Articles and Abstracts

Androgen receptor (AR) signaling is the most important driver of prostate cancer initiation, development, and progression, even into the castration-resistant state.  Androgen deprivation therapy (ADT) is the original “targeted therapy” in oncology.  The next generation androgen- and AR-targeted agents, such as abiraterone acetate, enzalutamide, apalutamide and darolutamide further prove the concept that AR signaling remains critical in even later disease states.  There are various mechanisms of resistance that continue to be inclusive of AR; this ranges from AR amplification, AR mutation, and potentially AR spliced variants.

Conference Coverage
Conference Highlights Written by Physician-Scientist
Presented by Russell Kent Pachynski, MD
( The need for additional effective therapies for metastatic castration resistant prostate cancer (mCRPC) is omnipresent, particularly as therapies previously used in later lines or only in CRPC are now being deployed in earlier disease states. Among well-established mechanisms of resistance are alterations in the androgen receptor (AR), including mutations and copy number changes, which effect its activity and ligand independent signaling. EPI-7386 is an aniten, a class of compounds which can inhibitor AR activity by binding to the N-terminal domain (NTD) irrespective of resistance abrogation in the ligand binding domain that may otherwise make AR signaling inhibitors ineffective, as supported by preclinical data. Trial of this agent in a first-in-human study in heavily pre-treated patients with mCRPC was undertaken (NCT04221222), and preliminary data are reported here.
Presented by Andrew Laccetti, MD, MS
( Alterations in the Androgen Receptor (AR) remain a common locus for castration resistance in prostate cancer (CRPC), and impact response to AR-targeted novel hormonal therapies, including enzalutamide. Dr. Laccetti and colleagues present preliminary safety and efficacy data on the combination of enzalutamide with a next generation antigen EPI-7386 in chemotherapy-exposed patients with CRPC prior to exposure to any AR pathway inhibitor.
Presented by Andrew Laccetti, MD, MS
Reno, Nevada ( -- ESSA Pharma Inc., a clinical-stage pharmaceutical company focused on developing novel therapies for the treatment of prostate cancer, announced that further analyses of initial clinical data from two Phase 1 studies of EPI-7386 in patients with metastatic castration-resistant prostate cancer ("mCRPC") will be presented at the 2023 American Society of Clinical Oncology Genitourinary Cancers Symposium ("ASCO GU"), taking place February 16-19, 2023, in San Francisco, California and online. EPI-7386 is a first-in-class N-terminal domain androgen receptor ("AR") inhibitor that suppresses androgen activity through a novel mechanism of action. The two poster presentations are available on the ASCO GU Digital Program and the "Publications" section of the Company's website at