Abstract: OBJECTIVE To evaluate the concentration, efficacy and toxicity of docetaxel in the treatment of advanced non-small cell lung cancer (NSCLC) by administration at different times. METHODS Sixty patients with locally advanced or metastatic NSCLC were enrolled into the study and divided to three groups. Each group were administrated of docetaxel at different time. A: administration at 8∶00 am (n=20), B: administration at 2∶00 pm (n=20), C: administration at 8∶00 pm (n=20)；cisplatin was administered at second day. Docetaxel 40 mg·m^-2, ivgtt, d1, 8; cisplatin 75 mg·m^-2, ivgtt, d1, every 21 days. HPLC was established for the determination of docetaxel at 1, 10, 24 h after administration, and evaluate the efficacy and toxicity after two cycles. RESULTS There was no statistic difference, but the main toxicities of B, C groups were higher. CONCLUSION A group is a better method for the treatment of NSCLC with mild toxicity and appropriate, it can be recommended for further clinical trail.