Human C1-esterase inhibitor

Serpin (serine Protease Inhibitor)Rx: PrescriptionCompound: Approved

Also known as: Berinert, C1-INH, Cinryze, Conestat alfa, Haegarda, Ruconest, SERPING1

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

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Summary

Human C1-esterase inhibitor (C1-INH) is a plasma-derived or recombinant serpin used to prevent and treat attacks of hereditary angioedema by restoring deficient C1-INH activity.

Mechanism of Action

Inhibits plasma serine proteases C1r, C1s, MASP-1, MASP-2, plasma kallikrein, and plasmin, thereby regulating complement activation and bradykinin generation.

Routes of Administration

IntravenousSubcutaneous

Goals & Uses

  • Routine prophylaxis of HAE attacksPreventionHigh
  • Pediatric HAE managementTreatmentModerate
  • Pre-procedural prophylaxis of HAEPreventionHigh
  • Acute treatment of HAE attacksTreatmentHigh
  • Hereditary angioedema prophylaxis and acute treatmentIndicationHigh
  • Capillary leak syndrome / sepsis-associated inflammationInvestigationalLow

Contraindications

  • Uncontrolled disseminated intravascular coagulationCoagulationModerate
  • Severe IgA deficiency with anti‑IgA antibodiesImmunologyModerate
  • Known hypersensitivity to C1-INH preparationsAllergy / HypersensitivityHigh
  • Hypersensitivity to C1-INH productAllergyHigh
  • Rabbit allergy (Ruconest/Conestat alfa)AllergyHigh
  • History of life-threatening thrombotic events (high-dose off-label use)Thrombotic RiskHigh

Adverse Effects

  • Hypersensitivity / anaphylaxisImmunologicalRare
  • HeadacheNeurologicCommonPain in the head or upper neck
  • Injection/infusion site reactionsLocalCommon
  • Thromboembolic eventsCardiovascularRare
  • Hypersensitivity reactionImmunologicRare
  • NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
  • PyrexiaGeneralUncommon
  • Injection site erythemaLocalCommonRedness at the injection site
  • ThrombosisHematologicRareFormation of a blood clot

Drug Interactions

  • Estrogen‑containing oral contraceptivesModerate
  • Estrogen-containing oral contraceptivesModerate
  • ACE inhibitorsModerate
  • Tissue plasminogen activator (tPA)Low
  • Antifibrinolytics (e.g., tranexamic acid)Low

Population Constraints

  • Patients with high thrombosis riskCardiovascularRelative
  • PregnancyReproductive SafetyRelative
  • Pediatric patients <1 yearAgeRelative
  • Pregnant womenReproductiveRelative
  • Elderly (>75 years)GeriatricRelative
  • Neonates / infants (off-label high-dose use)PediatricRelative

Regulatory Status

  • European UnionApprovedApproved: Hereditary angioedema prophylaxis, Acute treatment of hereditary angioedemaApproved under EMA for plasma‑derived C1‑INH products.
  • United StatesApprovedApproved: Hereditary angioedema prophylaxis, Acute treatment of hereditary angioedemaCinryze (SC), Berinert (IV), Haegarda (SC) approved.
  • United KingdomApprovedApproved: Hereditary angioedema prophylaxis, Acute treatment of hereditary angioedemaApproved by MHRA.

FDA‑approved (Cinryze, Berinert, Haegarda); EMA‑approved; indicated for HAE types I and II.

Evidence & Sources

No sources recorded yet.

Frequently Asked Questions

What is Human C1-esterase inhibitor?

Human C1-esterase inhibitor (C1-INH) is a plasma-derived or recombinant serpin used to prevent and treat attacks of hereditary angioedema by restoring deficient C1-INH activity.

What is Human C1-esterase inhibitor used for?

Human C1-esterase inhibitor is educationally associated with: Routine prophylaxis of HAE attacks, Pediatric HAE management, Pre-procedural prophylaxis of HAE, Acute treatment of HAE attacks, Hereditary angioedema prophylaxis and acute treatment, Capillary leak syndrome / sepsis-associated inflammation. Educational only — not medical advice.

How is Human C1-esterase inhibitor administered?

Recorded routes of administration: Intravenous, Subcutaneous.

What are the potential side effects of Human C1-esterase inhibitor?

Reported adverse effects include: Hypersensitivity / anaphylaxis, Headache, Injection/infusion site reactions, Thromboembolic events, Hypersensitivity reaction, Nausea, Pyrexia, Injection site erythema, Thrombosis. This list is not exhaustive — consult a qualified clinician.

Who should avoid Human C1-esterase inhibitor?

Recorded contraindications: Uncontrolled disseminated intravascular coagulation, Severe IgA deficiency with anti‑IgA antibodies, Known hypersensitivity to C1-INH preparations, Hypersensitivity to C1-INH product, Rabbit allergy (Ruconest/Conestat alfa), History of life-threatening thrombotic events (high-dose off-label use). Consult a qualified clinician before use.

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