Abstract: Objective: To investigate the efficacy of rubitecan for patients with malignant tumor and to ob -serve patients’tolerance to rubitecan. Methods:The laboratory examinations (including blood and urine rou -tine examination, coagulation test, blood biochemical test and electrocardiogram) were performed in patients treated with rubitecan orally once or continuously. Imaging for efficacy evaluation was carried out after continu -ous treatment of one cycle. Results: Thirty patients were enrolled into the single experiment and 20patients were enrolled into the consecutive experiment. The major adverse effects were Ⅰ~ Ⅱhematological toxicity, proteinuria, nausea, vomiting, and electrocardiographic changes. The efficacy could be assessed in 13pa-tients. PR was obtained in 1 patient and SD was obtained in8 patients. The disease control rate (DCR) was 69.2%.Conclusion:Oral administration of rubitecan is effective for patients with advanced and drug-resistent malignant tumor and can be well tolerated.