Background and objective Malignant grade and death rate are very high for non-small cell lung cancer, and gefitinib is a new molecule target anticancer drug. The aim of this meta analysis is to evaluate the clinical efficacy and safety of gefitinib for non-small cell lung cancer. Methods We searched the Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library, Issue 8, 2010), PubMed (1966-2010.8), EMBASE (1974-2010.8), CNKI (1994-2010.8), VIP (1989-2010.8), and CMD Digital Periodicals (1998-2010.8). Two reviewers independently evaluated the quality of the included studies and extracted the data. Meta-analyses were performed by RevMan 5.0 software. Results Thirteen randomized controlled trials (RCTs) involving 6,207 patients were included. The results of meta-analyses showed that: gefitinib showed no remarkable advantage in media survival time, 1 year survival rate, complete response rate (CRR), partial response rate (PRR), stable disease (SD) when compared to Placebo, Docetaxel, Cisplatin+Docetaxel, Pemetrexed. Gifitinib could increase overall survival rate compared to Docetaxel, Cisplatin+Docetaxel (RR=1.41, 95%CI: 1.10-1.80; RR=1.93, 95%: 1.26-2.94). When compared to Placebo, Docetaxel, gifitinib could improve life quality of Total-FACT-L improve rate (RR=1.42, 95%CI: 1.16-1.74; RR=1.66, 95%CI: 1.39-1.97). The major adverse event for gifitinib were rash/acne, dry skin, diarrhea. While gifitinib showed lower hematology toxicity. Conclusion Gifitinib shows more superiority for non-small cell lung cancer, and its clinical application is worthy to be advocated.