Abstract: Objective To evaluate clinical efficacy and adverse events of gefitinib in patients of non-small cell lung cancer（NSCLC）with brain metastasis. Methods NSCLC patients with brain metastases were treated with gefitinib. Gefitinib was given orally 250mg/d. The effect was evaluated according to RECIST 1.0 criterion. Survival analysis was compared with Kaplan-Meier method and Log-rank test respectively. The multivariate analysis was performed with Cox’s proportion risk model. Results Of all the 40 patients， in terms of intracranial lesions， complete response（CR） was observed in 3 patients（7.5％）， partial response（PR） was observed in 10 patients（25.0％）， stable disease（SD） in 26 patients（65.0％） and progressive disease（PD） in 1 patients（2.5％）， objective response rate（ORR） and disease control rate（DCR） were 32.5％ and 97.5％， respectively. As for systemic disease， PR was observed in 14 patients（35.0％）， SD in 23 patients（57.5％） and PD in 3 patients（7.5％）， RR and DCR were 35.0％ and 92.5％， respectively. The median time to disease progression（mTTP） was 245 days and it was related to the onset of brain metastasis（P=0.000） and solitary brain metastasis（P=0.015）， but there was no statistical difference among different subtypes of gender，age， brain radiotherapy，treatment opportunity，and smoking（P＞0.05）. The median overall survival time（mOS） was 590 days， and 1- and 2-year survival rates were 77.5％ and 30.0％， respectively. The multivariate analysis showed that OS had no statistical difference among subtypes. The improvement rates of respiratory systerm and nervous system were 67.7%（12/18） and 85.7%（12/14）. The common side effects were rash and diarrhea, which were mainly in grade 1-2.Conclusion The patients with heterochronous brain metastasis or solitary brain metastasis may have better time to progression. Gefitinib may be effective and tolerable in NSCLC patients with brain metastasis and appears to be a possible new treatment option.