Icatibant: Uses, Mechanism, and Side Effects

Hereditary angioedema attacks cause sudden, painful swelling that can be frightening when it strikes. Icatibant is a prescription treatment designed to interrupt an attack once it has started.

Key takeaways

• Icatibant is approved to treat acute attacks of hereditary angioedema (HAE) in adults 18 and older.
• It works by blocking the bradykinin B2 receptor, targeting the pathway that drives HAE swelling.
• It is sold under the brand name SAJAZIR and carries no boxed warning.
• At least 44 clinical trials have studied icatibant or related HAE treatments.
• FAERS reports for icatibant are dominated by hereditary angioedema itself, reflecting its use in that condition.

What Icatibant Is

Icatibant is a bradykinin B2 receptor antagonist, meaning it blocks a receptor that bradykinin normally activates. In hereditary angioedema, a missing or malfunctioning protein called C1-esterase-inhibitor allows a cascade that overproduces bradykinin. Bradykinin widens blood vessels and is believed to cause the localized swelling, inflammation, and pain typical of HAE. By competitively blocking the B2 receptor, icatibant interferes with bradykinin's action at the site of an attack.

What Icatibant Is Approved For

SAJAZIR (icatibant) injection is approved for treating acute attacks of hereditary angioedema in adults 18 years of age and older. It does not carry a boxed warning. The identifier for icatibant in the PubChem database is CID 6918173, for reference.

What The Evidence Shows

Icatibant and related HAE therapies have been evaluated across at least 44 registered clinical trials. One completed Phase 3 study, FAST-3, examined icatibant in patients experiencing acute HAE attacks. A separate completed Phase 3 trial assessed a different subcutaneous therapy, C1 esterase inhibitor, for preventing angioedema attacks in adolescents and adults with HAE.

Reported Side Effects

FAERS reports for icatibant, which reflect submitted reports rather than confirmed incidence or causation, are led by hereditary angioedema itself (3,575 reports), likely reflecting the condition being treated rather than a drug effect. Other frequently reported issues include drug ineffectiveness, dosing and product use issues, and changes in body weight in either direction. Injection site pain is also reported, consistent with a self-administered injectable therapy.