Targeting adenocarcinoma and enzalutamide‑resistant prostate cancer using the novel anti‑androgen inhibitor ADA‑308

Oncol Rep. 2024 Oct;52(4):132. doi: 10.3892/or.2024.8791. Epub 2024 Aug 12.

Abstract

Prostate cancer (PCa) is the leading cause of cancer‑related death among men worldwide. PCa often develops resistance to standard androgen deprivation therapy and androgen receptor (AR) pathway inhibitors, such as enzalutamide (ENZ). Therefore, there is an urgent need to develop novel therapeutic strategies for this disease. The efficacy of ADA‑308 was evaluated through in vitro assessments of AR activity and cell proliferation, alongside in vivo studies. ADA‑308 has emerged as a promising candidate, demonstrating potent inhibition of AR‑sensitive adenocarcinoma as well as ENZ‑resistant PCa cell lines. The results of the study revealed that ADA‑308 effectively blocked AR activity, including its nuclear localization, and inhibited cell proliferation in vitro. Furthermore, ADA‑308 demonstrated notable efficacy in vivo, with a robust antitumor response in ENZ‑resistant models. These findings establish the role of ADA‑308 as a potent AR inhibitor that overcomes resistance to AR‑targeted therapies and highlights its potential as a novel therapeutic approach in advanced PCa management.

Keywords: ARPIs; enzalutamide resistance; prostate cancer adenocarcinoma; treatment- resistance.

MeSH terms

  • Adenocarcinoma* / drug therapy
  • Adenocarcinoma* / pathology
  • Androgen Antagonists* / pharmacology
  • Androgen Antagonists* / therapeutic use
  • Androgen Receptor Antagonists / pharmacology
  • Androgen Receptor Antagonists / therapeutic use
  • Animals
  • Benzamides* / pharmacology
  • Benzamides* / therapeutic use
  • Cell Line, Tumor
  • Cell Proliferation* / drug effects
  • Drug Resistance, Neoplasm* / drug effects
  • Humans
  • Male
  • Mice
  • Nitriles* / pharmacology
  • Nitriles* / therapeutic use
  • Phenylthiohydantoin* / analogs & derivatives
  • Phenylthiohydantoin* / pharmacology
  • Phenylthiohydantoin* / therapeutic use
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / pathology
  • Receptors, Androgen* / metabolism
  • Xenograft Model Antitumor Assays

Substances

  • Phenylthiohydantoin
  • Nitriles
  • enzalutamide
  • Benzamides
  • Receptors, Androgen
  • Androgen Antagonists
  • AR protein, human
  • Androgen Receptor Antagonists

Grants and funding

This research was supported by funding from Aranda Pharma Ltd as well as the Prostate Cancer Foundation Young Investigator Award (to SN).