The combination of disulfiram and copper for cancer treatment

• Published in: Drug discovery today 2020-06, Vol.25 (6), p.1099-1108
• Main Authors: Li, Hong, Wang, Jingyu, Wu, Chunfu, Wang, Lihui, Chen, Zhe-Sheng, Cui, Wei
• Format: Article
• Language: English
• ISSN: 1359-6446; 1878-5832
• DOI: 10.1016/j.drudis.2020.04.003

•Disulfiram, an anti-alcoholism drug, was found owing anti-tumor activity.•The combination of Disulfiram and copper greatly enhances its anti-tumor efficacy.•Disulfiram in combination with copper has been shown to reverse drug resistance in cancer through targeting ALDH, NF-κB pathway, MAPK pathway and so on. Disulfiram (DSF) is a thiuram derivative that was developed to treat alcoholism but was also found to have antitumor activity. Copper (Cu), as a trace metal, has important roles in the body. Numerous studies have shown that the combination of DSF and copper (DSF/Cu) greatly enhances its antitumor efficacy. Given that the efficacy of DSF is well established and its safety profile is understood, repurposing DSF as a new anticancer drug is a promising strategy. Here, we summarize the pharmacological effects of DSF and the role of Cu in cancer, and focus on the antitumor effect of DSF/Cu, especially the mechanisms involved in enhancing drug sensibility by targeting specific molecules. We also provide rational strategies for using DSF as a cancer therapy.