作者: Mauricio Burotto , Syed Abbas Ali , Geraldine O’Sullivan Coyne
DOI: 10.1517/14740338.2014.973400
关键词: Tyrosine-kinase inhibitor 、 Internal medicine 、 EGFR inhibitors 、 Gefitinib 、 Clinical trial 、 Erlotinib 、 Afatinib 、 Erlotinib Hydrochloride 、 Medicine 、 Oncology 、 Context (language use) 、 Pharmacology
摘要: Introduction: The past decade has seen the development and widespread use of tyrosine kinase inhibitors (TKIs) targeting a mutated EGFR (mEGFR) for treatment metastatic NSCLC. We discuss main properties TKIs currently recommended mEGFR NSCLC: gefitinib, erlotinib afatinib.Areas covered: mechanism action, pharmacodynamics pharmacokinetics these drugs, with emphasis on historical context their preclinical clinical development, will be covered, including potential resistance mechanisms to first-generation that driven trial design second third generations inhibitors. Six Phase III trials comparing three cisplatin-based chemotherapy upfront NSCLC provide basis comparative safety toxicity analysis between agents. Class-related inhibitors, life-threatening effects, discussed.Expert opinion: Toxicity anal...