icatibant

Icatibant is a synthetic decapeptide that acts as a highly selective antagonist of the bradykinin B2 receptor. By blocking bradykinin from activating B2 receptors on vascular endothelium, it reduces edema and swelling associated with acute attacks of angioedema.

It is approved for the treatment of acute attacks of hereditary angioedema (HAE) in adults and in adolescents in some jurisdictions, particularly for HAE caused by C1 esterase inhibitor deficiency. It is not a substitute for other therapies in all forms of angioedema, and its use should follow regional guidelines and physician judgment.

Administration and dosing involve a single subcutaneous injection of 30 mg. If symptoms recur or persist, a second dose may be given after 6 hours, and a third dose may be administered if needed, with a maximum of three doses within 24 hours.

Pharmacokinetically, icatibant is delivered by subcutaneous injection and acts rapidly, with symptom relief typically observed within hours. Its effects are temporary, reflecting its antagonism of bradykinin signaling during an acute attack.

Common adverse events are injection-site reactions such as pain, erythema, and swelling, along with dizziness or nausea. Hypersensitivity reactions are uncommon. Icatibant is stored refrigerated (2–8°C) and prepared for self-administration where approved.

Development and regulatory history place icatibant as a targeted therapy for bradykinin-mediated angioedema, representing an alternative to C1 esterase inhibitor replacement in suitable patients. Its role remains established in guidelines for managing acute HAE attacks in eligible populations.