Objective To provide references for the further research and exploitation of Tetrandrine,we expatiate the progress in pharmacological effects on anti-tumor of Tetrandrine in recent years.Methods The literature about pharmacological effects on anti-tumor of Tetrandrine have been reviewed and analyzed which searched on Medline,Elsevierand CNKI database from 1994 to 2006.Results It was proved by experimentation that Tetrandrine not only inhibited some cancer cells proliferation,but also enhanced radiosensitizing effect of antitumor drug,altered multidrug resistance.The main anticancer mechanisms of Tetrandrine were inducing tumor cells apoptosis,down-regulating the expression of MRP.Conclusion Tetrandrine has various pharmacological actions and has a fine prospect in exploitation.