In this study, we examined the anti-cancer effect of gefitinib (trade name “Iressa”), an orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) on TGF-β-mediated EMT in NSCLC cells and the effect of its combination with integrin receptor antagonist cilengitide. The gene discussed is TGFB1; the disease is non-small cell lung carcinoma.