Osteosarcoma, a primary malignant bone tumor originating from mesenchymal cells, is the most prevalent bone malignancy in children and adolescents. Current standard treatment involves aggressive surgical resection aimed at maximal tumor removal; however, this inevitably creates extensive bone defects that substantially impair patients’ quality of life. Furthermore, the risks of postoperative tumor recurrence and metastasis critically influence therapeutic outcomes. With the continuous advancement of biomaterials, their applications in postsurgical osteosarcoma management have increased substantially. Biomaterial-based strategies are enabling diverse antineoplastic function and bone regeneration strategies. However, previous biomaterial strategies have typically focused on osteogenic or antitumor functions in isolation. The current research frontier is shifting toward developing integrated strategies that simultaneously achieve both effective tumor suppression and functional bone regeneration. This review strategically categorizes these emerging strategies into 3 distinct approaches: (a) Traditional bifunctional strategies: Integrating coloaded osteogenic and antitumor agents within a carrier. (b) Enhanced antitumor bifunctional strategies: Incorporating components or designs that actively boost the potency of the antitumor modality beyond simple codelivery. (c) Temporally controlled sequential strategies: Engineered to perform antitumor and pro-regeneration functions in a defined, sequential order. By critically analyzing the cutting-edge biomaterials employed in these strategies, we assessed their potential for clinical translation, emphasized the ongoing technical barriers, and outlined the challenges for future development.