Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu)

Eur J Cancer. 2007 Feb;43(3):481-9. doi: 10.1016/j.ejca.2006.11.007. Epub 2007 Jan 8.


Targeting of epidermal growth factor receptor (EGFR) and HER2 is a proven anti-cancer strategy. However, heterodimerisation, compensatory 'crosstalk' and redundancy exist in the ErbB network, and there is therefore a sound scientific rationale for dual inhibition of EGFR and HER2. Trials of approved agents in combination, for example trastuzumab and cetuximab, are underway. There is also a new generation of small molecule tyrosine kinase inhibitors (TKIs) and monoclonal antibodies (mABs) that target two or more ErbB receptors. Lapatinib, a TKI of EGFR and HER2, has shown clinical benefit in trastuzumab refractory breast cancer and is poised for FDA approval. Other agents include BIBW-2992 and HKI-272, irreversible TKIs of EGFR and HER2, and pertuzumab, a heterodimerisation inhibitor of EGFR and HER2.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal
  • Antineoplastic Agents / therapeutic use*
  • Clinical Trials, Phase I as Topic
  • ErbB Receptors / antagonists & inhibitors*
  • Genes, erbB-1
  • Genes, erbB-2
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Receptor, ErbB-2 / antagonists & inhibitors*


  • Antibodies, Monoclonal
  • Antineoplastic Agents
  • ErbB Receptors
  • Protein-Tyrosine Kinases
  • Receptor, ErbB-2