HOE 140

Although it is a rare disease, HAE is an autosomal dominant disorder that can be potentially life-threatening when swelling manifests itself within the upper airways. Antagonism of the constitutively expressed B2 receptor, therefore, would not only be beneficial in the treatment of HAE but also find application in inflammatory, allergic, and hyperalgesic disorders.Designed to possess enhanced metabolic stability with the inclusion of five non-proteinogenic amino acids, icatibant is a competitive and selective B2 receptor antagonist (devoid of activity against the inducible B1 receptor) with a K_i of 2.2±0.7 nM, and it is the first downstream targeting agent to receive regulatory approval. It joins purified C1 esterase inhibitor, danazol (an attenuated androgen), and tranexamic acid (an antifibrinolytic agent) as acute and prophylactic treatments for HAE.

Antagonist (bradykinin).

ChEBI: An acetate salt obtained by combining icatibant with acetic acid. Used for the treatment of acute attacks of hereditary angioedema in adult patients.