Eltrombopag
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Eltrombopag
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| 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 |
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| Identifiers | |
| CAS number | 496775-62-3 (olamine) |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C25H22N4O4 |
| Mol. mass | 442.467 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| 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 being developed by GlaxoSmithKline and Ligand Pharmaceuticals,[1] and is likely to be marketed in the US as Promacta and in the EU as Revolade. It is currently undergoing regulatory review in the US.
[edit] 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]
[edit] 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]
[edit] 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:. 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. doi:. 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. doi:. PMID 18046027.
