Abstract: Ferroptosis is intricately associated with the pathological mechanisms of central nervous system(CNS) diseases. However, the translational development of therapeutic agents faces significant challenges due to physiological structures such as the blood-brain barrier and the high susceptibility of the neural environment. This review summarizes recent advances in pharmacotherapeutic strategies targeting ferroptosis for CNS diseases, with a focus on the molecular regulatory mechanisms and clinical treatment approaches. Specifically, it discusses the application of nanodrug delivery systems modulating three core pathways: iron metabolism, lipid peroxidation, and the antioxidant system. Furthermore, the review highlights recent progress in integrated ferroptosis theranostic platforms and provides perspectives on current challenges and future directions, aiming to offer new insights for clinical diagnosis and treatment of CNS diseases.