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Eltrombopag information


Eltrombopag
Clinical data
Trade namesPromacta, Revolade, Alvaiz
Other namesSB-497115-GR
AHFS/Drugs.comMonograph
MedlinePlusa609011
License data
  • EU EMA: by eltrombopag olamine
  • US DailyMed: Eltrombopag_olamine
  • US FDA: Eltrombopag
Pregnancy
category
  • AU: B3[1]
Routes of
administration
By mouth
ATC code
  • B02BX05 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[1]
  • UK: POM (Prescription only)[2]
  • US: ℞-only[3]
  • EU: Rx-only[4]
Pharmacokinetic data
Bioavailability~52%[3]
Protein binding>99%
Metabolismextensive liver (through CYP1A2 and CYP2C8)
Elimination half-life21–35 hours
Excretionfeces (59%), urine (31%)
Identifiers
IUPAC name
  • 3'-{(2Z)-2-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]hydrazino}-2'-hydroxy-3-biphenylcarboxylic acid
CAS Number
  • 496775-61-2 ☒N
  • as olamine: 496775-62-3
PubChem CID
  • 9846180
  • as olamine: 135449331
DrugBank
  • DB06210 checkY
  • as olamine: DBSALT000063
ChemSpider
  • 21106301 checkY
  • as olamine: 28475107
UNII
  • S56D65XJ9G
  • as olamine: 4U07F515LG
KEGG
  • D03978
ChEBI
  • CHEBI:85010
ChEMBL
  • ChEMBL461101 ☒N
  • as olamine: ChEMBL3989691
CompTox Dashboard (EPA)
  • DTXSID5057753 Edit this at Wikidata
ECHA InfoCard100.128.125 Edit this at Wikidata
Chemical and physical data
FormulaC25H22N4O4
Molar mass442.475 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CC1=NN(c2ccc(C)c(C)c2)C(=O)/C1=N\Nc1cccc(-c2cccc(C(=O)O)c2)c1O
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/h4-13,26,30H,1-3H3,(H,32,33)/b27-22- checkY
  • Key:XDXWLKQMMKQXPV-QYQHSDTDSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Eltrombopag, sold under the brand name Promacta among others, is a medication used to treat thrombocytopenia (abnormally low platelet counts) and severe aplastic anemia.[3][4] Eltrombopag is sold under the brand name Revolade outside the US and is marketed by Novartis.[5] It is a thrombopoietin receptor agonist.[3] It is taken by mouth.[3][4]

Eltrombopag was discovered as a result of research collaboration between GlaxoSmithKline and Ligand Pharmaceuticals and is transferred to Novartis Pharmaceuticals.[5][6][7]

  1. ^ a b "Revolade Product Information". Therapeutic Goods Administration (TGA). Archived from the original on 23 May 2021. Retrieved 23 May 2021.
  2. ^ "Revolade 25 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 17 August 2020. Archived from the original on 23 May 2021. Retrieved 22 May 2021.
  3. ^ a b c d e "Promacta- eltrombopag olamine tablet, film coated Promacta- eltrombopag olamine powder, for suspension". DailyMed. Archived from the original on 23 May 2021. Retrieved 22 May 2021.
  4. ^ a b c "Revolade EPAR". European Medicines Agency (EMA). 17 September 2018. Archived from the original on 23 May 2021. Retrieved 22 May 2021.
  5. ^ a b "Ligand Sells Promacta Assets and Royalty for $827 Million" (Press release). Ligand Pharmaceuticals. 5 March 2019. Archived from the original on 24 June 2021. Retrieved 17 June 2021 – via Business Wire.
  6. ^ "Revolade". GSK Canada. Archived from the original on 28 June 2021. Retrieved 17 June 2021.
  7. ^ "Novartis announces completion of transactions with GSK". Sandoz (Press release). Archived from the original on 24 June 2021. Retrieved 17 June 2021.

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Upadacitinib

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Inflammatory cytokine

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Cytokine

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inhibitors: Agerafenib SCF (c-Kit) See here instead. Thrombopoietin Agonists: Eltrombopag Pegacaristim Promegapoietin Romiplostim Thrombopoietin (THPO, MGDF)...

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Cucurbitacin

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Lymphokine

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Janus kinase

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Interferon type I

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Ruxolitinib

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Macrophage inflammatory protein

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Epoetin alfa

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