Epidermal growth factor receptor first generation tyrosine-kinase inhibitors

The epidermal growth factor receptor (EGFR) oncogene was positioned as an attractive target for drug development in non-small cell lung cancer (NSCLC). Gefitinib and erlotinib were the first two reversible inhibitors of the EGFR kinase. The discovery of EGFR kinase domain-activating mutations that significantly correlated with a high likelihood of response to EGFR tyrosine-kinase inhibitors (TKIs) allowed to design studies to test these drugs as potential first-line therapies. In the same way, the feasibility of personalized medicine was established in patients with advanced NSCLC. Currently in the field of NSCLC with EGFR mutation have developed second and even third generation TKIs that would be gaining the positioning in the treatment of this subset population of NSCLC. In spite of this, without the knowledge that EGFR first generation TKIs have provided, we would not have gotten so far. We will review step by step how it was forged the exciting history of the subpopulation of lung cancer with EGFR mutated, through the various clinical trials performed with first generation TKIs that changed the focus, the future of NSCLC as well as survival of these patients.