Icatibant
Icatibant is an FDA-approved bradykinin B2 receptor antagonist. Attacks of hereditary angioedema are driven by excess bradykinin acting at the B2 receptor on vascular endothelium, which increases permeability and causes plasma extravasation into subcutaneous and submucosal tissue. Icatibant is a synthetic decapeptide containing five non-proteinogenic amino acids that competitively blocks the B2 receptor, halting that signal.
For research use only.
Key Facts
- CAS
- 130308-48-4
- Molecular Weight (MW)
- 1304.5 g/mol
- Half-life
- Mean elimination half-life of 1.4 ± 0.4 hours after subcutaneous injection (Firazyr label)
- FDA status
- Approved
- Evidence level
- FDA Approved
- Human dose established
- Yes
- Administration Route
- Subcutaneous
- Frequency
- As needed for an attack; repeat doses at least 6 hours apart, no more than 3 in 24 hours
- Last updated
- Nov 7, 2026
- Reviewed
- Nov 7, 2026
Research summary
Selective bradykinin B2 receptor antagonist approved for acute attacks of hereditary angioedema in adults and adolescents. It can be self-administered.
Research evidence
- Regulatory review (FDA label)2 reviewed sources
- Controlled human trialsNone in reviewed sources
- Early or uncontrolled human studiesNone in reviewed sources
- Lab & animal studiesNone in reviewed sources
How it works
Each step shows whether the sources Peptide Library has reviewed include that kind of research. Counts are reviewed sources, not every study ever published. Reviews and programme summaries that describe human use are shown as "reported", not as trials, and registered trials without published results are listed but not counted. A higher step means research has progressed further; it does not mean a compound works better or is safer. Compounds whose evidence has not been reviewed yet show "Not reviewed" instead of a guess.
Peptide Library's Icatibant profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.
Icatibant dosage evidence
Icatibant has an FDA-approved human dosage as Firazyr, for acute attacks of hereditary angioedema in adults aged 18 and older. The label dose is 30 mg by subcutaneous injection in the abdomen, repeated at intervals of at least 6 hours if the response is inadequate or symptoms return, with no more than 3 doses in 24 hours. Generic icatibant labels give the same dose.
| Human dosing established | Yes |
|---|---|
| Studied dose range | 30 mg per injection, up to 3 in 24 hours |
| Route | Subcutaneous |
| Frequency | As needed for an attack; repeat doses at least 6 hours apart, no more than 3 in 24 hours |
| Duration studied | Per attack |
| Half-life | Mean elimination half-life of 1.4 ± 0.4 hours after subcutaneous injection (Firazyr label) |
| Evidence level | FDA Approved |
| Last reviewed | 2026-11-07 |
Research-reported dosing
Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.
| Study / context | Population | Dose | Route | Frequency | Duration | Outcome studied | Source |
|---|---|---|---|---|---|---|---|
| FDA label — Firazyr, acute hereditary angioedema attacksFDA-approved label · FDA prescribing information | Adults aged 18 and older with hereditary angioedema | 30 mg | Subcutaneous, abdominal area, over at least 30 seconds | Once per attack; additional doses at least 6 hours apart if needed, maximum 3 in 24 hours | Per attack | Treatment of acute attacks of hereditary angioedema; studied in three controlled trials with 223 patients | FIRAZYR (icatibant) injection — FDA prescribing information, DailyMed |
| FDA label — Icatibant Injection (Teva), acute hereditary angioedema attacksFDA-approved label · FDA prescribing information | Adults aged 18 and older with hereditary angioedema | 30 mg | Subcutaneous, abdominal area | Additional doses at least 6 hours apart if needed, maximum 3 in 24 hours | Per attack | Treatment of acute attacks of hereditary angioedema | Icatibant Injection (Teva) — FDA prescribing information, DailyMed |
Where sources disagree
- Icatibant treats an attack once it has started; the label does not describe it as prevention between attacks. After treating a laryngeal attack, the label says to seek medical care right away because of the risk of airway obstruction.
- Safety and effectiveness in children under 18 have not been established, according to the label.
- Icatibant is supplied as a prefilled syringe delivering 30 mg in 3 mL (10 mg/mL), which patients may self-inject after training. DailyMed lists icatibant injection from several other companies as well as Firazyr.
Sequence & molecular data
| Molecular formula | C59H89N19O13S |
|---|---|
| Molecular weight | 1304.5 g/mol |
| CAS number | 130308-48-4 |
| PubChem CID | 6918173 |
| FDA UNII | 7PG89G35Q7 |
| ChEMBL | CHEMBL2028850 |
| DrugBank | DB06196 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
Attacks of hereditary angioedema are driven by excess bradykinin acting at the B2 receptor on vascular endothelium, which increases permeability and causes plasma extravasation into subcutaneous and submucosal tissue. Icatibant is a synthetic decapeptide containing five non-proteinogenic amino acids that competitively blocks the B2 receptor, halting that signal. The unnatural residues make it resistant to peptidase degradation.
Studies
Research statistics
1,450 PubMed publications · 14.6% human clinical research · 28 registered trials
Counts of published research through 2026-11-01, not evidence that it works. Publications by year, study types and trials · How publications are counted
Regulatory & research status
Icatibant is an FDA-approved product for specific labelled indications. Approval does not extend to the research contexts described on this page, and approved products are prescription medicines.
| FDA status | Approved |
|---|---|
| Research status | Approved product (see FDA status) |
| Availability | Prescription-Only |
| WADA (sport) | Unknown / Not Listed |
| Library classification | FDA-Approved |
How FDA approval, compounding and research-only status differ
Benefits
—
Icatibant side effects
No side effects listed yet for this entry.
Storage & stability
This compound is not supplied as a powder to be mixed, so the freeze-dried powder and reconstitution handling described for research peptides does not apply. Storage conditions are product-specific: follow the label or packaging of the product itself.
Icatibant: frequently asked questions
What is Icatibant?
Selective bradykinin B2 receptor antagonist approved for acute attacks of hereditary angioedema in adults and adolescents. It can be self-administered.
How does Icatibant work?
Attacks of hereditary angioedema are driven by excess bradykinin acting at the B2 receptor on vascular endothelium, which increases permeability and causes plasma extravasation into subcutaneous and submucosal tissue. Icatibant is a synthetic decapeptide containing five non-proteinogenic amino acids that competitively blocks the B2 receptor, halting that signal.
Is Icatibant FDA approved?
Yes. Icatibant is approved by the FDA, and approved products are prescription medicines. Approval is always for specific indications studied in clinical trials, so an approved status does not mean the compound is approved for every use it is discussed for. Research-chemical material sold under the same name is not the approved product.
What peptides are similar to Icatibant?
Compounds most often compared with Icatibant include Angiotensin II, Cetrorelix, Corticorelin and Cosyntropin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ.
References
- Efficacy of Treatment of Non-hereditary Angioedema — Clin Rev Allergy Immunol, 2018External reference
- Icatibant for hereditary angioedema — Drugs Today (Barc), 2009External reference
- Therapeutic potential of icatibant (HOE-140, JE-049) — Expert Opin Pharmacother, 2008External reference
- Icatibant, 2006External reference
- First reported case of Andes hantavirus cardiopulmonary syndrome treated with a combination of favipiravir, ribavirin, icatibant and baricitinib — Clin Microbiol Infect, 2026External reference
Related research, comparisons & guides
Related peptides
Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Nov 7, 2026 · Version 2
This Icatibant profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error
Track Icatibant research, inventory and reconstitution in the free Peptide Library app. Get the app for iOS or Android →