Abstract
Introduction: EGFR targeting is a valid and vital approach in the treatment of patients with lung cancer. However, all patients treated with reversible inhibitors develop acquired resistance over time. It is of paramount importance that novel agents are designed and developed to overcome such acquired resistance.Areas covered: The role of EGFR targeting in NSCLC, mechanisms of primary and acquired resistance to reversible inhibitors, and strategies to overcome resistance are examined. Preclinical and clinical data pertaining to BIBW 2992 in advanced solid tumors, and particularly in NSCLC, are also thoroughly reviewed. We hope that the reader will gain a comprehensive knowledge of the emerging field of resistance to EGFR inhibition, specifically relating to drugs being developed for lung cancer patients.Expert opinion: Irreversible dual inhibitors of EGFR-HER2 such as BIBW 2992 provide a promising approach to overcoming acquired resistance to erlotinib and gefitinib in lung cancer. It is yet to be seen whether the drug can overcome primary drug resistance or delay time to development of acquired resistance to EGFR-targeted agents in NSCLC.
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