Pharmacokinetic study of ferumoxytol: a new iron replacement therapy in normal subjects and hemodialysis patients

Am J Nephrol. Jul-Aug 2005;25(4):400-10. doi: 10.1159/000087212. Epub 2005 Jul 28.

Abstract

Background: Currently available intravenous iron preparations are not ideal, either because of safety concerns or dose limitations. We investigated the safety and pharmacokinetics of ferumoxytol, a new iron replacement therapy, in normal subjects and hemodialysis patients.

Methods: In a randomized, double-blind, ascending-dose study in normal volunteers (n = 41), 6 subjects received placebo, and 8 subjects each received ferumoxytol, at 1, 2 or 4 mg iron/kg, injected at 60 mg iron/min. The remaining subjects received 4 mg iron/kg at injection rates of 90 (n = 3), 180 (n = 3) or 1,800 mg iron/min (n = 5). In the second, open-label, ascending-dose study, 20 hemodialysis patients received 125 or 250 mg of iron over 5 min.

Results: In normal subjects, the blood half-life of ferumoxytol increased with increasing dose from 9.3 to 14.5 h (p < 0.05) but not with increasing rate of injection. The drug half-life in hemodialysis patients was similar to normal subjects. Ferumoxytol was not removed with hemodialysis. Serum iron (p < 0.001), transferrin saturation (p < 0.001) and ferritin increased in both populations. No serious adverse events were attributable to ferumoxytol.

Conclusion: Ferumoxytol was well tolerated in this study. Its pharmacokinetic properties and simplicity of administration suggest that it will be an attractive form of iron replacement therapy.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Anemia / drug therapy
  • Anemia / etiology
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Erythropoietin / therapeutic use
  • Female
  • Hematinics / pharmacokinetics*
  • Hematinics / therapeutic use
  • Humans
  • Kidney Failure, Chronic / complications
  • Kidney Failure, Chronic / therapy*
  • Male
  • Middle Aged
  • Renal Dialysis*
  • Treatment Outcome

Substances

  • Hematinics
  • Erythropoietin