Although erlotinib has proven efficacy in metastatic NSCLC and has been reported to confer a survival benefit for advanced NSCLC patients harboring EGFR mutations, resistance to erlotinib also occurs and reduces its efficacy.41, 42, 43 To overcome the problem of resistance, we combined the microtubule-binding agent MPT0B271 with erlotinib to increase the antitumor effects in the erlotinib-resistant human NSCLC cell line A549. This evidence concerns the gene EGFR and non-small cell lung carcinoma.