Tumors endanger the lives of individuals worldwide. They form and metastatize to nearby and distant tissues and organs in several ways, which greatly increase the difficulty of therapy. The continuous development and progress in nanomedicine has provided new insights in the treatment of tumors. Owing to their excellent properties of barium titanate (BaTiO 3 , BTO), especially piezoelectricity, BTO‐based nanomaterials have become popular among tumor therapy researchers in recent years. BTO‐based sonodynamic therapy (SDT) is considerably advanced than traditional therapies. Herein, first, the properties, structure, preparation technology, and working mechanism of BTO under ultrasonic stimulation is systematically introduced. Second, the research progress in BTO‐mediated SDT, electrical stimulation therapy, and BTO‐based SDT‐derived multimodal synergistic therapy in the field of tumor therapy is reviewed. Third, the biocompatibility, biodistribution, and bioelimination of BTO is summarized. Finally, the current problems associated with BTO‐mediated SDT as well as potential obstacles and opportunities in oncology and other biomedical fields are summarized and prospected.