Concizumab improves clot formation in hemophilia A under flow

J Thromb Haemost. 2024 Sep;22(9):2438-2448. doi: 10.1016/j.jtha.2024.05.020. Epub 2024 May 28.

Abstract

Background: Inhibition of tissue factor pathway inhibitor (TFPI) is an emerging therapeutic strategy for treatment of hemophilia. Concizumab is a monoclonal antibody that binds TFPI and blocks its inhibition of factor (F)Xa thereby extending the initiation of coagulation and compensating for lack of FVIII or FIX.

Objectives: The objective of this in vitro study was to evaluate how concizumab affects clot formation in hemophilia A under flow.

Methods: Blood was collected from normal controls or people with hemophilia A. An anti-FVIII antibody was added to normal controls to simulate hemophilia A with inhibitory antibodies to FVIII. Whole blood and recombinant activated FVII (rFVIIa, 25 nM) or concizumab (200, 1000, and 4000 ng/mL) were perfused at 100 s-1 over a surface micropatterned with tissue factor (TF) and collagen-related peptide. Platelet and fibrin(ogen) accumulation were measured by confocal microscopy. Static thrombin generation in plasma was measured in response to rFVIIa and concizumab.

Results: Concizumab (1000 and 4000 ng/mL) and rFVIIa both rescued (93%-101%) total platelet accumulation, but only partially rescued (53%-63%) fibrin(ogen) incorporation to normal control levels in simulated hemophilia A. Results using congenital hemophilia A blood confirmed effects of rFVIIa and concizumab. While these 2 agents had similar effect on clot formation under flow, concizumab enhanced thrombin generation in plasma under static conditions to a greater extent than rFVIIa.

Conclusion: TFPI inhibition by concizumab enhanced activation and aggregation of platelets and fibrin clot formation in hemophilia A to levels comparable with that of rFVIIa.

Keywords: blood coagulation; hemophilia A; hemorheology; lipoprotein-associated coagulation inhibitor; microfluidics.

MeSH terms

  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal, Humanized* / pharmacology
  • Antibodies, Monoclonal, Humanized* / therapeutic use
  • Blood Coagulation* / drug effects
  • Blood Platelets / drug effects
  • Blood Platelets / metabolism
  • Case-Control Studies
  • Factor VIII / metabolism
  • Factor VIIa*
  • Fibrin / metabolism
  • Hemophilia A* / blood
  • Hemophilia A* / drug therapy
  • Humans
  • Lipoproteins
  • Recombinant Proteins / pharmacology
  • Thrombin / metabolism

Substances

  • concizumab
  • Antibodies, Monoclonal, Humanized
  • Factor VIIa
  • Antibodies, Monoclonal
  • Recombinant Proteins
  • Thrombin
  • recombinant FVIIa
  • lipoprotein-associated coagulation inhibitor
  • Lipoproteins
  • Fibrin
  • Factor VIII