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]
Idiopathic thrombocytopenic purpura	3B64.10	Phase 3	[1]
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Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 1

Molecular Weight (mw)

442.5

Logarithm of the Partition Coefficient (xlogp)

5.4

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [2]
Half-life: The concentration or amount of drug in body reduced by one-half in 21 - 32 hours [3]

Adverse Drug Reaction (ADR)

ADR Term	Variation	Related DOT	DOT ID	REF
Thromboembolism	rs121909567	SERPINC1	OTDFATG0	[4]
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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	[5]

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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]

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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]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Antithrombin-III (SERPINC1)	OTDFATG0	ANT3_HUMAN	Drug Response	[4]

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Molecular Interaction Atlas (MIA)

MIA Detail

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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)

MEA Detail

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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]	[10]
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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]	[11]
Midostaurin	DMI6E0R	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Midostaurin.	Acute myeloid leukaemia [2A60]	[12]
Arn-509	DMT81LZ	Moderate	Accelerated clearance of Eltrombopag due to the transporter induction by Arn-509.	Acute myeloid leukaemia [2A60]	[12]
Gilteritinib	DMTI0ZO	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Gilteritinib.	Acute myeloid leukaemia [2A60]	[11]
Bedaquiline	DM3906J	Moderate	Increased risk of hepatotoxicity by the combination of Eltrombopag and Bedaquiline.	Antimicrobial drug resistance [MG50-MG52]	[13]
Ag-221	DMS0ZBI	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Ag-221.	BCR-ABL1-negative chronic myeloid leukaemia [2A41]	[11]
Pexidartinib	DMS2J0Z	Major	Increased risk of hepatotoxicity by the combination of Eltrombopag and Pexidartinib.	Bone/articular cartilage neoplasm [2F7B]	[14]
Tucatinib	DMBESUA	Moderate	Decreased metabolism of Eltrombopag caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[15]
PF-04449913	DMSB068	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by PF-04449913.	Chronic myelomonocytic leukaemia [2A40]	[12]
Revefenacin	DMMP5SI	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Revefenacin.	Chronic obstructive pulmonary disease [CA22]	[16]
Cannabidiol	DM0659E	Moderate	Increased risk of hepatotoxicity by the combination of Eltrombopag and Cannabidiol.	Epileptic encephalopathy [8A62]	[12]
Simeprevir	DMLUA9D	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Simeprevir.	Hepatitis virus infection [1E50-1E51]	[10]
GS-9857	DMYU6P5	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by GS-9857.	Hepatitis virus infection [1E50-1E51]	[17]
Brentuximab vedotin	DMWLC57	Moderate	Increased risk of hepatotoxicity by the combination of Eltrombopag and Brentuximab vedotin.	Hodgkin lymphoma [2B30]	[18]
Teriflunomide	DMQ2FKJ	Major	Increased risk of hepatotoxicity by the combination of Eltrombopag and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[19]
BMS-201038	DMQTAGO	Major	Increased risk of hepatotoxicity by the combination of Eltrombopag and BMS-201038.	Hyper-lipoproteinaemia [5C80]	[20]
Berotralstat	DMWA2DZ	Major	Decreased clearance of Eltrombopag due to the transporter inhibition by Berotralstat.	Innate/adaptive immunodeficiency [4A00]	[21]
Eluxadoline	DMYZ0P1	Major	Decreased clearance of Eltrombopag due to the transporter inhibition by Eluxadoline.	Irritable bowel syndrome [DD91]	[12]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Eltrombopag caused by PF-06463922 mediated induction of UGT.	Lung cancer [2C25]	[11]
Capmatinib	DMYCXKL	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Capmatinib.	Lung cancer [2C25]	[22]
Artesunate	DMR27C8	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Artesunate.	Malaria [1F40-1F45]	[10]
Idelalisib	DM602WT	Moderate	Increased risk of hepatotoxicity by the combination of Eltrombopag and Idelalisib.	Mature B-cell leukaemia [2A82]	[23]
Arry-162	DM1P6FR	Moderate	Decreased metabolism of Eltrombopag caused by Arry-162 mediated inhibition of UGT.	Melanoma [2C30]	[11]
Ubrogepant	DM749I3	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Ubrogepant.	Migraine [8A80]	[24]
Rimegepant	DMHOAUG	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Rimegepant.	Migraine [8A80]	[25]
Lasmiditan	DMXLVDT	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Lasmiditan.	Migraine [8A80]	[26]
Carfilzomib	DM48K0X	Major	Additive thrombogenic effects by the combination of Eltrombopag and Carfilzomib.	Multiple myeloma [2A83]	[11]
MK-4827	DMLYGH4	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by MK-4827.	Ovarian cancer [2C73]	[10]
Darolutamide	DMV7YFT	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Darolutamide.	Prostate cancer [2C82]	[27]
Tedizolid	DMG2SKR	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Tedizolid.	Skin and skin-structure infection [1F28-1G0Z]	[12]
Larotrectinib	DM26CQR	Moderate	Decreased clearance of Eltrombopag due to the transporter inhibition by Larotrectinib.	Solid tumour/cancer [2A00-2F9Z]	[10]
Deferiprone	DMS2M7O	Moderate	Decreased metabolism of Eltrombopag caused by Deferiprone mediated inhibition of UGT.	Thalassaemia [3A50]	[28]
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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
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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

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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	BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
3	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
4	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.
5	Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54.
6	Pharmacokinetics and hepatic uptake of eltrombopag, a novel platelet-increasing agent. Drug Metab Dispos. 2011 Jun;39(6):1088-96.
7	Assessment of the pharmacokinetic interaction between eltrombopag and lopinavir-ritonavir in healthy adult subjects. Antimicrob Agents Chemother. 2012 Jun;56(6):2846-51.
8	Eltrombopag-induced acute liver failure in a pediatric patient: a pharmacokinetic and pharmacogenetic analysis. Ther Drug Monit. 2018 Aug;40(4):386-388.
9	Eltrombopag for use in children with immune thrombocytopenia. Blood Adv. 2018 Feb 27;2(4):454-461.
10	Allred AJ, Bowen CJ, Park JW, et al. "Eltrombopag increases plasma rosuvastatin exposure in healthy volunteers." Br J Clin Pharmacol 72 (2011): 321-9. [PMID: 21434975]
11	Cerner Multum, Inc. "Australian Product Information.".
12	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
13	Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
14	Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
15	Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
16	Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
17	Product Information. Vosevi (sofosbuvir/velpatasvir/voxilaprevir). Gilead Sciences, Foster City, CA.
18	Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
19	Canadian Pharmacists Association.
20	Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
21	Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
22	Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
23	Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
24	Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
25	Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
26	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
27	Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
28	Product Information. Ferriprox (deferiprone). ApoPharma USA Inc, Rockville, MD.