The Neurokinin-1 Receptor Antagonist Aprepitant: An Intelligent Bullet against Cancer?

Miguel Muñoz1, Rafael Coveñas2

  • 1Research Laboratory on Neuropeptides (IBIS), Virgen del Rocío University Hospital, 41013 Sevilla, Spain.

Cancers
|September 23, 2020
PubMed

Insights

Neurokinin-1 receptor (NK-1R) antagonists, like aprepitant, show significant antitumor effects against various cancers. Repurposing aprepitant as an anticancer agent could offer a safe and effective new treatment option.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Neurokinin-1 receptor (NK-1R) antagonists exhibit antitumor properties, including antiproliferative, anti-Warburg, apoptotic, anti-angiogenic, and antimetastatic effects across diverse cancer types.
  • Aprepitant, an NK-1R antagonist approved for antiemetic use, has demonstrated these antitumor actions in preclinical studies.
  • The substance P (SP)/NK-1R system's potential link to cancer and depression warrants further investigation.

Purpose of the Study:

  • To review the multifaceted antitumor actions of aprepitant.
  • To explore the potential of repurposing aprepitant as a novel anticancer therapeutic agent.

Main Methods:

  • Review of in vivo and in vitro studies on NK-1R antagonists and aprepitant's anticancer effects.
  • Analysis of clinical data, including a case of successful combination therapy with aprepitant and radiotherapy for lung carcinoma.

Main Results:

  • Aprepitant exhibits broad-spectrum antitumor activities, including antiproliferative and anti-angiogenic effects.
  • A case report demonstrated successful tumor mass reduction and absence of side-effects using aprepitant combined with radiotherapy.
  • Preclinical data support aprepitant's potential in preventing cancer recurrence and metastasis.

Conclusions:

  • Aprepitant demonstrates significant potential as an anticancer agent due to its diverse antitumor mechanisms.
  • Repurposing aprepitant for cancer treatment is supported by existing evidence, suggesting its use in clinical practice.
  • Further research into the SP/NK-1R pathway may elucidate links between cancer and depression, offering new therapeutic avenues.

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