Abstract: Objective To compare the recently curative, noxious and side effects of drug combination of CPT-11 plus CAP and 5-Fu/CF in the treatment of advanced colorectal cancer.Methods 77 cases of advanced colorectal cancer diagnosed by pathology and histology were divided into 2 groups randomly.Experimental group(39 cases):CPT-11100mg/m² was injected in 90 minutes in d1, 8, capecitabine 1000mg/m² was taken twice a day in d1-14.Control group(38 cases):CF 200 mg was injected in d1, 2, followed by the injection of 5-Fu 400mg/m² in d1, 2 and the micro pumping of 5-Fu 600mg/m² over 48 hours in d2.The treatment was repeated every three weeks as one cycle and the treatment effect was evaluated after 2 cycles.Results The total effective rates of experimental group(39 cases)and control group(38 cases)are 48.7%(19cases)and 21.1%(8 cases), respectively.There is statistical significance between the two groups(P＜ 0.025).The main noxious and side effects were delayed diarrhea, leucopenia, nausea and vomiting, etc.There was no treatment related death.Conclusion The curative effect of drug combination of CPT-11 plus CAP is superior to 5-Fu/CF in the treatment of advanced colorectal cancer and the combination was recommended to be used widely.