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This information is for educational purposes only. Off-label drug use carries risks. Always consult a qualified physician before using any drug outside its approved indication.

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Disulfiram

Disulfiram

Brand names: Antabuse

Aldehyde Dehydrogenase InhibitorMetabolicmoderate evidenceActive Clinical Trials

ORIGINALLY APPROVED FOR

Alcohol Use Disorder (Aversion Therapy)

Disulfiram's anti-cancer activity was discovered when researchers noticed that alcoholics taking disulfiram had lower cancer rates. Its active metabolite diethyldithiocarbamate (DDC) chelates copper to form DDC-copper complexes that are potently cytotoxic to cancer cells. A landmark 2016 study found that disulfiram-copper destroys the NPL4 protein — which cancer cells need for protein quality control. High-copper tumour environments amplify this effect. Phase II trials are ongoing for GBM and breast cancer.

Molecular Pathways Targeted

Copper-NPL4ProteasomeNF-κBAldehyde Dehydrogenase (ALDH)ROS

Mechanism of Action in Cancer

DDC metabolite chelates Cu2+ → DDC-copper complex → inhibits NPL4 adaptor protein → blocks p97-NPL4 pathway → cancer cells unable to clear misfolded proteins → proteotoxic stress and cell death. Also inhibits proteasome 26S subunit, NF-κB, and ALDH (kills cancer stem cells that rely on ALDH for chemo-resistance).

Cancers Studied

GlioblastomaBreastProstateLungColorectalOvarianLiver

Typical Off-Label Dosing

200–500 mg daily (standard alcohol aversion dose). Many cancer protocols combine with copper supplementation (2–4 mg/day) to enhance DDC-copper complex formation. Often taken on an empty stomach. MUST avoid all alcohol absolutely.

* Dosing information from research literature only. Not a prescription. Requires physician supervision.

Cautions & Drug Interactions

  • ABSOLUTE contraindication with any alcohol — even in food, mouthwash, sauces — severe reaction
  • Hepatotoxicity — liver monitoring essential, avoid in liver disease
  • Drug interactions: warfarin (increased bleeding), phenytoin, benzodiazepines
  • CNS effects: peripheral neuropathy, psychosis (rare) with prolonged use
  • Cardiovascular: caution in heart disease — disulfiram-alcohol reaction can be fatal
  • Check all medications and food labels for hidden alcohol before starting
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