Pharmacokinetics of pegfilgrastim

Pharmacotherapy. 2003 Aug;23(8 Pt 2):9S-14S. doi: 10.1592/phco.23.9.9s.32888.

Abstract

Pegfilgrastim is a granulocyte colony-stimulating factor (G-CSF) with a long half-life and sustained duration of action. Pegfilgrastim is created with pegylation technology, whereby a 20-kD polyethylene glycol moiety is conjugated to filgrastim (recombinant human G-CSF), resulting in a larger molecule. Consequently, its renal clearance by glomerular filtration is minimized, making neutrophil-mediated clearance the predominant route of elimination. Preclinical animal data have shown that the clearance of pegfilgrastim depends on dosage and absolute neutrophil count, with pegfilgrastim having a longer circulating half-life and more sustained duration of action than filgrastim. The biologic effect of pegfilgrastim is prolonged in a neutropenic setting because few mature neutrophils are available to mediate its elimination. Clinical trials have suggested that neutrophil-mediated clearance of pegfilgrastim may be self-regulating and may therefore be specific to each patient's hematopoietic recovery.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / adverse effects
  • Area Under Curve
  • Clinical Trials as Topic
  • Drug Evaluation, Preclinical
  • Filgrastim
  • Granulocyte Colony-Stimulating Factor / analogs & derivatives
  • Granulocyte Colony-Stimulating Factor / pharmacokinetics*
  • Granulocyte Colony-Stimulating Factor / pharmacology
  • Half-Life
  • Humans
  • Metabolic Clearance Rate
  • Neutropenia / chemically induced
  • Neutropenia / drug therapy
  • Polyethylene Glycols
  • Recombinant Proteins

Substances

  • Antineoplastic Agents
  • Recombinant Proteins
  • Granulocyte Colony-Stimulating Factor
  • pegfilgrastim
  • Polyethylene Glycols
  • Filgrastim