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August 29, 2026International Journal of Molecular SciencesOpen Access

Repurposing Disulfiram for Cancer Therapy: Mechanistic Insights and Translational Challenges

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Authors

ABAnna Bilska‐WilkoszMGMagdalena GórnyMIMałgorzata Iciek

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Overview

Review uncovers anticancer mechanisms and translational obstacles of disulfiram across preclinical models, highlighting the necessity of nanocarriers to improve delivery and bioavailability.

Key Points

  • To outline the molecular mechanisms behind disulfiram's anticancer efficacy and examine the pharmacologic challenges impeding its clinical translation.
  • Reviewed preclinical evidence regarding the bioactivation of disulfiram into diethyldithiocarbamate and its copper complex, Cu(DDC)2.
  • Assessed pharmacological and physiological barriers to clinical efficacy, including bioavailability, metabolism, copper availability, and drug delivery systems.
  • Disulfiram coupled with copper induces cytotoxicity by driving oxidative stress, blocking the ubiquitin-proteasome system, inhibiting hydrogen sulfide synthesis, and altering thiol metabolism to trigger apoptosis.
  • Clinical utility is substantially restricted by rapid systemic metabolism, poor oral bioavailability, scarce physiological free copper, and an absence of predictive response biomarkers.

Cite This Study

Bilska‐Wilkosz et al. (2026) studied this question.

synapsesocial.com/papers/6a92997e8e5d7d1fc0c117fdhttps://doi.org/10.3390/ijms27177667
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