Authors: Catassi, Alessia; Cesario, Alfredo; Granone, Pierluigi; Russo, Patrizia

Source: Current Respiratory Medicine Reviews, Volume 3, Number 2, May 2007 , pp. 159-167(9)

Publisher: Bentham Science Publishers

Abstract:

The human epidermal growth factor receptor (EGFR) biology is not completely explained; however EGFRtargeting has formed the basis of extensive and growing drug development. Inhibition of receptor tyrosine kinase activity involved in the EGFR signalling cascade is a fundamental mechanism for the use of EGFR specific tyrosine kinase (TK) inhibitors exemplified by gefitinib (ZD1839, Iressa) and erlotinib (OSI-774, Tarceva). Despite initially promising results in chemotherapy-resistant patients with non small cell lung cancer (NSCLC), disappointing results from phase III trials of gefitinib in NSCLC have been of concern of some. When EGFR-targeting drugs were introduced into the clinic, the specific targets affected in human tumors were unknown. Recently, different studies reported that mutations in the TK domain of EGFR are strongly associated with gefitinib- or erlotinib-sensitivity in patients with NSCLC. This article reviews the rationale for targeting EGFR by TK inhibitors, the discovery of EGFR mutations and subsequent studies to define the incidence, spectrum and functions of EGFR mutations. This paper represents the effort of a lung cancer focused translational research team made up of molecular biologists, medical oncologists and thoracic surgeons. The final objective is to achieve a comprehensive, but simple, review of the current status of the shift from cytotoxic to molecularly targeted therapy in lung cancer treatment potentially useful in the planning of translational research trials.

Keywords: EGFR family; Non-small cell lung cancer (NSCLC); cell proliferation; Gefitinib; OSI-774

Document Type: Research article

DOI: http://dx.doi.org/10.2174/157339807780599135

Affiliations: 1: Translational Research B (Lung Cancer), Department of Integrated Medical Oncology, National Cancer Institute, Largo Rosanna Benzi 10, I-16132 Genoa, Italy.

Publication date: 2007-05-01

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• Current Respiratory Medicine Reviews publishes frontier reviews on all the latest advances on respiratory diseases and its related areas e.g. pharmacology, pathogenesis, clinical care, and therapy. The journal's aim is to publish the highest quality review articles dedicated to clinical research in the field. The journal is essential reading for all researchers and clinicians in respiratory medicine.

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