Current status of androgen receptor-splice variant 7 inhibitor niclosamide in castrate-resistant prostate-cancer

Invest New Drugs. 2018 Dec;36(6):1133-1137. doi: 10.1007/s10637-018-0653-2. Epub 2018 Aug 7.


Castrate-Resistant Prostate-Cancer (CRPC) is one of the most common malignancies occurring in men. Unfortunately, even if several recently approved agents clinically improved the outcome of CRPC patients, none of these is curative especially for a splice version of the Androgen Receptor (AR) AR-V7, which is a variant of the receptor constitutively activated and does not require the presence of androgens for the activation AR down-stream pathways. Since high AR-V7 expression is one of the most common features of CRPC, targeting this receptor variant is considered as one of the most promising strategies for treating this disease. Therefore anti-AR-V7 molecules could lead to a potential shift in paradigm in the treatment of CRPC. Niclosamide, an already FDA-approved anti-helminthic drug, was identified as a potent AR-V7 inhibitor in prostate cancer cells. Due to the recent positive preclinical results, niclosamide may be an interesting and novel type of targeted treatments for CRPC. This mini-review outlines the most recent pre- and clinical- data on the current status of niclosamide in the treatment of ARV7-positive CRPC patients.

Keywords: Androgen receptor; Androgen receptor splice variant 7; Castrate-resistant prostate-Cancer; Niclosamide.

Publication types

  • Review

MeSH terms

  • Alternative Splicing / genetics*
  • Clinical Trials as Topic
  • Humans
  • Male
  • Models, Biological
  • Niclosamide / therapeutic use
  • Prostatic Neoplasms, Castration-Resistant / drug therapy
  • Prostatic Neoplasms, Castration-Resistant / genetics*
  • Prostatic Neoplasms, Castration-Resistant / pathology
  • Receptors, Androgen / genetics*


  • Receptors, Androgen
  • Niclosamide