← All compounds · evidence tier first, by design
| Use | E1 | E2 | E3 | E4 | E5 | E6 | E7 | E8 |
|---|---|---|---|---|---|---|---|---|
| E1 Acute attacks of hereditary angioedema (C1-inhibitor deficiency) | E1 | |||||||
| E3 ACE-inhibitor-induced angioedema (off-label) | E3 |
Icatibant
Synthetic decapeptide: D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg, containing five non-proteinogenic or D-amino acids (hydroxyproline, beta-(2-thienyl)alanine, D-tetrahydroisoquinoline-3-carboxylic acid, octahydroindole-2-carboxylic acid); no standard one-letter sequence is given.
Non-standard residues or modifications: no plain one-letter sequence
Also: Icatibant acetate · Codes: HOE 140 · Brands: Firazyr
A synthetic ten-residue peptide that blocks the bradykinin B2 receptor. It is an approved prescription drug, given as a single-use prefilled syringe, for treating acute attacks of hereditary angioedema caused by C1-esterase-inhibitor deficiency. Generic versions are approved in the United States. It has also been studied, without approval, for angioedema caused by ACE-inhibitor drugs.
- US A approved
- EU A approved
- UK ? not verified
- CA A approved
- AU ? not verified
- JP ? not verified
- CN ? not verified
01Regulatory status, by jurisdiction
| Jurisdiction | Status | Detail and primary source |
|---|---|---|
| US | Approved | Firazyr (NDA 022150, Takeda Pharms USA) is listed in Drugs@FDA as a new molecular entity with priority review and orphan status, approved 25 August 2011; marketing status Prescription.“08/25/2011 ORIG-1 Approval Type 1 - New Molecular Entity PRIORITY; Orphan”Drugs@FDA: FDA-Approved Drugs - NDA 022150 (Firazyr) · retrieved 2026-10-10 |
| EU | Approved | Firazyr (EMEA/H/C/000899, Takeda) is centrally authorised; marketing authorisation issued 11 July 2008. EMA overview states use in adults, adolescents and children aged over 2 years.“Firazyr is a medicine used to treat the symptoms of attacks of hereditary angioedema in adults, adolescents and children aged over 2 years.”Firazyr | European Medicines Agency (EMA) · retrieved 2026-10-10 |
| CA | Approved | Health Canada Drug Product Database lists Firazyr (Takeda Canada Inc) with current status Marketed.“Current status: Marketed Current status date: 2021-07-21 Original market date: See footnote 1 2014-07-14 Product name: FIRAZYR”Drug Product Database: Product information - FIRAZYR · retrieved 2026-10-10 |
| UK AU JP CN | Not yet verified from a primary source. No status is shown rather than an unsourced one. | |
Sport (WADA): Not prohibited. Not named on the Prohibited List. As an approved medicine it also falls outside class S0, which covers only substances without current regulatory approval: “Any pharmacological substance which is not addressed by any of the subsequent sections of the List and with no current approval by any governmental regulatory health authority for human therapeutic use” WADA source
02What the human evidence shows
Acute attacks of hereditary angioedema (C1-inhibitor deficiency)
Three randomised, double-blind phase 3 trials were run. FAST-1 (placebo comparator) did not meet its primary endpoint; FAST-2 (tranexamic acid comparator) did; both were reported together. FAST-3, a larger placebo-controlled trial, reported shorter time to symptom relief with icatibant. Results are consistent in direction but FAST-1 was negative on its primary endpoint, which is stated here rather than omitted.
- [1] Report of FAST-1 (versus placebo, primary endpoint not met) and FAST-2 (versus tranexamic acid, shorter time to symptom relief with icatibant) in acute hereditary angioedema attacks
- [2] Shorter time to 50% symptom reduction with icatibant than placebo in acute cutaneous and abdominal hereditary angioedema attacks
Registered-study counts: ClinicalTrials.gov intervention search “icatibant hereditary angioedema”, fetched 2026-10-10. Registered studies include trials of other uses; the gap between registered and reported is itself a finding.
