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Eltrombopag


Eltrombopag
Systematic (IUPAC) name
3-[(5E)-5-[[1-(3,4-dimethylphenyl)-3-methyl-5-oxo- 2H-pyrazol-4-yl]hydrazinylidene]-6-oxo-1-cyclohexa- 1,3-dienyl]benzoic acid
Identifiers
CAS number	496775-61-2 496775-62-3 (olamine)
ATC code	?
PubChem	9846180
Chemical data
Formula	C₂₅H₂₂N₄O₄
Mol. mass	442.467 g/mol
SMILES	search in eMolecules, PubChem
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	Oral

Eltrombopag (rINN, codenamed SB-497115-GR) is a medication under development for conditions that lead to thrombocytopenia (abnormally low platelet counts). It is a small molecule agonist of the c-mpl (TpoR) receptor, which is the physiological target of the hormone thrombopoietin. It is under development by GlaxoSmithKline and Ligand Pharmaceuticals,^[1] and is likely to be marketed as Promacta.

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Development

In preclinical studies, the compound was shown to interact selectively with the thrombopoeitin receptor, leading to activation of the JAK-STAT signaling pathway and increased proliferation and differentiation of megakaryocytes. Animal studies confirmed that administration could increase platelet counts. In 73 healthy volunteers, higher doses of eltrombopag caused larger increases in the number of circulating platelets without tolerability problems.^[2]

Clinical trials

Eltrombopag has been studied, and shown to be effective, in two major clinical syndromes: idiopathic thrombocytopenic purpura^[3] and cirrhosis due to hepatitis C (in which low platelet counts may be a contraindication for interferon treatment).^[4]

References

^ GlaxoSmithKline presents rapidly expanding pipeline of oncology and supportive care compounds - GlaxoSmithKline. Retrieved on 2007-11-29.
^ Jenkins JM, Williams D, Deng Y, et al (2007). "Phase 1 clinical study of eltrombopag, an oral, nonpeptide thrombopoietin receptor agonist". Blood 109 (11): 4739–41. doi:10.1182/blood-2006-11-057968. PMID 17327409.
^ Bussel JB, Cheng G, Saleh MN, et al (2007). "Eltrombopag for the treatment of chronic idiopathic thrombocytopenic purpura". N. Engl. J. Med. 357: 2237-2247. PMID 18046028.
^ McHutchison JG, Dusheiko G, Shiffman ML (2007). "Eltrombopag for thrombocytopenia in patients with cirrhosis associated with hepatitis C". N. Engl. J. Med. 357: 2227-2236. PMID 18046027.