Niclosamide Applications in Cancer Therapeutics
Summary
Niclosamide, originally employed as an anthelmintic, has garnered considerable interest as a repurposed anticancer agent owing to its multifaceted mechanisms of action. It inhibits crucial oncogenic pathways—including Wnt/β-catenin, mTORC1 and STAT3 signalling—thereby inducing growth arrest and apoptosis across diverse tumour types. Concurrently, niclosamide acts as a mitochondrial uncoupler, disrupting the metabolic adaptations of cancer cells and counteracting the Warburg effect. Preclinical models have demonstrated that this dual activity not only curtails primary tumour growth but also impairs metastatic spread and diminishes cancer stem cell populations. Advances in drug formulation, such as the development of salt forms, nanosuspensions and biodegradable carriers, have addressed its poor water solubility and enhanced systemic exposure. Early-phase clinical trials have begun to explore its safety profile, pharmacokinetics and efficacy in patients with refractory malignancies. Collectively, these findings underscore niclosamide’s potential as a low-cost, multi-targeted therapeutic to complement existing regimens, overcome drug resistance and tackle the global burden of cancer.
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Niclosamide Applications in Cancer Therapeutics publication trend
The graph below shows the total number of articles in niclosamide applications in cancer therapeutics across all publications each year (not limited to Nature Index journals).
Technical terms
mTORC1: Mammalian target of rapamycin complex 1, a protein complex that regulates cell growth and metabolism in response to nutrients and growth factors.
Wnt/β-catenin signalling: A pathway controlling gene expression and cell fate, often dysregulated in cancer to promote proliferation and invasion.
Mitochondrial uncoupling: The process by which protons re-enter the mitochondrial matrix independent of ATP synthase, dissipating the proton gradient as heat and altering cellular energetics.
Pharmacokinetics: The study of how a drug is absorbed, distributed, metabolised and excreted by the body.
Metastasis: The spread of cancer cells from the primary tumour site to distant organs, leading to secondary tumour formation.
References
- Pharmacological advances and therapeutic applications of niclosamide in cancer and other diseases. European Journal of Medicinal Chemistry (2025).
- Niclosamide and its analogs are potent inhibitors of Wnt/β-catenin, mTOR and STAT3 signaling in ovarian cancer. Oncotarget (2016).
- Phase II trial to investigate the safety and efficacy of orally applied niclosamide in patients with metachronous or sychronous metastases of a colorectal cancer progressing after therapy: the NIKOLO trial. BMC Cancer (2018).
- Effect of mitochondrial uncouplers niclosamide ethanolamine (NEN) and oxyclozanide on hepatic metastasis of colon cancer. Cell Death & Disease (2018).
- Niclosamide Suppresses Cancer Cell Growth By Inducing Wnt Co-Receptor LRP6 Degradation and Inhibiting the Wnt/β-Catenin Pathway. PLOS ONE (2011).
- Drug Screening Identifies Niclosamide as an Inhibitor of Breast Cancer Stem-Like Cells. PLOS ONE (2013).
- The Anthelmintic Drug Niclosamide Induces Apoptosis, Impairs Metastasis and Reduces Immunosuppressive Cells in Breast Cancer Model. PLOS ONE (2014).
- Niclosamide loaded biodegradable chitosan nanocargoes: an in vitro study for potential application in cancer therapy. Royal Society Open Science (2017).
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