Approved & therapeutic
Icatibant
Firazyr, Sajazir
Icatibant is a synthetic bradykinin B2 receptor antagonist approved in the US for the treatment of acute attacks of hereditary angioedema in adults. It is given as a subcutaneous injection and can be self-administered.
- Status
- Icatibant is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- Mean elimination half-life of about 1.4 hours after subcutaneous administration.
- How it's taken
- Subcutaneous injection
- Mechanism
- Other
How Icatibant works
Hereditary angioedema attacks are driven by excess bradykinin, which increases vascular permeability and produces the characteristic swelling. Icatibant is a competitive antagonist selective for the bradykinin B2 receptor, blocking bradykinin from binding and thereby limiting the vascular leak. It treats an attack in progress; it is not a prophylactic agent.
What research has looked at
- In the phase 3 FAST-3 trial, the PRIMARY endpoint (median time to onset of symptom relief in the cutaneous and abdominal cohort: 43 patients on icatibant, 45 on placebo) was met: 2.0 hours with icatibant versus 19.8 hours with placebo (p<0.001).
- Secondary endpoints in the same trial also favoured icatibant: median time to onset of primary symptom relief 1.5 versus 18.5 hours (p<0.001), and median time to almost complete symptom relief 8.0 versus 36.0 hours (p=0.012). These are secondary, not primary, endpoints.
- It is approved for acute attacks of hereditary angioedema in adults, and the prefilled syringe formulation allows self-administration outside a clinical setting.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- The US label lists no contraindications and carries no Boxed Warning.
- Injection site reactions occurred in almost all patients in clinical trials (97 percent), including erythema, swelling, burning, pain and itching.
- Laryngeal attacks: the label directs that patients seek immediate medical attention at an appropriate healthcare facility after treating a laryngeal attack, since airway compromise can still occur despite treatment.
- Pyrexia (4 percent), transaminase elevations (4 percent), dizziness (3 percent) and rash were reported in trials at greater than 1 percent incidence.
- Drug interaction: as a bradykinin B2 receptor antagonist, icatibant may attenuate the antihypertensive effect of ACE inhibitors. Clinical trials excluded subjects taking ACE inhibitors, so there is no trial safety data for that combination. Use in ACE inhibitor-induced angioedema is NOT an approved indication and results have been inconsistent, with a small positive trial and a larger placebo-controlled trial failing to meet its primary endpoint. The US indication and label are restricted to adults 18 years and older; safety and effectiveness below 18 have not been established.
Sources
- PubMed research on Icatibant · NIH · National Library of Medicine
- DrugBank record for Icatibant · DrugBank
- Active clinical trials for Icatibant · U.S. National Library of Medicine
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Icatibant FAQ
What is Icatibant?
Icatibant is a synthetic bradykinin B2 receptor antagonist approved in the US for the treatment of acute attacks of hereditary angioedema in adults. It is given as a subcutaneous injection and can be self-administered.
How does Icatibant work?
Hereditary angioedema attacks are driven by excess bradykinin, which increases vascular permeability and produces the characteristic swelling. Icatibant is a competitive antagonist selective for the bradykinin B2 receptor, blocking bradykinin from binding and thereby limiting the vascular leak. It treats an attack in progress; it is not a prophylactic agent.
Is Icatibant FDA approved?
Yes. Icatibant is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Icatibant?
Reported half-life: Mean elimination half-life of about 1.4 hours after subcutaneous administration.
How is Icatibant taken?
Subcutaneous injection.
What side effects have been reported with Icatibant?
Reported in the sources: The US label lists no contraindications and carries no Boxed Warning; Injection site reactions occurred in almost all patients in clinical trials (97 percent), including erythema, swelling, burning, pain and itching; Laryngeal attacks: the label directs that patients seek immediate medical attention at an appropriate healthcare facility after treating a laryngeal attack, since airway compromise can still occur despite treatment; Pyrexia (4 percent), transaminase elevations (4 percent), dizziness (3 percent) and rash were reported in trials at greater than 1 percent incidence; Drug interaction: as a bradykinin B2 receptor antagonist, icatibant may attenuate the antihypertensive effect of ACE inhibitors. Clinical trials excluded subjects taking ACE inhibitors, so there is no trial safety data for that combination. Use in ACE inhibitor-induced angioedema is NOT an approved indication and results have been inconsistent, with a small positive trial and a larger placebo-controlled trial failing to meet its primary endpoint. The US indication and label are restricted to adults 18 years and older; safety and effectiveness below 18 have not been established.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.