Abstract: Objective: To evaluate the efficacy of oral vinorelbine plus cisplatin and IV vinorelbine plus cisplatin in ad -vanced non-small-cell lung cancer (NSCLC), and to appraise the progression-free survival, toxicity, and the safety of both therapeutic applications. Methods:Patients who met the inclusion criteria were randomly (1:1) assigned to the experimental group with oral vinorelbine plus cisplatin (arm A) or the control group with intravenous ( Ⅳ) vinorelbine plus cisplatin (arm B). Patients in both the groups were treated with the two therapeutic regimens administered once every 3 weeks. In the first course of treatment, the oral vinorelbine was administrated at a dose of 60mg/m2 on day1 and 8, while the IV vinorel-bine was administrated at a dose of 25mg/m2 on day1 and 8. In both groups, cisplatin was administrated at the dose of 80mg/m2 on day1. In the second course of treatment, the dose of oral vinorelbine was raised up to 80mg/m2and the IV vinorelbine was raised to30mg/m2 for the following cycles, if no severe hematological toxicity was found in these patients. Tumor response rate was appraised according to RECIST criteria, and the toxicity grading was appraised based on NCI-CTC Version 2.0. Results:A total of 39eligible subjects were enrolled in the Cancer Center of Sun Yat-Sen University, with 19in the experimental group and 20controls. Characteristics including gender, age, performance status, clinical stage, histo-types and smoking status were balanced in the patients of both groups. Data were analyzed in the intention-to-treat manner. The objective remission rate was 31.6% and 42.1% (P=0.737 ), and the clinical benefit rate was 52.6% and 68.4% (P=0.508 ) in arm A and B, respectively. The median progression-free survival was 85and 115 days, respectively, in arm A and B ( P=0.705 ). Toxic reactions in both groups included neutropenia, anemia, gastrointestinal reactions and phlebitis. Grade-2 phlebitis notably increased in arm B ( 68.4% vs.21.0%), with a statistically significant difference between the two groups ( P=0.008 ). No significant differences were found in the comparison of other adverse effects and grade- Ⅲ～Ⅳun toward reactions between the subjects of the 2 groups. Conclusion:The efficacy of oral vinorelbine plus cisplatin regimen is similar to that of the IV vinorelbine and cisplatin regimen in the cases with advanced non-small-cell lung cancer (NSCLC). The hematological toxicity and non-hematological toxicity were lower in the experimental group than in the controls. A larg- er-scale phase- Ⅲclinical study is needed to further evaluate the efficacy and toxicity of oral vinorelbine in Asian patients.