Described herein is use of a Caspase activator and an oncolytic virus in the preparation of an anti-tumor drug. As described, Caspase activator can enhance the anti-tumor effect of oncolytic virus, and the combination of Caspase activator and oncolytic virus produces a significant synergistic anti-tumor effect, and demonstrates an effective therapy for the treatment of tumors that are less sensitive to other pharmaceutical treatments.本發明屬於生物醫藥領域,涉及Caspase活化劑與溶瘤病毒的聯用在製備抗腫瘤藥物中的應用。本發明首次發現Caspase活化劑可以增加溶瘤病毒的抗腫瘤效應,兩者聯用起到極強的協同性作用,對用藥敏感性不高的腫瘤治療來說提供了一個有效的治療方案。