Abstract: Objective To compare the clinical efficacy and toxicity of irinotecan combined with Tegafur or 5-fluorouracil in the treatment for advanced rectal cancer patients. Methods Seventy-seven advanced gastric cancer patients, who received failed platiniferous regimen, were randomly divided into two groups, 36 patients in Group A were treated with irinotecan and Tegafur and 41 patients in Group B were treated with irinotecan and 5-fluorouracil. Curative effect and adverse reaction were evaluated according to WHO standard. Results The objective response rates in Group A and B were 41.7% and 39.2% individually. The major adverse reaction in Group A was tolerably hematologic toxicity, including thrombocytopenia leukopenia, anemia, diarrhea, etc. While main side effects in Group B were phlebitis, gastrointestinal reactions, etc. The median time to progression (TTP) in Group A and Group B were 4.8 and 3.1 months(P=0.001), respectively. Conclusion Both of two combined chemotherapy regimens have good curative effect, while Group A has longer TTP, milder adverse reaction and shorter hospitalization time.Irinotecan and tegafur could be a secondline chemotherapy for advanced gastric cancer patients who received failed platiniferous regimen.