Eltrombopag

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Structural formula
Structure of Eltrombopag
General
Non-proprietary name Eltrombopag
other names

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

Molecular formula C 25 H 22 N 4 O 4
External identifiers / databases
CAS number
  • 496775-61-2 (Eltrombopag)
  • 496775-62-3 (eltrombopag olamine)
EC number 610-469-9
ECHA InfoCard 100.128.125
PubChem 135449332
ChemSpider 19879943
DrugBank DB06210
Wikidata Q411588
Drug information
ATC code

B02 BX05

Drug class

Thrombopoietin receptor agonist

properties
Molar mass 442.47 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Eltrombopag - Code SB-497115-GR - ( trade names Revolade ® (EU, CH), Promacta ® (USA) ; manufacturer Novartis ) is a drug from the group of thrombopoietin receptor agonists, which is used in the treatment of idiopathic thrombocytopenic purpura ( ITP) is used. Eltrombopag was approved by the Food and Drug Administration (FDA) for the American market in November 2008 and for the EU by the European Commission in March 2010.

Since September 2015, Eltrombopag has also been approved in the EU for the treatment of adult patients with acquired severe aplastic anemia (SAA) who are either refractory to previous immunosuppressive therapy or who are heavily pretreated and not suitable for a haematopoietic stem cell transplant .

Clinical information

A thrombocytopenia resulting either from a formation disorder, z. B. due to a bone marrow insufficiency , or a turnover disorder with increased consumption of blood platelets. It is the most common cause of acquired hemorrhagic diathesis .

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

The results of a clinical phase III study showed that in 114 subjects with idiopathic thrombocytopenic purpura, daily oral administration of 50 mg eltrombopag led to a significant increase in the number of blood platelets. 80% of patients who receive eltrombopag will experience side effects. These are mainly headache, gastrointestinal disorders (e.g. nausea , diarrhea , vomiting ), insomnia, dry eyes and rash. No serious side effects were observed.

The positive results of the phase II studies were published at the end of 2007.

Chemical information

The monoethanolamine salt with the generic name Eltrombopag olamine is used in all finished preparations .

Individual evidence

  1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  2. ↑ a b Technical information Revolade , accessed on November 16, 2015.
  3. ↑ GSK: FDA approves Promacta® (eltrombopag), the first oral medication to increase platelet production for people with serious blood disorder. ( Memento of December 27, 2010 in the Internet Archive ) Press release, November 20, 2008.
  4. ↑ deutsche-apotheker-zeitung.de: Eltrombopag for chronic immune thrombocytopenia , March 23, 2010, accessed on January 4, 2014.
  5. ^ Supplement to the Pharmazeutische Zeitung 6/2011: New Medicinal Products 2010 , Pharmazeutische Zeitung, Feb. 10, 2011.
  6. ^ Eltrombopag for the treatment of chronic idiopathic thrombocytopenic purpura. N. Engl. J. Med. Nov. 29, 2007, 29; 357 (22): 2237-2247, PMID 18046028 .
  7. ↑ External identifiers or database links to Eltrombopag-Olamin : CAS number: 496775-62-3, EC number: 629-876-8, ECHA InfoCard: 100.158.114 , PubChem : 135449331 , ChemSpider : 28475107 , Wikidata : Q27260489 .