ESSA Pharma Presents Preclinical Data for its First Generation Androgen Receptor N-Terminal Domain Degrader at the 34th EORTC-NCI-AACR Symposium
ESSA Pharma Inc. (NASDAQ: EPIX) presented preclinical data for its first generation androgen receptor (AR) degrader, EPI-8207, at the 34th EORTC-NCI-AACR Annual Symposium in Barcelona. The data shows EPI-8207 effectively degrades AR, including splice variants and mutants associated with castration-resistant prostate cancer. This research highlights the potential of ANITAC in targeting AR signaling, a key driver in prostate cancer progression. The study indicates EPI-8207's high potency in inhibiting AR-dependent transcription, positioning ESSA for advancements in prostate cancer therapy.
- EPI-8207 demonstrated robust potency in degrading AR, including splice variants and clinically relevant mutants.
- High efficacy in inhibiting AR-dependent transcription was shown in preclinical models, indicating strong therapeutic potential.
- None.
SOUTH SAN FRANCISCO, California and VANCOUVER, Canada, Oct. 26, 2022 /PRNewswire/ - ESSA Pharma Inc. ("ESSA", or the "Company") (NASDAQ: EPIX), a clinical-stage pharmaceutical company focused on developing novel therapies for the treatment of prostate cancer, today announced the presentation of preclinical data for its lead first generation androgen receptor ("AR") ANITen bAsed Chimera ("ANITAC"™) N-terminal domain ("NTD") degrader in a poster session at the 34th EORTC-NCI-AACR Annual Symposium on Molecular Targets and Cancer Therapeutics in Barcelona, Spain.
The preclinical data demonstrate that EPI-8207, an ANITAC, shows robust potency degrading AR, including AR splice variants and clinically relevant AR mutants that can potentially drive disease progression in patients with castration-resistant prostate cancer ("CRPC"). In addition, EPI-8207 exhibits high potency in inhibiting AR-dependent transcription.
34th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics
Title: Advances in the Development of a Targeted N-Terminal Domain Androgen Receptor Degrader (ANITAC) for the Treatment of Prostate Cancer
Authors: Nan Hyung Hong, et al.
Abstract Number: 103
Session Title: New Drugs
The poster is available on the EORTC-NCI-AACR Annual Symposium website at www.eortc.org/ena and on the "Publications" section of the Company's website at www.essapharma.com.
Androgen receptor signaling is the main driver of prostate cancer progression and remains a crucial target for therapeutic intervention in late stages of the disease. While current antiandrogen therapies that directly or indirectly target the AR ligand-binding domain (LBD) are initially effective, resistance ultimately develops and new methods of inhibiting the AR pathway are needed.
ESSA's novel approach of targeting the N-terminal domain of the AR represents a new method of blocking AR signaling. Leveraging ESSA's scientific foundation in successfully targeting the NTD of the AR with a new class of small molecules called anitens, ESSA is developing the first generation of ANITen bAsed Chimera degraders targeting the AR NTD. In preclinical models, the orally bioavailable ANITAC degraders can eliminate forms of AR protein found in castration-resistant prostate cancer that can potentially drive disease progression including LBD mutants and LBD truncated splice variants.
Prostate cancer is the second-most commonly diagnosed cancer among men and the fifth most common cause of male cancer death worldwide (Globocan, 2018). Adenocarcinoma of the prostate is dependent on androgen for tumor progression and depleting or blocking androgen action has been a mainstay of hormonal treatment for over six decades. Although tumors are often initially sensitive to medical or surgical therapies that decrease levels of testosterone, disease progression despite castrate levels of testosterone can lead to metastatic CRPC ("mCRPC"). The treatment of mCRPC patients has evolved rapidly over the past ten years. Despite these advances, many patients with mCRPC fail or develop resistance to existing treatments, leading to continued disease progression and limited survival rates.
ESSA is a clinical-stage pharmaceutical company focused on developing novel and proprietary therapies for the treatment of patients with prostate cancer. For more information, please visit www.essapharma.com and follow us on Twitter under @ESSAPharma.
This release contains certain information which, as presented, constitutes "forward-looking information" within the meaning of the Private Securities Litigation Reform Act of 1995 and/or applicable Canadian securities laws. Forward-looking information involves statements that relate to future events and often addresses expected future business and financial performance, containing words such as "anticipate", "believe", "plan", "estimate", "expect", and "intend", statements that an action or event "may", "might", "could", "should", or "will" be taken or occur, or other similar expressions and includes, but is not limited to, statements regarding, presentations with respect to preclinical data for the AR ANITAC™ NTD degrader, the results of the initial preclinical data, including the favorable pharmaceutical properties of EPI-8207 and other statements surrounding the Company's preclinical evaluation of EPI-8207.
Forward-looking statements and information are subject to various known and unknown risks and uncertainties, many of which are beyond the ability of ESSA to control or predict, and which may cause ESSA's actual results, performance or achievements to be materially different from those expressed or implied thereby. Such statements reflect ESSA's current views with respect to future events, are subject to risks and uncertainties and are necessarily based upon a number of estimates and assumptions that, while considered reasonable by ESSA as of the date of such statements, are inherently subject to significant medical, scientific, business, economic, competitive, political and social uncertainties and contingencies. In making forward looking statements, ESSA may make various material assumptions, including but not limited to (i) the accuracy of ESSA's financial projections; (ii) obtaining positive results of clinical trials; (iii) obtaining necessary regulatory approvals; and (iv) general business, market and economic conditions.
Forward-looking information is developed based on assumptions about such risks, uncertainties and other factors set out herein and in ESSA's Quarterly Report on Form 10-Q dated August 4, 2022 under the heading "Risk Factors", a copy of which is available on ESSA's profile on EDGAR at www.sec.gov and on the SEDAR website at www.sedar.com, and as otherwise disclosed from time to time on ESSA's EDGAR and SEDAR profiles. Forward-looking statements are made based on management's beliefs, estimates and opinions on the date that statements are made and ESSA undertakes no obligation to update forward-looking statements if these beliefs, estimates and opinions or other circumstances should change, except as may be required by applicable United States and Canadian securities laws. Readers are cautioned against attributing undue certainty to forward-looking statements.
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