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

Marta Castiglia, Giuseppe Cicero, Antonio Russo, Giuseppe Bronte, Eugenio Fiorentino, Francesco Passiglia, Patrick Pauwels, Christian Rolfo, Elisa Giovannetti, Jan Van Meerbeeck, Sergio Rizzo

Risultato della ricerca: Article

43 Citazioni (Scopus)

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 - 2014

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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

All Science Journal Classification (ASJC) codes

  • Hematology
  • Oncology
  • Geriatrics and Gerontology

Cita questo

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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 = "Marta Castiglia and Giuseppe Cicero and Antonio Russo and Giuseppe Bronte and Eugenio Fiorentino and Francesco Passiglia and Patrick Pauwels and Christian Rolfo and Elisa Giovannetti and {Van Meerbeeck}, Jan and Sergio Rizzo",
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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 - Castiglia, Marta

AU - Cicero, Giuseppe

AU - Russo, Antonio

AU - Bronte, Giuseppe

AU - Fiorentino, Eugenio

AU - Passiglia, Francesco

AU - Pauwels, Patrick

AU - Rolfo, Christian

AU - Giovannetti, Elisa

AU - Van Meerbeeck, Jan

AU - Rizzo, Sergio

PY - 2014

Y1 - 2014

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/10447/99172

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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