Objective To systematically review the cost-effectiveness of gefitinib for advanced non-small cell lung cancer (NSCLC), in order to provide the economics values of gefitinib for clinical application. Method We electronically searched databases including PubMed, Ovid, Embase, Cochrane Library, Medline, China National Knowledge Internet, VIP, and Wanfang database for articles about the cost-effectiveness of gefitinib for advanced NSCLC patients from January 1946 to October 2017, and then performed a systematic literature review of economic evaluations of geftinib. Results A total of 20 independent studies were included in the present systematic review, in which 8 were the first-line treatment, 9 were the second-line treatment, 1 was the third-line treatment, and 2 were maintenance treatment. The most common comparison was gefitinib vs. chemotherapy (n=7), and other comparisons were gefitinib vs. erlotinib (n=4), gefitinib vs. docetaxel (n=3), gefitinib vs. placebo (n=2), gefitinib vs. icotinib (n=2), gefitinib vs. afatinib (n=1), and gefitinib vs. other treatments (n=1). For the advanced NSCLC patients, the first- or second-line treatment with gefitinib compared to chemotherapy was considered to be more cost-effective, especially in patients with mutated epidermal growth factor receptor gene. As the second-line treatment, gefitinib was considered to be more economical than erlotinib and docetaxel. Conclusion Gefitinib is considered to be a cost-effective strategy for the advanced NSCLC patients as the first- or second-line therapy.