Objective:To observe the clinical effects and toxicity of gefitinib in treatment of patients with advanced non-small cell lung cancer (NSCLC) who failed to respond to prior chemotherapy. Methods: Sixty-four patients with advanced NSCLC were admitted to our hospital from Jun. 2005 to Aug. 2009. Gefitinib was given orally (250 mg) once daily to NSCLC patients until disease progression or the development of intolerable toxicity, and the clinical results were observed. Results: No patients showed complete response (CR), 22 patients showed partial response (PR), 23 patients maintained stable disease (SD), and 19 patients had disease progression (PD), with the overall response rate (CR+PR) being 34.38%, the stability disease rate being 35.94%, and disease control rate (CR+PR+SD) being 70.31%. The median survival period in our group was 5.9 months. Twenty-three patients of 64 (35.94%) were alive till the follow-up time. The effect of gefitinib was associated with gender and smoking (P<0.05), with better effect seen in females and non-smokers. The most common drug-related adverse events included grade ⅠorⅡ skin rash (32.81%, 26.57%) and diarrhea (12.5%). Conclusion:Gefitinib can relieve NCSLC-related symptoms in chemotherapy-resistant advanced NCSLC patients, especially in females and non-smokers; it is a safety, effective, and tolerable drug.