Ferroptosis is closely related to iron metabolism, lipid metabolism, and amino acid metabolism, which contribute to the production of reactive oxygen species, mitochondrial damage, and cell death. Ferroptosis has recently been recognized as a key regulatory mechanism during tumor development, including in acute leukemia. This review considers the inhibitory effects of drugs on the occurrence and development of acute leukemia, by regulating key proteins or factors involved in the above three metabolic pathways of ferroptosis and by interfering with the production of lipid peroxides. We also point out the deficiencies in current research and describe the role of ferroptosis in acute leukemia. The application of these findings in clinical trials will provide new ideas for future research and the treatment of leukemia.