|Other names||Hoe 140, JE 049|
|Drug class||Bradykinin B2 receptors inhibitor|
|Main uses||Hereditary angioedema (HAE) with insufficient C1-esterase inhibitor|
|Side effects||Redness, itching, and pain at the site of injection|
|Typical dose||30 mg|
|Chemical and physical data|
|Molar mass||1304.54 g·mol−1|
|3D model (JSmol)|
Icatibant, sold under the brand name Firazyr, is a medication used to treat attacks of hereditary angioedema (HAE) in people with insufficient C1-esterase inhibitor. It does not appear effective for angioedema due to ACE inhibitors. It is given by injection under the skin.
Common side effects include redness, itching, and pain at the site of injection. Other side effects may include fever, headache, and nausea. Safety in pregnancy is unclear. It is a bradykinin B2 receptors inhibitor.
Icatibant was approved for medical use in Europe in 2008 and the United States in 2011. In the United Kingdom it costs the NHS about £1,400 per dose. In the United States this amount costs about 3,600 USD.
Mechanism of action
Bradykinin is a peptide-based hormone that is formed locally in tissues, very often in response to a trauma. It increases vessel permeability, dilates blood vessels and causes smooth muscle cells to contract. Bradykinin plays an important role as the mediator of pain. Surplus bradykinin is responsible for the typical symptoms of inflammation, such as swelling, redness, overheating and pain. These symptoms are mediated by activation of bradykinin B2 receptors. Icatibant acts as a bradykinin inhibitor by blocking the binding of native bradykinin to the bradykinin B2 receptor. Little is known about the effects of icatibant on the bradykinin B1 receptor.
Society and culture
In the EU, the approval by the European Commission (July 2008) allows Jerini to market Firazyr in the European Union's 27 member states, as well as Switzerland, Liechtenstein and Iceland, making it the first product to be approved in all EU countries for the treatment of HAE. In the US, the drug was granted FDA approval on August 25, 2011.
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