Disulfiram
CAS number:97-77-8
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Molecular Formula:
C10H20N2S4
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Molecular Weight:
296.5g/mol
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Brief Introduction:
Disulfiram (DSF), originally developed as an anti-alcoholism drug, has drawn attention for its potential in treating various diseases beyond its initial use. According to recent literature, DSF exerts neuroprotective effects by modulating inflammation and redox balance in the brain. In a 2025 study published in Molecules, DSF was evaluated in a rat model of lipopolysaccharide (LPS)-induced neuroinflammation. While it did not improve memory impairment caused by LPS, it significantly increased the level of non-protein thiols (mainly glutathione), suggesting an antioxidative effect that may help mitigate oxidative stress during inflammation. Separately, in cancer research, DSF has been shown to target cancer stem cells (CSCs), particularly in non-small cell lung cancer (NSCLC). It inhibits CSC traits and enhances the cytotoxicity of chemotherapeutic agents when used in combination with copper. However, its clinical application has been limited by a short half-life in the bloodstream. To overcome this, researchers developed a PLGA-nano-encapsulated form of DSF, which showed improved stability and efficacy in both in vitro and in vivo models.
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Properities:
Chemical name Tetraethylthiuram disulfide [2] Common name Disulfiram (brand: Antabuse) [1], [2], [3] Chemical structure Contains disulfide bond; formula involves S–S and N(C2H5)2 functional groups [2] Administration route Oral [2], [3] Absorption 80–90% absorbed from the gastrointestinal tract [2] Distribution Highly lipophilic; distributes widely into adipose tissue; crosses blood–brain barrier [2] Metabolites DDTC (diethyldithiocarbamate), DDTC-Me, DETC-Me, CS2 [2] Elimination half-life (parent) ~7 hours [2] Elimination half-life (metabolites) DDTC ~15 h, DDTC-Me ~22 h, CS2 ~9–13 h [2] Dosage range (typical) 250–500 mg/day [2], [3] Maximum dosage 500 mg/day (up to 3500 mg/week in some therapeutic regimens) [2], [3] Mechanism of action (alcohol use disorder) Inhibits ALDH → acetaldehyde accumulation → aversive reaction [2], [3] Mechanism of action (cancer/infection) Chelates metals (Cu, Zn) → ROS generation → apoptosis in cancer cells [1], [2] Mechanism of action (antibacterial) Modifies bacterial enzymes via thiol–disulfide exchange [2] IC50 in leukemia cells Ranges from 45 to 81 nM [1] Side effects Flushing, nausea, vomiting, headache, hypotension, tachycardia, cardiac complications (in ADR) [3] Safety concerns Hepatotoxicity, inter-subject variability, possible fatal alcohol–disulfiram reaction (rare) [2], [3] Protein targets ALDH, dopamine β-hydroxylase, superoxide dismutase, carboxylesterase, cholinesterase [2] Initial synthesis year 1881 [2] FDA approval year for AUD 1951 [2] Known plasma levels (250 mg dose) Disulfiram ~0.3–0.4 μg/mL; DDTC ~0.7–1.4 μg/mL; DDTC-Me ~0.3–1.2 μg/mL [2] Drug interactions Copper (Cu) enhances disulfiram cytotoxicity in leukemia cells [1] Common diseases treated Alcohol Use Disorder, Cocaine Addiction, Leukemia, Infections (e.g. Borrelia burgdorferi) [1], [2], [3] -
References:
[1]: FDA-approved disulfiram as a novel treatment for aggressive leukemia (Journal of Molecular Medicine, 2024)
[2]: Disulfiram: Mechanisms, Applications, and Challenges (Antibiotics, 2023)
[3]: Effectiveness of Disulfiram as Adjunct to Addiction‐Focused Treatment for Persons With Severe Alcohol Use Disorder (Addiction Biology, 2025)
Organosulfur compounds
DSF contains sulfur atoms, specifically in disulfide and thiuram moieties, making it part of the organosulfur family.
Thiuram compounds
Disulfiram is a derivative of thiuram disulfide, characterized by the presence of the (R₂NC(S)S–S) unit.
Carbamodithioates
Disulfiram (DSF) contains two diethyldithiocarbamate groups, a subclass of carbamodithioates.
Prodrugs
DSF is considered a prodrug because it is metabolized in the body to form active compounds, such as diethyldithiocarbamate.
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