Pharmacokinetic and pharmacodynamic properties of EGFR inhibitors under clinical investigation

Cancer Treat Rev. 2004 May;30(3):255-68. doi: 10.1016/j.ctrv.2003.10.003.


The epidermal growth factor receptor (EGFR) is overexpressed in many solid tumours. Targeting EGFR is emerging as a potential strategy to incorporate into cancer treatment regimens. Recent data have contributed to our understanding of the therapeutic potentials and limitations of EGFR targeted therapy. In this review, we present a comprehensive analysis of the various anti-EGFR agents presently in clinical trials. Specifically, we compare the pharmacokinetic and pharmacodynamic properties of these EGFR inhibitors examined in preclinical and clinical studies. These data should enable the clinician to select the most suitable EGFR targeting agent based on objective data.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Animals
  • Antibodies, Monoclonal / administration & dosage
  • Antibodies, Monoclonal / pharmacokinetics*
  • Antibodies, Monoclonal, Humanized
  • Biological Availability
  • Cetuximab
  • Clinical Trials, Phase I as Topic
  • Clinical Trials, Phase II as Topic
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / metabolism
  • Follow-Up Studies
  • Gefitinib
  • Humans
  • Infusions, Intravenous
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Quinazolines / administration & dosage
  • Quinazolines / pharmacokinetics*


  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Quinazolines
  • ErbB Receptors
  • Cetuximab
  • Gefitinib