disulfiram
Trade name: antabuse
Approved
Aug 28, 1951
Disulfiram is a carbamate derivative used as an alcohol deterrent. It is a relatively nontoxic substance when administered alone, but markedly alters the intermediary metabolism of alcohol. Disulfiram blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake causing an accumulation of acetaldehyde in the blood producing highly unpleasant symptoms. Disulfiram blocks the oxidation of alcohol through its irreversible inactivation of aldehyde dehydrogenase, which acts in the second step of ethanol utilization. In addition, disulfiram competitively binds and inhibits the peripheral benzodiazepine receptor, which may indicate some value in the treatment of the symptoms of alcohol withdrawal, however this activity has not been extensively studied. Used for the treatment and management of chronic alcoholism. — NCATS
Clinical trial activity
55 trials · 69 clinical orgs · 12 marketing orgs
Earliest trial started Sep 1, 1994 (NCT00000278)
Timeline
1950s
1980s
- Mar 31, 1981
Watson Pharmaceuticals — Marketing Organization
- Mar 31, 1981
Teva — Marketing Organization
- Dec 8, 1983
Odyssey Pharmaceuticals — Marketing Organization
- Aug 14, 1984
Par Pharmaceuticals — Marketing Organization
- Aug 14, 1984
Strides Pharma Science — Marketing Organization
1990s
- Jan 1, 1994
Earliest Phase 2 Sponsor(trial)
2000s
- Jan 1, 2002
Earliest Phase 1 Sponsor(trial)
2010s
- Mar 28, 2011
Sigmapharm Laboratories — Marketing Organization
- Dec 31, 2012
Chartwell Pharmaceuticals — Marketing Organization
- Aug 8, 2013
Alvogen — Marketing Organization
- Feb 5, 2014
West-Ward Pharmaceutical — Marketing Organization
- Feb 5, 2014
Hikma — Marketing Organization
- Mar 4, 2015
Mylan — Marketing Organization
- Mar 4, 2015
Dash Pharms — Marketing Organization
Indications
Approved for
Studied for
- Alcohol-Induced Disorders · Phase 1/Phase 2
- Alcohol-Related Disorders · Phase 2
- Analgesics, Opioid · Phase 2
- Anxiety Disorders · Phase 4
- Breast Neoplasms · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 2/Phase 3
- Cocaine-Related Disorders · Phase 4
- COVID-19 · Phase 2
- Fatigue · Phase 1/Phase 2
- Glioblastoma · Phase 2/Phase 3
- Glioma · Phase 2/Phase 3
- HIV · Phase 1/Phase 2
- HIV Infections · Phase 1/Phase 2
- Hyperhidrosis · Phase 2
- Machiavellianism · Phase 1
- Macular Degeneration · Phase 1/Phase 2
- Melanoma · Phase 2
- Methamphetamine · Phase 1/Phase 2
- Multiple Myeloma · Phase 1
- Neoplasms · Phase 1
- Neoplasms, Germ Cell and Embryonal · Phase 2
- Obesity · Early Phase 1
- Opioid-Related Disorders · Phase 2
- Pancreatic Neoplasms · Phase 2
- Prostatic Neoplasms · Phase 1
- Quality of Life · Phase 1/Phase 2
- Retina · Phase 1/Phase 2
- Retinal Dystrophies · Phase 1
- Retinitis Pigmentosa · Phase 1
- Sarcoma · Phase 1
- Stargardt Disease · Phase 1
- Substance-Related Disorders · Phase 1
Mechanism of action
- Aldehyde dehydrogenaseINHIBITOR
ALDH2 inhibitor
Approval history
- approvedPriority reviewAug 28, 1951
Chemistry & pharmacology
SMILES
CCN(CC)C(=S)SSC(=S)N(CC)CC- Mol. weight
- 296.539 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaDisulfiram ↗
- NCATSTR3MLJ1UAI ↗
- ChEMBLCHEMBL964 ↗
Also known as
- 1,1'-dithiobis(n,n-diethylthioformamide)
- 1,1'-dithiobis(n,n-diethylthioformamide)
- ant-1403
- antabuse
- antabuse
- antabuse
- antabuse
- antabuse (tn)
- antabuse (tn)
- bis(diethylthiocarbamoyl) disulfide
- bis(diethylthiocarbamoyl) disulfide
- disulfiram
- disulfiram
- disulfiram
- disulfiram
- disulfiram
