Details of the Drug-Related molecule(s) Expression 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(s) Related to This Drug


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 Highest Status REF
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Approved [3]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [4]

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

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Thrombopoietin receptor (MPL) DTT MPL 2.7 3.186 2.35 3.766
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 8.165 6.597 6.591 6.397
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

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 between Disease Section and Healthy Individual Tissue

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.