Icatibant

Icatibant, trade name Firazyr, is medication that has been approved by the European Commission for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in adults with C1-esterase-inhibitor deficiency. It is not effective in angioedema caused by medication from the ACE inhibitor class, as shown in a 2017 trial. It is a peptidomimetic consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. Icatibant acts as a bradykinin inhibitor by blocking the binding of native bradykinin to the bradykinin B2 receptor.  >> Read More

Icatibant (also called JE049 or HOE140) is a synthetic decapeptide that has a similar structure as bradykinin but contains 5 nonproteinogenic amino acids (D-Arg, L-Hyp, L-Thi, D-Tic, and L-Oic). It is stable and not degraded by bradykinin-cleaving enzymes like carboxypeptidase N (or kininase I) and angiotensin converting enzyme (or kininase II). The study drug was provided by the Jerini AG (Berlin, Germany).

Treatment of acute edema attacks in hereditary angioedema with a bradykinin receptor-2 antagonist (Icatibant)

Icatibant is a selective bradykinin B2 receptor antagonist with, like bradykinin itself, an affinity for the B2 receptor. It does not interact with bradykinin B1 receptors or other peptide receptors. Icatibant reverses increased vascular permeability in C1 esterase inhibitor–knockout mice, inhibits bradykinin-induced vasodilation in humans and, in a phase 1 study, showed dose- and time-dependent inhibition of bradykinin-induced effects in vivo. In a phase 2 study, symptoms improved significantly after open-label treatment with icatibant in 15 patients with hereditary angioedema having acute cutaneous or abdominal attacks.

Icatibant, a New Bradykinin-Receptor Antagonist, in Hereditary Angioedema