- disulfiram
- disulfiram
- disulfiram
- disulfiram
- disulfiram
- disulfiram
- esperal
- esperal
- n,n,n',n'-tetraethylthiuram disulfide
- n,n,n',n'-tetraethylthiuram disulfide
- nsc-25953
- nsc-25953
- ora102
- tetraethylthioperoxydicarbonic diamide
- tetraethylthioperoxydicarbonic diamide
- tetraethylthiram disulfide
- tetraethylthiuram disulfide
- tetraethylthiuram disulfide
- tetraethylthiuram disulphide
- tetraethylthiuram disulphide
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06793488 | Early Phase 1 (Phase 1) | Mar 1, 2025 | Columbia University, National Institute on Alcohol Abuse and Alcoholism (NIAAA) |
| NCT06319872 | Phase 1 | Nov 1, 2024 | University of Rochester |
| NCT05667415 | N/A | Jun 1, 2023 | First People's Hospital of Hangzhou, Zhejiang University |
| NCT05626920 | Phase 1/Phase 2 (Phase 2) | Jan 31, 2023 | University of Washington |
| NCT05210374 | Phase 1 | Dec 31, 2022 | Case Western Reserve University, University of Rochester |
| NCT05162001 | Early Phase 1 (Phase 1) | Nov 21, 2021 | Laboratorios Doctor Macías, Universidad de Guanajuato |
| NCT04521335 | Phase 1 | Dec 31, 2020 | Cantex Pharmaceuticals, University of Utah |
| NCT04485130 | Phase 2 | Dec 1, 2020 | University of California, San Francisco |
| NCT04594343 | Phase 2 | Nov 20, 2020 | Augusto Mota, Spring Research Foundation |
| NCT04502589 | Phase 1/Phase 2 (Phase 2) | Oct 15, 2020 | National Institute on Alcohol Abuse and Alcoholism (NIAAA), Virginia Commonwealth University |
| NCT04265274 | Phase 2 | Jan 1, 2020 | National Cancer Institute, Slovakia |
| NCT03714555 | Phase 2 | Jun 30, 2019 | Cantex Pharmaceuticals, HonorHealth Research Institute |
| NCT03950830 | Phase 2 | May 14, 2019 | National Cancer Institute, Slovakia |
| NCT03891667 | Phase 1/Phase 2 (Phase 2) | Apr 1, 2019 | Columbia University, FDC Foundation, Research Foundation for Mental Hygiene, Inc. |
| NCT03363659 | Phase 2 | Mar 28, 2018 | University of Wisconsin |
| NCT03323346 | Phase 2 | Sep 29, 2017 | Palacky University, The Institute of Molecular and Translational Medicine, Czech Republic |
| NCT03198559 | Phase 1/Phase 2 (Phase 2) | Aug 8, 2017 | Merck, Monash University, The Peter Doherty Institute, University of Melbourne |
| NCT03151772 | Early Phase 1 (Phase 1) | Aug 1, 2017 | University of Gothenburg |
| NCT03034135 | Phase 2 | Mar 9, 2017 | Cantex Pharmaceuticals, Washington University in St. Louis |
| NCT02963051 | Phase 1 | Feb 1, 2017 | Duke University, Give 1 For Dad Campaign, Peter Michael Foundation, V Foundation |
Organizations
Research & Development (69)
Marketing (17)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Alvogen | For profit | MKTG | Aug 8, 2013 |
| Alvogen | For profit | SYN | Aug 8, 2013 |
| Chartwell Pharmaceuticals | For profit | MKTG | Dec 31, 2012 |
| Dash Pharms | For profit | MKTG | Mar 4, 2015 |
| Hikma | For profit | MKTG | Feb 5, 2014 |
| Hikma | For profit | SYN | Feb 5, 2014 |
| Mylan | For profit | MKTG | Mar 4, 2015 |
| Mylan | For profit | SYN | Mar 4, 2015 |
| Odyssey Pharmaceuticals | For profit | MKTG | Dec 8, 1983 |
| Par Pharmaceuticals | For profit | MKTG | Aug 14, 1984 |
| Sigmapharm Laboratories | For profit | MKTG | Mar 28, 2011 |
| Strides Pharma Science | For profit | MKTG | Aug 14, 1984 |
| Teva | For profit | NDA2 | Aug 28, 1951 |
| Teva | For profit | MKTG | Mar 31, 1981 |
| Teva | For profit | NDA | Aug 28, 1951 |
| Watson Pharmaceuticals | For profit | MKTG | Mar 31, 1981 |
| West-Ward Pharmaceutical | For profit | MKTG | Feb 5, 2014 |