OBJECTIVE： To evaluate therapeutic efficacy and safety of ubenimex combined with chemotherapy in the treatment of malignant tumor， and to provide evidence-based reference in clinic. METHODS： Retrieved from Central， PubMed， CJFD， VIP and Wanfang database，  randomized controlled trials （RCTs） about ubenimex combined with chemotherapy （trial group） vs. single chemotherapy （control group） in the treatment of malignant tumor were collected. The quality of studies were evaluated by bias risk evaluation criteria of Cochrane system evaluator manual 5.1.0 after screening literatures and extracting data. Meta-analysis was performed by using Rev Man 5.3 statistical software. RESULTS： A total of 12 RCTs were included， involving 762 patients. The results of Meta-analysis showed that： shorter-term response rate [RR＝1.24，95％CI（1.08，1.43），P＝0.002] and the improvement rate of life quality Karnofsky score [RR＝1.69，95％CI（1.46，1.95），P＜0.001] in trial group were significantly higher than control group； the incidence of gastrointestinal toxicity [RR＝0.74，95％CI（0.57，0.94），P＝0.02] and leucocyte suppression rate[Ⅰ°-Ⅳ°（＜3 months）：RR＝0.54， 95％CI（0.37，0.79），P＝0.002；Ⅲ°-Ⅳ°：RR＝0.44， 95％CI（0.29，0.68），P＜0.001] were significantly lower than control group， with statistical significance. CONCLUSIONS： Ubenimex combined with chemotherapy can improve malignant tumor， shorter-term efficacy and life quality， and reduce gastrointestinal and marrow toxicity.