Multicenter evaluation of the hemostatic activity of emicizumab in patients with severe hemophilia A

J Thromb Haemost. 2024 Jul;22(7):1857-1866. doi: 10.1016/j.jtha.2024.03.022. Epub 2024 Apr 6.

Abstract

Background: Emicizumab has been approved for the prophylaxis of patients with hemophilia A with or without inhibitors. However, spontaneous and trauma-induced breakthrough bleeds have been reported in patients on emicizumab prophylaxis, and no laboratory assay has been validated to evaluate the hemostatic activity of emicizumab.

Objectives: The thrombin generation assay (TGA) could be a surrogate marker of the hemostatic efficacy of emicizumab. The correlation between TGA and the methods used to measure emicizumab blood concentration was evaluated in this study.

Methods: TGA was modified by the use of a trigger reagent combining a very low concentration of tissue factor and activated factor (F)XI. Emicizumab quantification was performed by 3 methods: the modified 1-step FVIII assay and 2 methods based on liquid chromatography and mass spectrometry (LC-MS).

Results: Using tissue factor/activated FXI-triggered TGA and platelet-poor plasma, a relationship was observed between the area under the thrombin generation curve (endogenous thrombin potential [ETP]) and the clinical response of patients to emicizumab. The ultrastructure of fibrin clots was consistent with ETP results and showed that emicizumab had a hemostatic activity equivalent to 20 to 30 IU/dL of FVIII. Finally, pharmacokinetic/pharmacodynamic analyses showed no correlation between ETP and LC-MS nor with modified 1-stage FVIII assay, but a statistically significant correlation between the LC-MS methods and the time-to-peak results of the TGA.

Conclusion: Using a modified TGA, this study showed that patients who experienced breakthrough bleeds while on emicizumab had a lower thrombin-generating capacity compared with others with good clinical response to emicizumab.

Keywords: drug monitoring; emicizumab; endogenous thrombin potential; mass spectrometry; thrombin generation assay.

Publication types

  • Multicenter Study

MeSH terms

  • Adolescent
  • Adult
  • Antibodies, Bispecific* / blood
  • Antibodies, Bispecific* / pharmacokinetics
  • Antibodies, Bispecific* / pharmacology
  • Antibodies, Bispecific* / therapeutic use
  • Antibodies, Monoclonal, Humanized* / pharmacokinetics
  • Antibodies, Monoclonal, Humanized* / pharmacology
  • Antibodies, Monoclonal, Humanized* / therapeutic use
  • Blood Coagulation / drug effects
  • Blood Coagulation Tests
  • Child
  • Chromatography, Liquid
  • Hemophilia A* / blood
  • Hemophilia A* / drug therapy
  • Hemorrhage / blood
  • Hemostasis* / drug effects
  • Hemostatics / pharmacokinetics
  • Hemostatics / pharmacology
  • Hemostatics / therapeutic use
  • Humans
  • Male
  • Mass Spectrometry
  • Middle Aged
  • Severity of Illness Index
  • Thrombin* / metabolism
  • Treatment Outcome
  • Young Adult

Substances

  • emicizumab
  • Antibodies, Monoclonal, Humanized
  • Antibodies, Bispecific
  • Thrombin
  • Hemostatics