6533b7d5fe1ef96bd1265243
RESEARCH PRODUCT
Are erlotinib and gefitinib interchangeable, opposite or complementary for non-small cell lung cancer treatment? Biological, pharmacological and clinical aspects
Sergio RizzoMarta CastigliaChristian RolfoJan P. Van MeerbeeckGiuseppe CiceroPatrick PauwelsFrancesco PassigliaGiuseppe BronteFrancesca Lo VulloAntionio RussoElisa GiovannettiEugenio Fiorentinosubject
Oncologymedicine.medical_specialtyLung NeoplasmsEGFR; Erlotinib; Gefitinib; Lung cancer; NSCLC; Tyrosine kinaseSettore MED/06 - Oncologia MedicaEGFRAntineoplastic Agentsmedicine.disease_causeNSCLCErlotinib HydrochlorideGefitinibGrowth factor receptorPharmacokineticsCarcinoma Non-Small-Cell LungInternal medicineHumansMedicineLung cancerLungProtein Kinase InhibitorsneoplasmsTyrosine kinasebusiness.industryGefitinibHematologyOncogene Addictionmedicine.diseaserespiratory tract diseasesErbB ReceptorsOncologyErlotinibQuinazolinesHuman medicineErlotinibLung cancerbusinessCarcinogenesisTyrosine kinasemedicine.drugdescription
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 pharmacoldnetic features. Therefore, this review integrates preclinical data with clinical evidences of TKIs to guide the optimization of currently available treatments in advanced NSCLC patients. (C) 2013 Published by Elsevier Ireland Ltd.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2014-01-01 |