Icatibant, sold under the brand name Firazyr, is a medication for the symptomatic treatment of acute attacks of

hereditary angioedema Hereditary angioedema (HAE) is a disorder that results in recurrent attacks of severe swelling. The swelling most commonly affects the arms, legs, face, intestinal tract, and airway. If the intestinal tract is affected, abdominal pain and vo ...

(HAE) in adults with C1-esterase-inhibitor deficiency. It is not effective in angioedema caused by medication from the

ACE inhibitor Angiotensin-converting-enzyme inhibitors (ACE inhibitors) are a class of medication used primarily for the treatment of high blood pressure and heart failure. This class of medicine works by causing relaxation of blood vessels as well as a decr ...

class. It is a

peptidomimetic A peptidomimetic is a small protein-like chain designed to mimic a peptide. They typically arise either from modification of an existing peptide, or by designing similar systems that mimic peptides, such as peptoids and β-peptides. Irrespective ...

consisting of ten

amino acid Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although over 500 amino acids exist in nature, by far the most important are the 22 α-amino acids incorporated into proteins. Only these 22 a ...

s, which is a selective and specific antagonist of

bradykinin Bradykinin (BK) (from Greek ''brady-'' 'slow' + ''-kinin'', ''kīn(eîn)'' 'to move') is a peptide that promotes inflammation. It causes arterioles to dilate (enlarge) via the release of prostacyclin, nitric oxide, and endothelium-derived hyperpo ...

B₂ receptors.

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 cell Smooth muscle is one of the three major types of vertebrate muscle tissue, the others being skeletal and cardiac muscle. It can also be found in invertebrates and is controlled by the autonomic nervous system. It is non- striated, so-called becau ...

s to contract. Bradykinin plays an important role as the mediator of pain. Surplus

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

Legal status

Icatibant received

orphan drug An orphan drug is a medication, pharmaceutical agent that is developed to treat certain rare medical conditions. An orphan drug would not be profitable to produce without government assistance, due to the small population of patients affected by th ...

status in Australia, the EU, Switzerland, and the US for the treatment of hereditary angioedema (HAE). In the EU, the approval by the European Commission (July 2008) allows

Jerini Jerini AG was a pharmaceutical company based in Berlin, Germany, which focused on the discovery and development of novel peptide-based drugs. Using a proprietary technology platform, Peptides-to-Drugs (P2D), Jerini pursued disease indications for ...

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 hereditary angioedema. In the US, the drug was granted FDA approval in August 2011.

References

{{Authority control Anti-inflammatory agents Peptide therapeutics Orphan drugs Drugs developed by Takeda Pharmaceutical Company