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Updated: Sep 26, 2025

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
Published on: February 6, 2015
Repurposing Disulfiram as a Chemo-Therapeutic Sensitizer: Molecular Targets and Mechanisms
Feilong Sun1,2, Hongzhi Wang1,3, Jinfu Nie1,3
1Anhui Province Key Laboratory of Medical Physics and Technology, Institute of Health and Medical Technology, Hefei Institutes of Physical Science, Chinese Academy of Sciences, Hefei, Anhui, China.
Abstract:
Currently, chemotherapy is still the main strategy for cancer treatment. However, chemotherapy resistance remains a challenge. Disulfiram (DSF) is an FDA-approved medicine for the treatment of alcoholism; however, it was later revealed to have anticancer properties. Importantly, numerous studies have shown that DSF can be employed as a chemotherapeutic sensitizer to enhance the anticancer efficacy of chemo-drugs in a variety of cancers. Furthermore, the combinations of DSF and chemo-drugs have been tested in clinical trials. In the review, we summarized the possible molecular targets and mechanisms of DSF to reverse chemo-resistance. We also further discussed the opportunities and challenges of DSF as a chemo-therapeutic sensitizer. In conclusion, DSF could be a potentially repurposed drug that sensitizes cancer cells to chemotherapy in the clinic.
Insights
Disulfiram (DSF), an alcoholism drug, shows promise in reversing chemotherapy resistance in cancer. Clinical trials explore DSF combinations to enhance chemotherapy effectiveness, offering a potential repurposed treatment strategy.
Area of Science:
- Oncology
- Pharmacology
Background:
- Chemotherapy remains a primary cancer treatment strategy.
- Chemotherapy resistance is a significant clinical challenge, limiting treatment efficacy.
- Disulfiram (DSF), an FDA-approved alcoholism medication, exhibits anticancer properties.
Purpose of the Study:
- To review the molecular targets and mechanisms by which Disulfiram (DSF) reverses chemotherapy resistance.
- To discuss the potential and challenges of using DSF as a chemotherapeutic sensitizer.
Main Methods:
- Literature review of studies on Disulfiram (DSF) and its role in cancer therapy.
- Analysis of preclinical and clinical data regarding DSF in combination with chemotherapy drugs.
Main Results:
- Disulfiram (DSF) has demonstrated efficacy in sensitizing various cancer types to chemotherapy.
- Multiple studies and clinical trials support the use of DSF in combination therapies.
- Identified molecular targets and mechanisms involved in DSF-mediated chemo-resistance reversal.
Conclusions:
- Disulfiram (DSF) shows significant potential as a repurposed drug to overcome chemotherapy resistance.
- DSF can enhance the efficacy of conventional chemotherapy, offering new therapeutic opportunities.
- Further clinical investigation is warranted to fully establish DSF's role in cancer treatment.
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