Abstract Ferroptosis is an iron‐dependent form of regulated cell death driven by lipid peroxidation, characterized by distinct ultrastructural alterations such as mitochondrial shrinkage and disruption of cristae. As an emerging therapeutic target in oncology, ferroptosis opens new therapeutic perspectives for a range of diseases, including cancer. Recent studies have demonstrated that ferroptosis induction exhibits superior efficacy in tumor regulation compared to certain conventional treatment modalities. However, the process of ferroptosis is intricately regulated by multiple signaling pathways involving iron metabolism, lipid metabolism, and disturbances in redox homeostasis, thereby limiting the effectiveness of single‐induction strategies. With advances in nanotechnology, a variety of nanomaterials have been engineered to induce ferroptosis through multi‐level regulatory systems or to serve as delivery vehicles for small‐molecule agents, significantly enhancing targeting capability toward tumor tissues. This review systematically summarizes recent advances in the molecular mechanisms, regulatory networks, pathological roles, small‐molecule inducers, and nanocarrier‐based targeted therapeutic strategies related to ferroptosis. It should be noted that, as a rapidly evolving research field, the application of ferroptosis in cancer therapy remains at an early stage. This article further discusses key challenges and future directions for its translation into clinical precision therapies, and concludes with critical scientific questions that demand urgent investigation in future research.
Xu et al. (2026) studied this question.