Eltrombopag

IUPAC: 3 - { N-[1 - (3,4- dimethylphenyl )-3- methyl-5- oxo-1, 5 - dihydropyrazol - ( 4Z ) -ylidene ] hydrazine } -2- hydroxybiphenyl - 3-carboxylic acid

B02BX05

Thrombopoietin receptor agonist

Template: Infobox chemical / molecular formula search available

Eltrombopag - Code SB - 497115 -GR - (trade name Revolade ® (EU, CH), Promacta ® ( USA); manufacturer GlaxoSmithKline) is a drug from the group of thrombopoietin receptor agonist, which is used in the treatment of thrombocytopenia. In late November 2008, the drug approved by the Food and Drug Administration ( FDA) for the American market. The Marketing Authorisation Application to the European Medicines Agency ( European Medicines Agency) was successful in March 2010.

Clinical information

Thrombocytopenia resulting either from an educational disorder, eg due to bone marrow failure, or at a sales failure with increased consumption of platelets. It is the most common cause of acquired hemorrhagic diathesis.

With Eltrombopag is a non-peptide, orally active thrombopoietin receptor agonist. This drug stimulates the proliferation and differentiation of megakaryocytes - the precursor cells of the thrombocytes ( platelets) - which leads to an increase in the platelet concentration.

The results of a Phase III clinical study showed that at the 114 subjects with idiopathic thrombocytopenic purpura, the daily oral administration of 50 mg of eltrombopag led to a significant increase in the number of platelets. In 80% of patients receiving eltrombopag, experience side effects. These are mainly headache, gastrointestinal disturbances ( eg, nausea, diarrhea, vomiting), insomnia, dry eyes, and skin rash. Serious side effects were not observed.

The positive results of the phase II studies were published on 29 November 2007 already in the NEJM (New England Journal of Medicine ).

Chemical information

All finished products, the olamine salt is used with the generic name eltrombopag olamine. The CAS number is 496775-62-3, the molar mass is 564.63 g · mol -1 and the molecular formula is C29H36N6O6.