PMID- 21660144 OWN - NLM STAT- MEDLINE DCOM- 20111003 LR - 20240317 IS - 1110-7251 (Electronic) IS - 1110-7243 (Print) IS - 1110-7243 (Linking) VI - 2011 DP - 2011 TI - Gefitinib in non small cell lung cancer. PG - 815269 LID - 10.1155/2011/815269 [doi] LID - 815269 AB - 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. FAU - Costanzo, Raffaele AU - Costanzo R AD - Medical Oncology Unit, Thoraco-Pulmonary Department, National Cancer Institute, 80131 Napoli, Italy. FAU - Piccirillo, Maria Carmela AU - Piccirillo MC FAU - Sandomenico, Claudia AU - Sandomenico C FAU - Carillio, Guido AU - Carillio G FAU - Montanino, Agnese AU - Montanino A FAU - Daniele, Gennaro AU - Daniele G FAU - Giordano, Pasqualina AU - Giordano P FAU - Bryce, Jane AU - Bryce J FAU - De Feo, Gianfranco AU - De Feo G FAU - Di Maio, Massimo AU - Di Maio M FAU - Rocco, Gaetano AU - Rocco G FAU - Normanno, Nicola AU - Normanno N FAU - Perrone, Francesco AU - Perrone F FAU - Morabito, Alessandro AU - Morabito A LA - eng PT - Journal Article PT - Review DEP - 20110523 PL - United States TA - J Biomed Biotechnol JT - Journal of biomedicine & biotechnology JID - 101135740 RN - 0 (Antineoplastic Agents) RN - 0 (Protein Kinase Inhibitors) RN - 0 (Quinazolines) RN - EC 2.7.10.1 (ErbB Receptors) RN - S65743JHBS (Gefitinib) SB - IM MH - Antineoplastic Agents/adverse effects/therapeutic use MH - Carcinoma, Non-Small-Cell Lung/*drug therapy MH - ErbB Receptors/*antagonists & inhibitors/genetics/therapeutic use MH - Gefitinib MH - Humans MH - Lung Neoplasms/*drug therapy MH - Mutation MH - Protein Kinase Inhibitors/adverse effects/*therapeutic use MH - Quinazolines/*adverse effects/*therapeutic use PMC - PMC3110340 EDAT- 2011/06/11 06:00 MHDA- 2011/10/04 06:00 PMCR- 2011/05/23 CRDT- 2011/06/11 06:00 PHST- 2010/12/17 00:00 [received] PHST- 2011/03/15 00:00 [accepted] PHST- 2011/06/11 06:00 [entrez] PHST- 2011/06/11 06:00 [pubmed] PHST- 2011/10/04 06:00 [medline] PHST- 2011/05/23 00:00 [pmc-release] AID - 10.1155/2011/815269 [doi] PST - ppublish SO - J Biomed Biotechnol. 2011;2011:815269. doi: 10.1155/2011/815269. Epub 2011 May 23.