Abstract: OBJECTIVE To investigate the progress in effects on anti-tumor and its mechanisms of tetrandrine. METHODS Literatures about the effects of tetrandrine on anti-tumor and its mechanisms have been reviewed and analyzed. RESULTS Tetrandrine can inhibit the growth of tumor cells. It also can reduce the incidence of tumor by antioxidation. Moreover, it can enhance the sensitivity to radiation by abrogating the G₂/M arrest induced by X-ray. Finally, it can reduce the toxic reaction caused by radiotherapy and chemotherapy. CONCLUSION Tetrandrine plays a great important role in anti-tumor though several different kinds of mechanism.