 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Fd&c yellow no. 6; Magnesium stearate; Mannitol; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hypromelloses; Povidones; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [6]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium stearate; Mannitol; Ferric oxide red; Ferrosoferric oxide; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hypromelloses; Povidones; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Novartis Pharmaceuticals Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag 50 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Fd&c blue no. 2; Magnesium stearate; Mannitol; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hypromelloses; Povidones; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline; Novartis Pharmaceuticals Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag 75 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium stearate; Mannitol; Ferric oxide red; Ferrosoferric oxide; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hypromelloses; Povidones; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline; Novartis Pharmaceuticals Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag 100 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium stearate; Mannitol; Ferric oxide yellow; Ferrosoferric oxide; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hypromelloses; Povidones; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag Olamine eq 50mg acid tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium Stearate; Mannitol; Microcrystalline Cellulose; Povidone; Sodium Starch Glycolate; Hypromellose; Iron Oxide Black; Polyethylene Glycol 400; Titanium Dioxide; Fd&C Blue No. 2 Aluminum Lake
                   Dosage Form Tablet
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [7]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag Olamine eq 12.5mg acid tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium Stearate; Mannitol; Microcrystalline Cellulose; Povidone; Sodium Starch Glycolate; Hypromellose; Iron Oxide Black; Polyethylene Glycol 400; Titanium Dioxide; Polysorbate 80
                   Dosage Form Tablet
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [7]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag Olamine eq 100mg acid tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium Stearate; Mannitol; Microcrystalline Cellulose; Povidone; Sodium Starch Glycolate; Polyvinyl Alcohol; Talc; Iron Oxide Black; Polyethylene Glycol 400; Titanium Dioxide; Iron Oxide Yellow; Iron Oxide Black
                   Dosage Form Tablet
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [7]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag Olamine eq 25mg acid tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium Stearate; Mannitol; Microcrystalline Cellulose; Povidone; Sodium Starch Glycolate; Hypromellose; Iron Oxide Black; Polyethylene Glycol 400; Titanium Dioxide; Fd&C Yellow No. 6 Aluminum Lake
                   Dosage Form Tablet
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [7]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag Olamine eq 75mg acid tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium Stearate; Mannitol; Microcrystalline Cellulose; Povidone; Sodium Starch Glycolate; Hypromellose; Iron Oxide Black; Polyethylene Glycol 400; Titanium Dioxide; Iron Oxide Red
                   Dosage Form Tablet
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [7]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Eltrombopag Olamine eq 12.5mg acid/packet for suspension Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Mannitol; Sucralose; Xanthan Gum
                   Dosage Form For Suspension
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sucralose DIG Info Carbonic anhydrase II (Ki = 300 nM) [8]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
          Eltrombopag Olamine eq 25mg acid/packet for suspension Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Mannitol; Sucralose; Xanthan Gum
                   Dosage Form For Suspension
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sucralose DIG Info Carbonic anhydrase II (Ki = 300 nM) [8]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
References
1 FDA label for approved eltrombopag from the official website of the U.S. Food and Drug Administration.
2 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
6 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
7 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
8 Sweet Binders: Carbonic Anhydrase IX in Complex with Sucralose. ACS Med Chem Lett. 2018 May 10; 9(7):657-661.

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