Chemotherapy is one of the traditional methods for cancer. It plays an important role in tumor therapy. Currently, the clinical commonly used antitumor drugs had defects like poor efficacy, side effects and so on, while it had many problems like taking long time and big input to develop new antitumor drugs. In recent years, studies have found that a large number of drugs which are of clear clinical safety and have been widely applied in clinic for non-tumor disease may have anti-tumor effect, such as astragalus, tripterygium wilfordii, metformin, aspirin and so on, and they were put into thorough research. In this paper reviewed were the research progress on antitumor effects of traditionally non-antitumor drugs.