Abstract: Because of the advantages of the low toxicity, specificity and nonresistance compared with chemotherapy, the peptides with antitumor activity had become the research hotspot. Here, we reviewed the sources and preparation techniques, quantitative structure activity relationships (QSAR) and antitumor mechanism of the antitumor peptides, and pointed out their prospects and possible problems in tumor therapy based on the achievement of the home and abroad research over the past decades.