At the beginning, several first-generation EGFR-targeted TKIs, such as Erlotinib and Gefitinib, had been approved by U.S. FDA for the treatment of NSCLC patients that harbor activating mutations in the EGFR (L858R or delE746-A750) (Cohen et al., 2003; Cohen et al., 2005; Cataldo et al., 2011). The gene discussed is EGFR; the disease is non-small cell lung carcinoma.