The invention belongs to the field of medicine and biotechnology, and relates to a synergistic drug compound for treating tumors and a preparation method thereof. The drug compound is composed of one or more cell autophagy inhibitors and arginase, especially human recombinant Arginase is made into a synergistic drug compound for treating tumors, and the synergistic drug compound can inhibit autophagy by inhibiting autophagy through autophagy inhibitors to increase tumor cells' ability to arginase. sensitivity, and enhance the therapeutic effect of arginase, especially human recombinant arginase, on tumors, especially triple-negative breast cancer cells. The drug compound of the present invention can be used for clinical treatment of breast cancer, melanoma, lung cancer, brain tumor, lymphoma, leukemia and myeloma.