Acute kidney injury (AKI) is a major health concern owing to its high morbidity and mortality rates, to which there are no drugs or treatment methods, except for renal replacement therapy. Therefore, identifying novel therapeutic targets and drugs for treating AKI is urgent. Ferroptosis is an iron-dependent and lipid-peroxidation-driven regulatory form of cell death and is closely associated with the occurrence and development of AKI. Traditional Chinese medicine (TCM) has unique advantages in treating AKI due to its natural origin and efficacy. In this review, we summarize the mechanisms underlying ferroptosis and its role in AKI, and TCM compounds that play essential roles in the prevention and treatment of AKI by inhibiting ferroptosis. This review suggests ferroptosis as a potential therapeutic target for AKI, and that TCM compounds show broad prospects in the treatment of AKI by targeting ferroptosis.