Pharmacodynamics of eftrenonacog-alfa (rFIX-Fc) in severe hemophilia B patients: A real-life study

Eur J Pharmacol. 2021 Jan 15:891:173764. doi: 10.1016/j.ejphar.2020.173764. Epub 2020 Nov 27.

Abstract

Eftrenonacog-alfa is a recombinant factor IX-Fc fusion protein increasingly prescribed in hemophilia B patients. We aimed to assess its pharmacodynamics (PD) in real-life setting via FIX activity measurement and thrombin generation assay (TGA). Sixty samples from 15 severe hemophilia B treated patients were collected at different time points. FIX activity was measured using product-specific one-stage clotting assay (reference method) and two chromogenic assays (CSA) (Biophen FIX and Rox FIX). TGA was triggered with 1 pM tissue factor. Five parameters were analyzed: lag time (LT), time to peak (TTP), peak height (PH), endogenous thrombin potential (ETP), and velocity. PD models were built to characterize their relationships with FIX activity, using mixed effects models. Mean trough FIX level was estimated at 4.64 (±1.50) IU/dl with a recovery at 0.78 (±0.16) IU/dl per 1 IU/kg injected dose. FIX activity ranged between 1 and 86 IU/dl with 21.5 IU/dl median value. Biophen FIX and Rox FIX allowed reliable measurements except in samples with FIX <20 IU/dl in which values were underestimated (delta >30%). PD models revealed that velocity was the most sensitive TGA parameter to FIX activity followed by PH, ETP, TTP and finally LT. Following FIX activity peak after eftrenonacog-alfa injection, velocity decreased first, followed by PH then ETP. Both CSA failed to accurately measure FIX in severe hemophilia B patients receiving eftrenonacog-alfa throughout the measuring range. TGA could be an additional valuable tool to evaluate hemostasis balance in treated patients.

Keywords: Chromogenic assay; Extended half-life factor IX; One-stage clotting assay; Pharmacodynamics; Thrombin generation assay.

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Blood Coagulation Tests*
  • Coagulants / adverse effects
  • Coagulants / pharmacokinetics
  • Coagulants / therapeutic use*
  • Drug Monitoring*
  • Factor IX / adverse effects
  • Factor IX / pharmacokinetics
  • Factor IX / therapeutic use*
  • Hemophilia B / blood
  • Hemophilia B / diagnosis
  • Hemophilia B / drug therapy*
  • Hemostasis / drug effects*
  • Humans
  • Immunoglobulin Fc Fragments / adverse effects
  • Immunoglobulin Fc Fragments / therapeutic use*
  • Male
  • Middle Aged
  • Predictive Value of Tests
  • Recombinant Fusion Proteins / adverse effects
  • Recombinant Fusion Proteins / pharmacokinetics
  • Recombinant Fusion Proteins / therapeutic use*
  • Reproducibility of Results
  • Severity of Illness Index
  • Treatment Outcome
  • Young Adult

Substances

  • Coagulants
  • Immunoglobulin Fc Fragments
  • Recombinant Fusion Proteins
  • factor IX Fc fusion protein
  • Factor IX