Androgen receptor splice variant 7 expression levels distinguish AR-mutated from nonmutated metastatic castration-resistant prostate cancers

Read full text
Authors: Alec Paschalis, Ines Figueiredo, Denisa Bogdan, Arian Lundberg, Rita Santos, Bora Gürel, Tarek Taha, Ossian Longoria, Ana Ferreira, Claudia Bertan, Nicholas Brittain, Ryan Nelson
+12 more Laura Walker, Antje Neeb, Jonathan C. Welti, Wei Yuan, Costas Mitsopoulos, Stephen R. Plymate, Michael C. Haffner, Adam G. Sowalsky, Suzanne Carreira, Adam Sharp, Luke Gaughan, Johann de Bono
Cited by: 1
References: 45

Abstract

New androgen receptor (AR) pathway inhibitors (ARPIs) in clinical development, including AR degraders and CYP11A inhibitors, largely target ligand-dependent AR activation and have reported antitumor activity in metastatic castration-resistant prostate cancer (mCRPC) resistant to established ARPIs, predominately against tumors with AR mutations. We hypothesized that AR-mutated mCRPC exhibits lower AR splice variant 7 (AR-V7) expression and remains full-length-AR (FL-AR) driven, explaining, in part, the antitumor activity of these AR ligand-binding domain (LBD) targeting drugs. The data herein demonstrate that mCRPC tissue biopsies with detectable AR mutations express significantly lower levels of AR-V7 protein and associate with better overall survival and enhanced sensitivity to ARPIs. This is independent of differences in the total number of global splicing events but may be related to differences in splicing factor expression between AR-mutated and nonmutated mCRPC. In conclusion, AR-mutated mCRPC frequently exhibits low AR-V7 expression, arguably explaining the enhanced sensitivity to ARPIs observed in these cancers. Consequently, AR mutation status may serve as a biomarker to predict response to AR-directed therapies.

Fields of Study & Subjects

Prostate Cancer Treatment and Research Estrogen and related hormone effects Prostate Cancer Diagnosis and Treatment

Publication details

Journal / source
Journal of Clinical Investigation
Publisher
American Society for Clinical Investigation
Volume
136
Issue
7
Publication date
31 March 2026
Language
EN