Icatibant [HOE 140, JE 049] is a potent, specific and selective peptidomimetic bradykinin β2-receptor antagonist. It has a modified peptide structure, and is the first bradykinin receptor antagonist to act on the guinea-pig trachea without demonstrating agonist effects. Icatibant was originated by Hoechst Marion Roussel (now Sanofi-Aventis).
Jerini is seeking a partner for development and marketing of icatibant for the treatment of refractory ascites in liver cirrhosis, angioedema and burns.
In August 2004, Aventis merged with Sanofi-Synthelabo to form Sanofi-Aventis.
Icatibant has shown an excellent safety profile in phase I studies. In December 2003, Jerini demonstrated positive results in the phase IIa study. Results obtained were statistically significant and clinically relevant. At the BIO 2004 International Annual Convention (BIO-2004) [San Francisco, CA, USA; 6–9 June 2004], Jerini reported plans to initiate phase IIb trials in this indication in the second half of...
KeywordsBradykinin Angioedema Quinapril Hereditary Angioedema Orphan Drug Status
- 1.Profiles of participating companies. BIO 2004: Annual International Convention. Business Forum: 6 Jun 2004Google Scholar
- 6.Proud D. Clinical application of kinin antagonists. Canadian Journal of Physiology and Pharmacology 72 (Suppl. 2): 19, 1994Google Scholar
- 9.Wirth KJ, Gehring D, Schölkens BA. Effect of HOE 140 on bradykinin-induced bronchoconstriction in anaesthetised guinea pigs. Naunyn-Schmiedeberg’s Archives of Pharmacology 344 (Suppl. 2): R141, 1991Google Scholar
- 12.Gaudron P, Hu K, Zdrojewski T, et al. AT1-receptor blocker versus angiotensin converting enzyme inhibitor in acute myocardial Role of dosage and bradykinin on remodelling, hemodynamics and mortality in the rat model. Journal of the American College of Cardiology 31 (Suppl. 2A): 311, Feb 1998CrossRefGoogle Scholar
- 18.Sakamoto T, Elwood W, Barnes PJ. Evaluation of a bradykinin antagonist (HOE 140) against bradykinin and platelet activating factor induced airway responses in the guinea pig. Thorax 47: 241P, Mar 1992Google Scholar
- 19.Sakamoto T, Elwood W, Barnes PJ, et al. Effect of Hoe 140, a new bradykinin receptor antagonist, on bradykinin- and platelet- activating factor-induced bronchoconstriction and airway microvascular leakage in guinea pig. European Journal of Pharmacology 213: 367–373, 31 Mar 1992PubMedCrossRefGoogle Scholar
- 20.Sakamoto T, Elwood W, Barnes PJ. Effect of a novel bradykinin antagonist (HOE140) against bradykinin, platelet activating factor, sodium metabisulfite and allergen induced airway responses in the guinea pig. American Review of Respiratory Disease 145: A859, Apr 1992Google Scholar
- 23.Featherstone RL, Parry JE, Church MK. The effects of kinin antagonism with HOE 140 on the response of guinea-pigs to allergen. Clinical and Experimental Allergy 23 (Suppl. 1): 32, Feb 1993Google Scholar
- 26.Avery J, Barber C. A topical bradykinin antagonist first clinical trial of icatibant nasal spray in seasonal allergic rhinitis. Allergy and Clinical Immunology News (Suppl. 2): 415, 1994Google Scholar