Abstract: Copper ions are an essential trace element for normal development of the organism and involved in various physiological processes. Abnormal copper metabolism leads to cytotoxic stress and cell death. Cuproptosis is a newly proposed type of regulatory cell death that differs from other cell death pathways, such as apoptosis, ferroptosis, and autophagy. It involves the accumulation of copper ions and mitochondrial metabolism. In recent years, multiple studies have revealed the role of cuproptosis in the occurrence, progression, and treatment of tumors. The toxic effect of copper ionophores on tumor cells has attracted much attention. This article reviews the mechanism of cuproptosis and current progress in the research of different tumors, as well as advancements in the use of copper ionophores in oncotherapy.