title: Gefitinib in non small cell lung cancer.
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.
authors.affiliation: Medical Oncology Unit, Thoraco-Pulmonary Department, National Cancer Institute, 80131 Napoli, Italy.
authors.forename: Raffaele
authors.initials: R
authors.lastname: Costanzo
authors.forename: Maria Carmela
authors.initials: MC
authors.lastname: Piccirillo
authors.forename: Claudia
authors.initials: C
authors.lastname: Sandomenico
authors.forename: Guido
authors.initials: G
authors.lastname: Carillio
authors.forename: Agnese
authors.initials: A
authors.lastname: Montanino
authors.forename: Gennaro
authors.initials: G
authors.lastname: Daniele
authors.forename: Pasqualina
authors.initials: P
authors.lastname: Giordano
authors.forename: Jane
authors.initials: J
authors.lastname: Bryce
authors.forename: Gianfranco
authors.initials: G
authors.lastname: De Feo
authors.forename: Massimo
authors.initials: M
authors.lastname: Di Maio
authors.forename: Gaetano
authors.initials: G
authors.lastname: Rocco
authors.forename: Nicola
authors.initials: N
authors.lastname: Normanno
authors.forename: Francesco
authors.initials: F
authors.lastname: Perrone
authors.forename: Alessandro
authors.initials: A
authors.lastname: Morabito
mesh_terms: D000970:Antineoplastic Agents / Q000009:adverse effects / Q000627:therapeutic use; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000627:therapeutic use; D000077156:Gefitinib; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy*; D009154:Mutation; D047428:Protein Kinase Inhibitors / Q000009:adverse effects / Q000627:therapeutic use*; D011799:Quinazolines / Q000009:adverse effects* / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D066246:ErbB Receptors; D000077156:Gefitinib