Icatibant

Summary

Icatibant is a synthetic decapeptide bradykinin B2 receptor antagonist approved for the acute treatment of hereditary angioedema (HAE) attacks in adults. It mimics the structure of bradykinin but acts as a competitive antagonist, rapidly reducing edema, pain, and other symptoms of acute HAE episodes.

Mechanism of Action

Selective competitive antagonist of the bradykinin B2 receptor, blocking the binding of bradykinin and thereby inhibiting vasodilation, increased vascular permeability, and edema formation mediated by the kallikrein-kinin system.

Routes of Administration

Goals & Uses

• Prevention of HAE attacksOff Label/InvestigationalLow
• ACE inhibitor-induced angioedemaInvestigationalModerate
• Bradykinin-mediated angioedema (non-HAE)InvestigationalLow
• Acute treatment of hereditary angioedema attacksApproved IndicationHigh

Contraindications

• Unstable angina pectorisCardiovascularModerate
• Ischemic heart diseaseCardiovascularModerate
• Hypersensitivity to icatibant or excipientsAllergyHigh

Adverse Effects

• RashDermatologicUncommonSkin eruption or discoloration
• Injection site reactionsLocalCommon
• NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
• PyrexiaGeneralUncommon
• Transaminase elevationHepaticRare
• DizzinessNeurologicUncommonFeeling faint, lightheaded, or unsteady

Drug Interactions

• ACE inhibitorsModerate

Population Constraints

• PregnancyReproductive SafetyRelative
• Pediatric patients under 2 yearsAgeAbsolute
• Severe hepatic impairmentOrgan ImpairmentRelative
• BreastfeedingReproductiveRelative

Regulatory Status

• European UnionApprovedApproved: Symptomatic treatment of acute attacks of hereditary angioedema in adultsEMA approved July 2008; marketed as Firazyr; centralized procedure.
• United StatesApprovedApproved: Acute attacks of hereditary angioedema (HAE) in adults and pediatric patients 2 years and olderFDA approved August 2011 (NDA 022150); marketed as Firazyr by Shire (now Takeda).
• United KingdomApprovedApproved: Symptomatic treatment of acute attacks of hereditary angioedema in adultsApproved via retained EU authorization; continues to be marketed post-Brexit.

Approved by the FDA (2011) and EMA (2008) for acute treatment of HAE attacks in adults due to C1-inhibitor deficiency. FDA later expanded use to adolescents (12 years and older) in some labeling updates. Marketed as Firazyr.

Evidence & Sources

No sources recorded yet.