Antitumor activity of HER-2 inhibitors

Cancer Lett. 2005 Sep 8;227(1):9-23. doi: 10.1016/j.canlet.2004.11.015. Epub 2004 Dec 15.


Activation of intracellular mitogenic signal transduction pathways driven by the ErbB family of receptor tyrosine kinases has been implicated in a variety of cancers. Amongst these, the tumorigenic roles of the Epidermal Growth Factor receptor (EGFR) and HER-2 have been most extensively studied. Therapeutic antibodies and small molecule kinase inhibitors targeting EGFR have recently received regulatory agency approval for the treatment of colon and lung cancer, respectively. In this review, I briefly describe these agents and their potential use in inhibiting the growth of tumors that overexpress HER-2. I also discuss other therapeutics currently available or being developed specifically to target HER-2 dependent tumors.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Drug Resistance, Neoplasm
  • ErbB Receptors / antagonists & inhibitors
  • Humans
  • Intracellular Signaling Peptides and Proteins / therapeutic use*
  • Lapatinib
  • Neoplasms / drug therapy
  • Pyrimidines / therapeutic use
  • Pyrroles / therapeutic use
  • Quinazolines / therapeutic use
  • Receptor, ErbB-2 / analysis
  • Receptor, ErbB-2 / antagonists & inhibitors*
  • Receptor, ErbB-2 / physiology


  • Antineoplastic Agents
  • Intracellular Signaling Peptides and Proteins
  • Pyrimidines
  • Pyrroles
  • Quinazolines
  • protein kinase modulator
  • Lapatinib
  • PKI 166
  • ErbB Receptors
  • Receptor, ErbB-2