Our results show that FZKA enhances the effect of Gefitinib-induced lung cancer cell apoptosis via inhibition of STAT3, followed by increasing protein expression of Bax and Bim, concomitantly decreasing Bcl-2 and Mcl-1 protein levels, leading to decrease of MMP and release of Cyt-C from mitochondria to cytoplasm, and significantly activating Caspase-9 and Caspase-3. Here, STAT3 is linked to lung cancer.