Recombinant C1-inhibitor: effects on coagulation and fibrinolysis in patients with hereditary angioedema

BioDrugs. 2012 Feb 1;26(1):43-52. doi: 10.2165/11599490-000000000-00000.

Abstract

Background: Recombinant human C1-inhibitor (rhC1INH; Ruconest®) has been developed for treatment of acute angioedema attacks in patients with hereditary angioedema (HAE) due to heterozygous deficiency of C1INH. Previous reports suggest that administration of plasma-derived C1INH products may be associated with an increased risk for thromboembolic complications.

Objectives: Our aim is to evaluate the effects of rhC1INH on coagulation and fibrinolysis in symptomatic HAE patients.

Methods: Levels of various coagulation and fibrinolytic parameters were determined in pre- and post-exposure plasma samples from HAE patients included in a randomized clinical trial. Patients were treated with either saline, or 50 or 100 U/kg rhC1INH for an acute angioedema attack.

Results: Prior to rhC1INH treatment, the majority of patients had low to normal activated partial thromboplastin times (aPTT) and increased levels of prothrombin fragment 1+2, thrombin-antithrombin complexes, D-dimers and plasmin-antiplasmin complexes, all of which indicate activation of both coagulation and fibrinolysis. Infusion of rhC1INH at doses up to 100 U/kg did not affect these parameters except for a dose-dependent prolongation of aPTT, confirming that rhC1INH is an inhibitor of the contact system, and that F1+2 levels decreased.

Conclusion: Coagulation and fibrinolytic systems are activated in HAE patients suffering from an acute angioedema attack. Treatment with rhC1INH at 50 or 100 U/kg had no effect on parameters reflecting activation of these systems except for a significant effect on aPTT, which likely reflects a pharmacodynamic effect of rhC1INH, and a reduction on plasma levels of the prothrombin activation fragment F1+2. We conclude that these results argue against a prothrombotic effect of treatment with this rhC1INH product in HAE patients.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Angioedemas, Hereditary / blood*
  • Angioedemas, Hereditary / complications
  • Angioedemas, Hereditary / drug therapy*
  • Blood Coagulation / drug effects*
  • Complement C1 Inhibitor Protein / administration & dosage
  • Complement C1 Inhibitor Protein / adverse effects*
  • Complement C1 Inhibitor Protein / therapeutic use
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / adverse effects
  • Enzyme Inhibitors / therapeutic use
  • Female
  • Fibrinolysis / drug effects*
  • Humans
  • Male
  • Middle Aged
  • Models, Cardiovascular
  • Recombinant Proteins / administration & dosage
  • Recombinant Proteins / adverse effects
  • Recombinant Proteins / therapeutic use
  • Thromboembolism / chemically induced*

Substances

  • Complement C1 Inhibitor Protein
  • Enzyme Inhibitors
  • Recombinant Proteins
  • conestat alfa