Icatibant

Icatibant, sold under the brand name Firazyr, is a medication for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in adults with C1-esterase-inhibitor deficiency.[2][3][4] It is not effective in angioedema caused by medication from the ACE inhibitor class.[5]

Icatibant
Clinical data
Trade namesFirazyr
Other namesHoe 140, JE 049[1]
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration    		Subcutaneous
    ATC code
    Legal status
    Legal status
    • AU: S4 (Prescription only)
    • US: ℞-only
    • In general: ℞ (Prescription only)
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC59H89N19O13S
    Molar mass1304.54 g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    It is a peptidomimetic consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. It cost about US$8,000 to 9,000 per dose as of 2014.[6][7]

    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.

    Regulatory status

    Icatibant received orphan drug 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 to market Firazyr in the European Union's 27 member states, as well as Switzerland, Lichtenstein and Iceland, making it the first product to be approved in all EU countries for the treatment of HAE.[2] In the US, the drug was granted FDA approval on August 25, 2011.[8]

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    See also

    References
    1. "Icatibant: HOE 140, JE 049, JE049". Drugs in R&D. 5 (6): 343–8. 2004. doi:10.2165/00126839-200405060-00006. PMID 15563238.
    2. "Jerini Receives European Commission Approval for Firazyr (Icatibant) in the Treatment of HAE" (Press release). Jerini AG. 15 July 2008. Retrieved 22 July 2008.
    3. "Firazyr- icatibant acetate injection, solution". DailyMed. 16 December 2019. Retrieved 17 April 2020.
    4. "Firazyr EPAR". European Medicines Agency (EMA). Retrieved 17 April 2020.
    5. Sinert R, Levy P, Bernstein JA, Body R, Sivilotti ML, Moellman J, et al. (September–October 2017). "Randomized Trial of Icatibant for Angiotensin-Converting Enzyme Inhibitor-Induced Upper Airway Angioedema". The Journal of Allergy and Clinical Immunology. In Practice. 5 (5): 1402–1409.e3. doi:10.1016/j.jaip.2017.03.003. PMID 28552382.
    6. "Icatibant Spares Invasive Airway Maneuver for Angioedema". Medscape. Retrieved 12 April 2020.
    7. Cole, SW; Lundquist, LM (January 2013). "Icatibant for the treatment of hereditary angioedema". The Annals of Pharmacotherapy. 47 (1): 49–55. doi:10.1345/aph.1R423. PMID 23249729.
    8. "FDA Approves Shire's FIRAZYR (icatibant injection) for Acute Attacks of Hereditary Angioedema (HAE)" (Press release). Shire. Retrieved 28 August 2011.
    • "Icatibant". Drug Information Portal. U.S. National Library of Medicine.
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