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Sigma-1 Receptor Ligands for CNS Cancer Treatment

Anchalee Prasansuklab1,2, Stephen T Safrany3, Sirikalaya Brimson4

  • 1College of Public Health Sciences, Chulalongkorn University, Bangkok, 10330, Thailand.

CNS Drugs
|September 18, 2025
PubMed

Insights

Repurposing existing drugs targeting sigma receptors offers a novel strategy for cancer treatment, especially for central nervous system (CNS) cancers. These sigma receptor ligands may overcome drug resistance and blood-brain barrier challenges.

Area of Science:

  • Neuroscience
  • Oncology
  • Pharmacology

Background:

  • Conventional cancer therapies face challenges like nonspecificity, multidrug resistance, and poor blood-brain barrier (BBB) penetration for central nervous system (CNS) cancers.
  • Sigma receptors, particularly sigma-1, are implicated in neurodegeneration and pain, and are overexpressed in many cancers, yet their anticancer potential is underexplored.
  • Sigma receptors regulate crucial cancer processes including cell survival, proliferation, differentiation, and autophagy.

Purpose of the Study:

  • To explore the potential of repurposing existing neuroactive drugs as anticancer agents, focusing on their sigma receptor activity.
  • To investigate the role of sigma-1 receptor ligands in modulating autophagy for cancer treatment, particularly CNS cancers.
  • To review the autophagic, anticancer, and sigma-receptor activities of specific neuroactive drugs like haloperidol, rimcazole, fluoxetine, and donepezil.

Main Methods:

  • Literature review of studies on sigma receptor ligands and their effects on cancer cells.
  • Analysis of existing neuroactive drugs (haloperidol, rimcazole, fluoxetine, donepezil) for their sigma receptor binding and anticancer properties.
  • Examination of the link between sigma-1 receptor modulation, autophagy, and cancer progression.

Main Results:

  • Sigma receptors are promising therapeutic targets due to their role in cell survival, proliferation, and differentiation.
  • Sigma-1 receptor activity is linked to the regulation of autophagy, a key process in cancer development.
  • Several neuroactive drugs acting as sigma receptor ligands show potential anticancer benefits, including for CNS cancers.

Conclusions:

  • Drug repurposing of sigma receptor ligands presents a cost-effective and time-efficient approach to developing novel anticancer therapies.
  • Neuroactive drugs targeting sigma receptors may overcome challenges associated with conventional cancer treatments, including drug resistance and BBB penetration.
  • Further research into sigma receptor-modulating drugs could lead to effective treatments for various cancers, especially those affecting the CNS.

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