Icatibant

Synthetic Bradykinin B2 Receptor Antagonist PeptideRx: PrescriptionCompound: Approved

Also known as: D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]-bradykinin, Firazyr, HOE-140, HOE‑140, Icatibant acetate, JE049

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

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Summary

Icatibant is a synthetic decapeptide (HOE‑140) administered subcutaneously to treat acute attacks of hereditary angioedema (HAE) in adults.

Mechanism of Action

Selective competitive antagonist of the bradykinin B2 receptor, blocking bradykinin‑mediated vasodilation and increased vascular permeability.

Routes of Administration

Subcutaneous

Goals & Uses

  • Prevention of HAE attacksOff Label/InvestigationalLow
  • ACE inhibitor-induced angioedemaInvestigationalModerate
  • Bradykinin-mediated angioedema (non-HAE)InvestigationalLow
  • Prevention of airway obstructionLife‑threatening Event MitigationHigh
  • Acute hereditary angioedema attack reliefSymptom ControlHigh
  • Acute treatment of hereditary angioedema attacksApproved IndicationHigh

Contraindications

  • Unstable angina pectorisCardiovascularModerate
  • Severe cardiovascular disease (unstable angina, recent MI)CardiovascularModerate
  • Known hypersensitivity to icatibant or any excipientsAllergyHigh
  • Ischemic heart diseaseCardiovascularModerate
  • Hypersensitivity to icatibant or excipientsAllergyHigh

Adverse Effects

  • RashDermatologicUncommonSkin eruption or discoloration
  • Injection site reactionsLocalCommon
  • HeadacheNeurologicCommonPain in the head or upper neck
  • NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
  • PyrexiaGeneralUncommon
  • Transaminase elevationHepaticRare
  • Injection site reactions (pain, erythema, swelling)LocalCommon
  • DizzinessNeurologicUncommonFeeling faint, lightheaded, or unsteady

Drug Interactions

  • C1‑esterase inhibitor concentratesLow
  • ACE inhibitorsLow

Population Constraints

  • PregnancyReproductive SafetyRelative
  • Pediatric patients (<18 years)AgeAbsolute
  • Pregnant or breastfeeding womenReproductiveRelative
  • Pediatric patients under 2 yearsAgeAbsolute
  • Severe hepatic impairmentOrgan ImpairmentRelative
  • BreastfeedingReproductiveRelative

Regulatory Status

  • European UnionApprovedApproved: Acute hereditary angioedema attacksEMA approval 2009.
  • United StatesApprovedApproved: Acute hereditary angioedema attacks in adultsFDA approved 2008.
  • United KingdomApprovedApproved: Acute hereditary angioedema attacksMHRA approval; same as EU.

Approved in the US (FDA 2008), EU, and UK for acute HAE attacks; marketed as Firazyr.

Evidence & Sources

No sources recorded yet.

Frequently Asked Questions

What is Icatibant?

Icatibant is a synthetic decapeptide (HOE‑140) administered subcutaneously to treat acute attacks of hereditary angioedema (HAE) in adults.

What is Icatibant used for?

Icatibant is educationally associated with: Prevention of HAE attacks, ACE inhibitor-induced angioedema, Bradykinin-mediated angioedema (non-HAE), Prevention of airway obstruction, Acute hereditary angioedema attack relief, Acute treatment of hereditary angioedema attacks. Educational only — not medical advice.

How is Icatibant administered?

Recorded routes of administration: Subcutaneous.

What are the potential side effects of Icatibant?

Reported adverse effects include: Rash, Injection site reactions, Headache, Nausea, Pyrexia, Transaminase elevation, Injection site reactions (pain, erythema, swelling), Dizziness. This list is not exhaustive — consult a qualified clinician.

Who should avoid Icatibant?

Recorded contraindications: Unstable angina pectoris, Severe cardiovascular disease (unstable angina, recent MI), Known hypersensitivity to icatibant or any excipients, Ischemic heart disease, Hypersensitivity to icatibant or excipients. Consult a qualified clinician before use.