Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase

Expert Rev Anticancer Ther. 2003 Jun;3(3):269-79. doi: 10.1586/14737140.3.3.269.


Overexpression of the epidermal growth factor receptor (EGFR) is correlated with a poor prognosis in several human malignancies. In addition, cancers overexpressing EGFR respond poorly to both chemotherapy and radiation therapy. Therefore, EGFR is a viable target for cancer therapy. This review will address how EGFR blockade modulates signal transduction, leading to alterations in the cell cycle progression with secondary inhibition of proliferation and differentiation of cancer cells. As a prototypical example, erlotinib (Tarceva), a reversible EGFR tyrosine kinase inhibitor will be discussed. This drug has demonstrated promising antitumor activity in Phase II trials in several solid tumors and definitive Phase III studies to demonstrate clinical benefit have completed accrual.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic / statistics & numerical data
  • Drug Delivery Systems / methods*
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / biosynthesis
  • ErbB Receptors / physiology*
  • Erlotinib Hydrochloride
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Quinazolines / administration & dosage*
  • Quinazolines / chemistry


  • Quinazolines
  • Erlotinib Hydrochloride
  • ErbB Receptors