کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
3328928 1212362 2012 15 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): A better mousetrap? A review of the clinical evidence
موضوعات مرتبط
علوم پزشکی و سلامت پزشکی و دندانپزشکی هماتولوژی
پیش نمایش صفحه اول مقاله
Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): A better mousetrap? A review of the clinical evidence
چکیده انگلیسی

The discovery of activating epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer (NSCLC) in 2004 heralded the era of molecular targeted therapy in NSCLC. First-generation small molecule, reversible tyrosine kinase inhibitors (TKIs) of EGFR, gefitinib and erlotinib, had been approved for second- or third-line treatment of NSCLC prior to the knowledge of these mutations. However, resistance to gefitinib and erlotinib invariably develops after prolonged clinical use. Two second-generation irreversible EGFR TKIs, afatinib (BIBW 2992) and dacomitinib (PF-00299804), that can potentially overcome the majority of these resistances are in late stage clinical development. Here I will review the clinical data of EGFR TKIs and discuss the appropriate future role of afatinib and dacomitinib in NSCLC: whether as replacement of erlotinib or gefitinib or only after erlotinib or gefitinib failure and whether different subgroups would benefit from different approaches.


► The development of reversible EGFR inhibitors was a critical step in NSCLC therapy.
► Recently, irreversible and/or multitargeted inhibitors have also been evaluated.
► Clinical trials will help to determine the potential activity of these agents.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Critical Reviews in Oncology/Hematology - Volume 83, Issue 3, September 2012, Pages 407–421
نویسندگان
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