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

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42 Citations (Scopus)

Abstract

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.

Original languageEnglish (US)
Pages (from-to)269-279
Number of pages11
JournalExpert Review of Anticancer Therapy
Volume3
Issue number3
StatePublished - Jun 2003

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Drug Delivery Systems
Epidermal Growth Factor Receptor
Protein-Tyrosine Kinases
Neoplasms
Cell Differentiation
Signal Transduction
Cell Cycle
Radiotherapy
Erlotinib Hydrochloride
Drug Therapy
Pharmaceutical Preparations
Therapeutics

Keywords

  • EGFR
  • Erlotinib
  • Phosphorylation
  • Tarceva®
  • Tyrosine kinase

ASJC Scopus subject areas

  • Pharmacology
  • Cancer Research

Cite this

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abstract = "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{\circledR}), 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.",
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AU - Goel, Sanjay

AU - Perez-Soler, Roman

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AB - 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.

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