Novel androgen receptor inhibitors in prostate cancer: What do we know so far?

Crit Rev Oncol Hematol. 2025 Nov:215:104857. doi: 10.1016/j.critrevonc.2025.104857. Epub 2025 Jul 17.

Abstract

Prostate cancer (PC) is the second most common cancer among males, following lung cancer, more frequently occurring at an advanced age. Even nowadays, early diagnosis represents a challenge and validated screening methods are still missing. To date, multiple therapeutic strategies are available and a tailored approach is possible. The backbone of PC therapy is represented by the inhibition of the androgen signaling pathway, which mediates tumor cells growth. In this current therapeutic scenario, androgen-receptors signaling inhibitors (ARSIs) play a role in improving cancer treatment. This paper provides an overview of the currently available treatment options, focusing on the new drugs (ARSIs), their actual implications and future developments. METHODS: We conducted a research from Pubmed and Embase database regarding the terms 'prostate cancer', 'ARSI', 'androgen receptor inhibitors', ''enzalutamide", "apalutamide", and "Darolutamide". Original full-text articles published in English were reviewed. Based on this research 185 potentially relevant articles were found, limiting our research to the period 2019-2025 of publication. 75 articles were excluded on the basis of abstract, title or the content.

Keywords: Androgen receptor inhibitors; Prostate cancer; Treatment.

Publication types

  • Review

MeSH terms

  • Androgen Receptor Antagonists* / pharmacology
  • Androgen Receptor Antagonists* / therapeutic use
  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Benzamides / therapeutic use
  • Humans
  • Male
  • Nitriles / therapeutic use
  • Prostatic Neoplasms* / drug therapy
  • Prostatic Neoplasms* / metabolism
  • Receptors, Androgen* / metabolism
  • Signal Transduction / drug effects

Substances

  • Androgen Receptor Antagonists
  • Receptors, Androgen
  • Antineoplastic Agents
  • Benzamides
  • Nitriles