Icatibant , the bradykinin B2 receptor antagonist with target to the interconnected kinin systems

Charignon, Delphine; Späth, Peter; Martin, Ludovic; Drouet, Christian (2012). Icatibant , the bradykinin B2 receptor antagonist with target to the interconnected kinin systems. Expert opinion on pharmacotherapy, 13(15), pp. 2233-47. London: Informa Healthcare 10.1517/14656566.2012.723692

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INTRODUCTION: HOE-140/ Icatibant is a selective, competitive antagonist to bradykinin (BK) against its binding to the kinin B2 receptor. Substitution of five non-proteogeneic amino acid analogues makes icatibant resistant to degradation by metalloproteases of kinin catabolism. Icatibant has clinical applications in inflammatory and vascular leakage conditions caused by an acute (non-controlled) production of kinins and their accumulation at the endothelium B2 receptor. The clinical manifestation of vascular leakage, called angioedema (AE), is characterized by edematous attacks of subcutaneous and submucosal tissues, which can cause painful intestinal consequences, and life-threatening complications if affecting the larynx. Icatibant is registered for the treatment of acute attacks of the hereditary BK-mediated AE, i.e., AE due to C1 inhibitor deficiency. AREAS COVERED: This review discusses emerging knowledge on the kinin system: kinin pharmacological properties, biochemical characteristics of the contact phase and kinin catabolism proteases. It underlines the responsibility of the kinins in AE initiation and the potency of icatibant to inhibit AE formation by kinin-receptor interactions. EXPERT OPINION: Icatibant antagonist properties protect BK-mediated AE patients against severe attacks, and could be developed for use in inflammatory conditions. More studies are required to confirm whether or not prolonged and frequent applications of icatibant could result in the impairment of the cardioprotective effect of BK.

Item Type:

Journal Article (Further Contribution)

Division/Institute:

04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Pharmacology

UniBE Contributor:

Späth, Peter Julius

ISSN:

1465-6566

Publisher:

Informa Healthcare

Language:

English

Submitter:

Factscience Import

Date Deposited:

04 Oct 2013 14:35

Last Modified:

17 Mar 2015 21:25

Publisher DOI:

10.1517/14656566.2012.723692

PubMed ID:

22970904

Web of Science ID:

000308946500011

URI:

https://boris.unibe.ch/id/eprint/14096 (FactScience: 220904)

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