Are erlotinib and gefitinib interchangeable, opposite or complementary for non-small cell lung cancer treatment? Biological, pharmacological and clinical aspects.

Eugenio Fiorentino, Antonio Russo, Giuseppe Cicero, Sergio Rizzo, Giuseppe Bronte, Marta Castiglia, Francesco Passiglia, Rolfo, C; Giovannetti, E; Pauwels, P; Vullo, Fl; Van Meerbeeck, J

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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.
Lingua originaleEnglish
pagine (da-a)300-313
Numero di pagine14
RivistaCRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY
Volume89
Stato di pubblicazionePublished - 2013

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Non-Small Cell Lung Carcinoma
Epidermal Growth Factor Receptor
Pharmacology
Protein-Tyrosine Kinases
erbB-1 Genes
Mutation
Therapeutics
Oncogenes
Pharmaceutical Preparations
Carcinogenesis
Pharmacokinetics
Lung
gefitinib
Erlotinib Hydrochloride
Neoplasms

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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.",
author = "Eugenio Fiorentino and Antonio Russo and Giuseppe Cicero and Sergio Rizzo and Giuseppe Bronte and Marta Castiglia and Francesco Passiglia and {Rolfo, C; Giovannetti, E; Pauwels, P; Vullo, Fl; Van Meerbeeck, J}",
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T1 - Are erlotinib and gefitinib interchangeable, opposite or complementary for non-small cell lung cancer treatment? Biological, pharmacological and clinical aspects.

AU - Fiorentino, Eugenio

AU - Russo, Antonio

AU - Cicero, Giuseppe

AU - Rizzo, Sergio

AU - Bronte, Giuseppe

AU - Castiglia, Marta

AU - Passiglia, Francesco

AU - Rolfo, C; Giovannetti, E; Pauwels, P; Vullo, Fl; Van Meerbeeck, J

PY - 2013

Y1 - 2013

N2 - 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.

AB - 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.

UR - http://hdl.handle.net/10447/104198

M3 - Article

VL - 89

SP - 300

EP - 313

JO - Critical Reviews in Oncology/Hematology

JF - Critical Reviews in Oncology/Hematology

SN - 1040-8428

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