title: Are erlotinib and gefitinib interchangeable, opposite or complementary for non-small cell lung cancer treatment? Biological, pharmacological and clinical aspects.
abstract: Gefitinib and erlotinib are the two anti-epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) approved for treatment of advanced NSCLC patients. These drugs target one of the most important pathways in lung carcinogenesis and are able to exploit the phenomenon of 'oncogene addiction', with different efficacy according to EGFR gene mutational status in tumor samples. Gefitinib has been approved only for EGFR mutation bearing patients regardless the line of treatment, while erlotinib is also indicated in patients without EGFR mutation who undergo second- or third-line treatment. Some studies evaluated the main differences between these drugs both for direct comparison and to improve their sequential use. In particular, toxicity profile resulted partially different, and these observations may be explained by several molecular and pharmacokinetic features. Therefore, this review integrates preclinical data with clinical evidences of TKIs to guide the optimization of currently available treatments in advanced NSCLC patients.
authors.affiliation: Medical Oncology, Department of Surgical and Oncology Sciences, University of Palermo, Palermo, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Bronte
authors.affiliation: Phase I-Early Clinical Trials Unit, Oncology Department and Multidisciplinary Oncology Center Antwerp (MOCA) Antwerp University Hospital, Edegem, Belgium.
authors.forename: Christian
authors.initials: C
authors.lastname: Rolfo
authors.affiliation: Department Medical Oncology, VU University Medical Center, Amsterdam, The Netherlands.
authors.forename: Elisa
authors.initials: E
authors.lastname: Giovannetti
authors.affiliation: Medical Oncology, Department of Surgical and Oncology Sciences, University of Palermo, Palermo, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Cicero
authors.affiliation: Molecular Pathology Unit, Pathology Department and Multidisciplinary Oncology Center Antwerp (MOCA) Antwerp University Hospital, Edegem, Belgium.
authors.forename: Patrick
authors.initials: P
authors.lastname: Pauwels
authors.affiliation: Medical Oncology, Department of Surgical and Oncology Sciences, University of Palermo, Palermo, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Passiglia
authors.affiliation: Medical Oncology, Department of Surgical and Oncology Sciences, University of Palermo, Palermo, Italy.
authors.forename: Marta
authors.initials: M
authors.lastname: Castiglia
authors.affiliation: Medical Oncology, Department of Surgical and Oncology Sciences, University of Palermo, Palermo, Italy.
authors.forename: Sergio
authors.initials: S
authors.lastname: Rizzo
authors.affiliation: Medical Oncology, Department of Surgical and Oncology Sciences, University of Palermo, Palermo, Italy.
authors.forename: Francesca Lo
authors.initials: FL
authors.lastname: Vullo
authors.affiliation: Surgical Oncology, Department of Surgical and Oncology Sciences, University of Palermo, Palermo, Italy.
authors.forename: Eugenio
authors.initials: E
authors.lastname: Fiorentino
authors.affiliation: Thoracic Oncology, Multidisciplinary Oncology Center Antwerp (MOCA) Antwerp University Hospital, Edegem, Belgium.
authors.forename: Jan
authors.initials: J
authors.lastname: Van Meerbeeck
authors.affiliation: Medical Oncology, Department of Surgical and Oncology Sciences, University of Palermo, Palermo, Italy. Electronic address: antonio.russo@usa.net.
authors.forename: Antonio
authors.initials: A
authors.lastname: Russo
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use*; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism / Q000473:pathology; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000235:genetics; D000069347:Erlotinib Hydrochloride; D000077156:Gefitinib; D006801:Humans; D008168:Lung / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism / Q000473:pathology; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011799:Quinazolines / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D000069347:Erlotinib Hydrochloride; D066246:ErbB Receptors; D000077156:Gefitinib
keywords: EGFR; Erlotinib; Gefitinib; Lung cancer; NSCLC; Tyrosine kinase