Drug Repurposing in Cancer Treatment
Comprehensive Drug Repurposing Portfolio
Phenylbutyrate
Original Use: Urea cycle disorders
Mechanism: HDAC inhibitor and PDK1 inhibitor
Action: Depletes glutamine in cancer cells, induces cellular differentiation, and enhances chemotherapy effectiveness
Niclosamide
Original Use: Anti-parasitic
Mechanism: Inhibits Wnt/Ξ²-catenin pathway, STAT3, and suppresses RAS
Action: Reduces cancer cell proliferation and increases apoptosis.
Ivermectin
Original Use: Anti-parasitic
Mechanism: Inhibits Ξ²-catenin/EGFR/ERK/Akt/NF-ΞΊB pathways
Action: Inhibits tumor growth and reverses drug resistance.
Metformin
Original Use: Diabetes medication
Mechanism: Activates AMPK, inhibits mitochondrial respiration
Action: Limits glucose availability to cancer cells and enhances therapy efficacy.
Itraconazole
Original Use: Antifungal
Mechanism: Inhibits tumor angiogenesis and targets cancer stem cells
Action: Particularly effective in ovarian cancer, melanoma, and other solid tumors.
Mebendazole
Original Use: Antiparasitic
Mechanism: Targets multiple cancer-associated pathways
Action: Overcomes drug resistance, particularly effective in ovarian and thyroid cancers.
Fenbendazole
Original Use: Antiparasitic
Mechanism: Inhibits tumor growth and enhances immune response
Action: Enhances immune cell-mediated tumor killing.
Orlistat
Original Use: Weight loss medication
Mechanism: Inhibits fatty acid synthase (FASN)
Action: Reduces cancer cell proliferation and induces apoptosis in pancreatic and breast cancer.
Disulfiram
Original Use: Alcohol dependence treatment
Mechanism: Inhibits proteasome and ALDH, disrupts metal homeostasis
Action: Induces oxidative stress and modulates tumor immune microenvironment.
Fexofenadine
Original Use:Anti-histamine
Mechanism: Selective H1-antagonist
Action: Acts by selectively antagonizing H1 receptors on cell surfaces across various organ systems, thereby affecting inflammatory mediators.
Additional Repurposed Agents
Anti-inflammatory drug reducing cancer growth by targeting inflammation, stimulating T-cell proliferation, and inhibiting metastasis.
SERM for breast cancer with efficacy in glioma and melanoma. Synergizes with melatonin.
Antimalarial drug inhibiting autophagy in cancer cells, enhancing treatment efficacy.
mTOR inhibitor preventing cancer cell growth and proliferation.
Beta-blocker inhibiting angiogenesis and targeting triple-negative breast cancer.
Modulates immune system and gene expression, potentially slowing cancer progression.
NSAID inducing apoptosis via COX-2 inhibition, synergizes with curcumin and aspirin.
Carbonic anhydrase inhibitor limiting tumor growth by reducing pH and affecting metabolism.
PPI altering tumor microenvironment acidity and improving chemotherapy efficacy.
Diuretic selectively targeting breast cancer cells by inhibiting survival pathways.
Promotes mitochondrial function, reduces oxidative stress, and inhibits lactic acid production.
Antibiotic reversing EMT and inhibiting metastasis in melanoma and lung cancer.
Inhibits autophagy, enhances chemo/radiotherapy susceptibility, reverses drug resistance.
Common painkiller and anti-inflammatory with significant anti-cancer properties.
Research Resources
Comprehensive Spreadsheet Analysis
References
⚠️ Important Information: This content is for informational and educational purposes only. It is based on scientific research but is not medical advice. These repurposed drugs can interact with medications and may not be suitable for everyone. Always consult with a qualified healthcare professional before considering any treatment, particularly for serious conditions like cancer. Repurposed drugs should never replace conventional cancer treatment unless under the guidance of qualified oncologists.
Last updated: September 2025
