As a new manner of cell death, cuproptosis depends on the accumulation of copper ions in cells. Copper ion is an essential trace element in normal physiological state of organisms. The excess of free copper in cells not only has toxic effect on normal cells, but also plays its specific killing function on tumor cells. Copper transporter 1 (CTR1) is a key transporter of transmembrane uptake of copper ions by cells. As a regulator of cuproptosis, its mutation and expression changes in tumors have an impact on the distribution of copper ions inside and outside the cells. It may participate in multiple biological processes such as proliferation, invasion and migration of tumor cells by regulating the pathway of cuproptosis. This article reviews the cuproptosis pathway mediated by CTR1 and the potential value of CTR1 in tumor treatment, elaborates the importance of copper ion homeostasis regulation for normal life activities and the mechanism of CTR1 in regulating cuproptosis, and discusses the potential value of CTR1 as a new target for tumor therapy, so as to provide a theoretical basis for the treatment of tumor patients.