Drug intelligence / Profile preview

disulfiram + copper

Development stage
Phase 2
Lead developer
Cantex Pharmaceuticals
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Disulfiram + copper is a combination therapy under investigation primarily for cancer treatment. Disulfiram, a thiocarbamate derivative long approved for alcoholism, acts as a metal chelator and forms complexes with copper ions. When combined with copper (often as copper gluconate), the resulting complex exhibits potent anticancer activity in preclinical models and early clinical trials. The mechanism of action involves inhibition of aldehyde dehydrogenase, proteasome inhibition, stimulation of reactive oxygen species (ROS) production, and induction of cell death pathways selectively in cancer cells—especially those with elevated intracellular copper levels. The active metabolite diethyldithiocarbamate (DDC) forms a cytotoxic complex with Cu(II), which can penetrate tumor cells and induce apoptosis via oxidative stress and other mechanisms. This combination is being repurposed for oncology indications such as glioblastoma, pancreatic cancer, prostate cancer, among others[1][2][3][5][6].

Other names
disulfiram/copper gluconatecopper gluconate/disulfiram
02

Targets

ALDH2 (Mitochondrial Aldehyde Dehydrogenase)NPL4 (Nuclear protein localization protein 4 cofactor–valosin-containing protein segregase complex)ALDH1A1 (Aldehyde dehydrogenase 1 family member A1)Ferroptosis (Ferroptosis regulators)26S proteasome

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