Class act: safety comparison of approved tyrosine kinase inhibitors for non-small-cell lung carcinoma

作者: Mauricio Burotto , Syed Abbas Ali , Geraldine O’Sullivan Coyne

DOI: 10.1517/14740338.2014.973400

关键词: Tyrosine-kinase inhibitorInternal medicineEGFR inhibitorsGefitinibClinical trialErlotinibAfatinibErlotinib HydrochlorideMedicineOncologyContext (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...

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