Icatibant

FDA-approved bradykinin B2 receptor antagonistEstablished

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.

Calculate Dose

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.

FDA Approved
Dosage evidence summary for Icatibant
Human dosing establishedYes
Studied dose range30 mg per injection, up to 3 in 24 hours
RouteSubcutaneous
FrequencyAs needed for an attack; repeat doses at least 6 hours apart, no more than 3 in 24 hours
Duration studiedPer attack
Half-lifeMean elimination half-life of 1.4 ± 0.4 hours after subcutaneous injection (Firazyr label)
Evidence levelFDA Approved
Last reviewed2026-11-07

Research-reported dosing

Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.

Research-reported dosing for Icatibant, one row per studied regimen
Study / contextPopulationDoseRouteFrequencyDurationOutcome studiedSource
FDA label — Firazyr, acute hereditary angioedema attacksFDA-approved label · FDA prescribing informationAdults aged 18 and older with hereditary angioedema30 mgSubcutaneous, abdominal area, over at least 30 secondsOnce per attack; additional doses at least 6 hours apart if needed, maximum 3 in 24 hoursPer attackTreatment of acute attacks of hereditary angioedema; studied in three controlled trials with 223 patientsFIRAZYR (icatibant) injection — FDA prescribing information, DailyMed
FDA label — Icatibant Injection (Teva), acute hereditary angioedema attacksFDA-approved label · FDA prescribing informationAdults aged 18 and older with hereditary angioedema30 mgSubcutaneous, abdominal areaAdditional doses at least 6 hours apart if needed, maximum 3 in 24 hoursPer attackTreatment of acute attacks of hereditary angioedemaIcatibant 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.
Icatibant dosage in published studies and labels →

Sequence & molecular data

Sequence and molecular data for Icatibant
Molecular formulaC59H89N19O13S
Molecular weight1304.5 g/mol
CAS number130308-48-4
PubChem CID6918173
FDA UNII7PG89G35Q7
ChEMBLCHEMBL2028850
DrugBankDB06196

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.

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.

Regulatory and research status for Icatibant
FDA statusApproved
Research statusApproved product (see FDA status)
AvailabilityPrescription-Only
WADA (sport)Unknown / Not Listed
Library classificationFDA-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

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 →