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

详细信息    查看全文

• 作者：Giuseppe Bronte ; Christian Rolfo ; Elisa Giovannetti ; Giuseppe Cicero ; Patrick Pauwels ; Francesco Passiglia ; Marta Castiglia ; Sergio Rizzo ; Francesca Lo Vullo ; Eugenio Fiorentino ; Jan Van Meerbeeck ; Antonio Russo
• 关键词：Lung cancer ; Gefitinib ; Erlotinib ; Tyrosine kinase ; EGFR ; NSCLC
• 刊名：Critical Reviews in Oncology/Hematology
• 出版年：February, 2014
• 年：2014
• 卷：89
• 期：2
• 页码：300-313
• 全文大小：1777 K

文摘

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 鈥榦ncogene addiction鈥? 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.