Chemotherapy is one of the main tumor therapy in clinic,but the system toxicity of antitumor agent and its low concentration in the specific tumor position are still important disturbing factors in tumor treatment.Prodrug,which is from the modification of active drug constructure or pharmaceutical dosage form,greatly overcome the defect of chemotherapy agent and open a new way in target tumor treatment.At present,new advanced antitumor prodrugs contain directed-enzyme activated prodrug,carrier prodrug,lipophilic prodrug and so on.Several antitumor prodrugs have been reviewed.