The Repurposing of Non-Peptide Neurokinin-1 Receptor Antagonists as Antitumor Drugs: An Urgent Challenge for

Rafael Coveñas1,2, Francisco D Rodríguez2,3, Prema Robinson4

  • 1Laboratory of Neuroanatomy of the Peptidergic Systems, Institute of Neurosciences of Castilla y León (INCYL), University of Salamanca, 37007 Salamanca, Spain.

Insights

The substance P (SP)/neurokinin-1 receptor (NK-1R) system drives cancer growth. Aprepitant, an NK-1R antagonist, shows broad-spectrum anticancer effects, offering a potential new therapeutic strategy for various cancer types.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • The substance P (SP)/neurokinin-1 receptor (NK-1R) system plays a crucial role in cancer progression.
  • NK-1R activation by SP promotes tumor proliferation, migration, angiogenesis, the Warburg effect, and inhibits apoptosis.
  • Tumor cells exhibit NK-1R overexpression, impacting their viability.

Purpose of the Study:

  • To review the potential of NK-1R antagonists, specifically Aprepitant, as a broad-spectrum anticancer agent.
  • To update current information on Aprepitant's efficacy in various cancer types.
  • To highlight the urgent need for repurposing Aprepitant as an anticancer drug.

Main Methods:

  • Review of existing literature on the SP/NK-1R system in cancer.
  • Analysis of studies investigating NK-1R antagonists, particularly Aprepitant.
  • Evaluation of Aprepitant's effects alone and in combination therapies.

Main Results:

  • NK-1R antagonists effectively block SP-mediated pro-cancer effects.
  • Aprepitant demonstrates broad-spectrum anticancer activity across multiple tumor types.
  • Combination therapy with Aprepitant may improve cure rates and quality of life.

Conclusions:

  • Repurposing the antiemetic Aprepitant as an anticancer drug is a promising therapeutic strategy.
  • Targeting the SP/NK-1R pathway offers a novel approach to cancer treatment.
  • Further research is warranted to fully explore Aprepitant's antitumor potential.

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