Pharmacokinetic modelling and validation of the half-life extension needed to reduce the burden of infusions compared with standard factor VIII

Haemophilia. 2018 May;24(3):376-384. doi: 10.1111/hae.13483. Epub 2018 May 6.

Abstract

Introduction: Currently, no universally accepted definition of extended half-life (EHL) recombinant FVIII (rFVIII) exists. Identifying the minimum half-life extension ratio required for a reduction in dosing frequency compared with standard rFVIII could enable a more practical approach to decisions around prophylaxis with EHL rFVIII.

Aim: To identify the half-life extension ratio required to decrease rFVIII dosing frequency by at least 1 day while maintaining the proportion of patients with plasma rFVIII levels above 1 IU/dL and without increasing the total weekly dose.

Methods: A previously published population pharmacokinetic model for standard rFVIII was used to estimate the percentage of patients with factor VIII (FVIII) levels always >1 IU/dL using various benchmark regimens. Using modelling, dosing frequency was reduced while rFVIII half-life was extended until the percentage of patients with FVIII >1 IU/dL equalled that of the benchmark regimen.

Results: Benchmark 3×/wk dosing totalling 100 IU/kg/wk of rFVIII resulted in 56.6% of patients with FVIII levels always >1 IU/dL. With 2×/wk dosing, totalling 80 or 90 IU/kg/wk, half-life extensions required to maintain 56.6% of patients at FVIII levels >1 IU/dL were 1.30 and 1.26, respectively. A half-life extension ratio of 1.33 was required to change dosing from every 48 hours to every 72 hours (both at 105 IU/kg/wk) while maintaining 92.8% of patients with FVIII >1 IU/dL.

Conclusion: Based on this investigation, EHL rFVIII products should have a minimum half-life extension ratio of 1.3 to provide a reduction in dosing frequency from 3× to 2×/wk compared with standard rFVIII products while maintaining the same minimum FVIII trough level.

Keywords: administration and dosage; factor VIII; haemophilia A; half-life; pharmacokinetics; quality of life.

Publication types

  • Comparative Study

MeSH terms

  • Dose-Response Relationship, Drug
  • Factor VIII / administration & dosage*
  • Factor VIII / pharmacokinetics*
  • Factor VIII / therapeutic use
  • Half-Life
  • Hemophilia A / drug therapy
  • Humans
  • Models, Biological*
  • Recombinant Proteins / administration & dosage*
  • Recombinant Proteins / pharmacokinetics*
  • Recombinant Proteins / therapeutic use

Substances

  • Recombinant Proteins
  • Factor VIII