Pro- and anticoagulant factors facilitate thrombin generation and balance the haemostatic response to FEIBA(®) in prophylactic therapy

Haemophilia. 2016 Jul;22(4):615-24. doi: 10.1111/hae.12873. Epub 2016 Feb 15.

Abstract

Introduction: FEIBA(®) consists of zymogens and traces of activated forms of procoagulant factors II, VII, IX, X, anticoagulants protein C and TFPI, and small amounts of cofactors FV, FVIII and protein S, in a balanced ratio. As shown previously, FII-FXa complex plays a key role in FEIBA's mode of action (MoA).

Methods: Thrombin generation (TG) was measured by spiking coagulation factors, cofactors and inhibitors to high titer FVIII inhibitor plasma, and in plasma samples from patients in a phase 3 clinical study evaluating the safety and efficacy of FEIBA prophylaxis in haemophilia A patients with inhibitors.

Results: Increasing the FXa/FII ratio improved TG, while adding coagulation enzyme components had a negligible effect. Adding FX, FIX, and FVII increased the peak thrombin and decreased the lag time. The presence of FV and phospholipids led to faster TG, while protein C and protein S reduced the amount of peak thrombin. TFPI appeared to have no effect. Patients on prophylaxis with FEIBA(®) showed higher peak thrombin and AUC with elevated FII, FX, FIX, FVIIa, and protein C levels, and experienced significantly less bleeding episodes than those receiving on-demand treatment.

Conclusion: These experiments showed that although the FII-FXa complex induced immediate thrombin formation on the activated platelet surface, other procoagulant components of FEIBA were necessary to achieve an optimal thrombin burst. The presence of the pro- and anti-coagulants in FEIBA provides a haemostatic balance, and is thus expected to prevent thrombotic events. Recent clinical data verified the postulated MoA of FEIBA in prophylaxis treatment.

Keywords: FEIBA; haemophilia; inhibitors; prophylaxis; thrombin generation.

MeSH terms

  • Antibodies, Neutralizing / blood
  • Anticoagulants / chemistry*
  • Blood Coagulation Factors / metabolism*
  • Blood Coagulation Tests
  • Coagulants / metabolism*
  • Hemophilia A / blood
  • Hemophilia A / pathology
  • Humans
  • Models, Molecular
  • Severity of Illness Index
  • Thrombin / analysis*
  • Thrombin / metabolism

Substances

  • Antibodies, Neutralizing
  • Anticoagulants
  • Blood Coagulation Factors
  • Coagulants
  • anti-inhibitor coagulant complex
  • Thrombin