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FDA Approved Cardiovascular & Renal

Icatibant

also known as: Firazyr, HOE 140

The bradykinin blocker for angioedema — a synthetic decapeptide B2 receptor antagonist that stops acute swelling attacks within 30 minutes.

A synthetic 10-amino-acid peptidomimetic that selectively antagonizes bradykinin B2 receptors, FDA-approved for the treatment of acute attacks of hereditary angioedema (HAE) in adults.

Mechanism of action

Selective competitive antagonist at bradykinin B2 receptor. In HAE, C1-esterase inhibitor deficiency leads to excess bradykinin causing vascular leak and edema. Icatibant blocks B2R activation, reversing swelling within 30-60 minutes.

Primary uses

  • Acute hereditary angioedema attacks (FDA-approved)
  • ACE inhibitor-induced angioedema (off-label)

Typical dosing

30 mg single SC injection per attack; may repeat q6h (max 3/24h) (subcutaneous)

Self-administered using prefilled syringe. Onset typically within 30-60 minutes.

Regulatory status

FDA-approved August 2011 as Firazyr for acute HAE attacks in adults. Self-administered via subcutaneous injection.

References

  1. [pubmed] Cicardi M, et al. "Icatibant, a new bradykinin-receptor antagonist, in hereditary angioedema." N Engl J Med. 2010;363(6):532-541.

Related peptides

Bradykinin

The vasoactive peptide behind ACE inhibitor cough — an endogenous inflammatory mediator that connects cardiovascular pharmacology to angioedema, pain, and allergic responses.

Angiotensin II

Giapreza — the first new vasopressor class approved in decades. FDA-approved December 2017 (La Jolla Pharmaceutical) for catecholamine-resistant septic / distributive shock based on the ATHOS-3 trial (NEJM 2017, n=321). Engages a third vasoconstrictor pathway (RAAS / AT1) independent of catecholamines and vasopressin — useful when both of those axes are desensitised.

Vasopressin

Vasostrict — the endogenous antidiuretic hormone as an ICU vasopressor. FDA-approved April 2014 for adults with vasodilatory shock (post-cardiotomy, sepsis) who remain hypotensive despite fluids and catecholamines. Works through V1a receptors on vascular smooth muscle — a receptor axis pharmacologically distinct from catecholamine receptors, preserving its vasopressor effect when adrenergic receptors are desensitised.
Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.