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Journal of Biomedicine and Biotechnology
Volume 2011 (2011), Article ID 815269, 14 pages
http://dx.doi.org/10.1155/2011/815269
Review Article

Gefitinib in Non Small Cell Lung Cancer

1Medical Oncology Unit, Thoraco-Pulmonary Department, National Cancer Institute, 80131 Napoli, Italy
2Clinical Trials Unit, National Cancer Institute, 80131 Napoli, Italy
3Medical Oncology Unit, Azienda Ospedaliera Pugliese-Ciaccio, 88100 Catanzaro, Italy
4Direzione Scientifica, National Cancer Institute, 80131 Napoli, Italy
5Thoracic Surgery, Thoraco-Pulmonary Department, National Cancer Institute, 80131 Napoli, Italy
6Cellular Biology and Biotherapy, National Cancer Institute, 80131 Napoli, Italy
7Centro di Ricerche Oncologiche di Mercogliano (CROM), 83013 Mercogliano, Italy

Received 17 December 2010; Accepted 15 March 2011

Academic Editor: Cesare Gridelli

Copyright © 2011 Raffaele Costanzo et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Gefitinib is an oral, reversible, tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) that plays a key role in the biology of non small cell lung cancer (NSCLC). Phase I studies indicated that the recommended dose of gefitinib was 250 mg/day. Rash, diarrhea, and nausea were the most common adverse events. The positive results obtained in early phase 2 clinical trials with gefitinib were not confirmed in large phase 3 trials in unselected patients with advanced NSCLC. The subsequent discovery that the presence of somatic mutations in the kinase domain of EGFR strongly correlates with increased responsiveness to EGFR tyrosine kinase inhibitors prompted phase 2 and 3 trials with gefitinib in the first line-treatment of EGFR-mutated NSCLC. The results of these trials have demonstrated the efficacy of gefitinib that can be now considered as the standard first-line treatment of patients with advanced NSCLC harbouring activating EGFR mutations.