ACE-inhibitor-induced angioedema (off-label)
Results conflict. A small randomised phase 2 trial (27 participants) compared icatibant with glucocorticoid plus antihistamine and reported faster resolution of swelling. A larger randomised, placebo-controlled phase 3 trial in emergency departments found no difference from placebo in time to meeting discharge criteria. The indication is not approved.
- [3] Shorter time to complete resolution of oedema with icatibant than with glucocorticoid plus antihistamine in a small randomised trial
- [4] No difference between icatibant and placebo in time to meeting discharge criteria in ACE-inhibitor-induced upper airway angioedema
Registered-study counts: ClinicalTrials.gov intervention search “icatibant ACE inhibitor angioedema”, fetched 2026-10-10. Registered studies include trials of other uses; the gap between registered and reported is itself a finding.
Key registered trials
| NCT | Title (as registered) | Phase | Status |
|---|---|---|---|
| NCT00097695 | Subcutaneous Treatment With Icatibant for Acute Attacks of Hereditary Angioedema | 3 | Completed |
| NCT00500656 | Subcutaneous Treatment With Icatibant for Acute Attacks of Hereditary Angioedema (HAE) | 3 | Completed |
| NCT00912093 | A Study of Icatibant in Patients With Acute Attacks of Hereditary Angioedema (FAST-3) | 3 | Completed |
| NCT01154361 | AMelioration of Angiotensin Converting Enzyme Inhibitor Induced Angioedema Study | 2 | Completed |
| NCT01919801 | Blinded Safety & Efficacy Placebo Controlled Study of Icatibant for Angiotensin Converting Enzyme Inhibitor Induced Angioedema | 3 | Completed |
03Safety signals
- Injection-site reactions [2]
Local injection-site reactions (erythema, swelling, pain) were the most commonly reported adverse events in the placebo-controlled FAST-3 trial.
04What is unknown
- Whether icatibant shortens ACE-inhibitor-induced angioedema is unresolved: a small positive phase 2 trial and a larger negative phase 3 trial conflict
- No randomised evidence is cited for use as short-term prophylaxis before procedures
- Efficacy in non-hereditary forms of bradykinin-mediated angioedema other than ACE-inhibitor-induced (e.g. acquired C1-inhibitor deficiency) rests on case reports not reviewed here
- Status in the UK, Australia, Japan and China was not verified from regulator sources for this record
05Product quality
No independent purity results have been published for this compound yet. The purity programme will publish full methods and vendor-named results, passes and failures, once its protocol has had legal review.
06Citations
- Icatibant, a New Bradykinin-Receptor Antagonist, in Hereditary Angioedema (2010). doi:10.1056/NEJMoa0906393
- Randomized placebo-controlled trial of the bradykinin B2 receptor antagonist icatibant for the treatment of acute attacks of hereditary angioedema: the FAST-3 trial (2011). doi:10.1016/j.anai.2011.08.015
- A Randomized Trial of Icatibant in ACE-Inhibitor–Induced Angioedema (2015). doi:10.1056/nejmoa1312524
- Randomized Trial of Icatibant for Angiotensin-Converting Enzyme Inhibitor–Induced Upper Airway Angioedema (2017). doi:10.1016/j.jaip.2017.03.003
Every DOI is resolved against Crossref and every NCT number against ClinicalTrials.gov, title for title, before publication. Regulatory sources are cited inline above with a verbatim quote and retrieval date.
07Mechanism
Icatibant is a selective competitive antagonist of the bradykinin B2 receptor; in hereditary angioedema, swelling is attributed to excess bradykinin acting at this receptor.
Mechanism is placed last on purpose: a plausible mechanism is not evidence that a compound works in people.
Reviewed by OSMF research team (AI-assisted, source-verified) on 2026-10-10. Found an error? It goes in the corrections log: report it.