- Data
presented at the 2021 AACR-NCI-EORTC Virtual International
Conference on Molecular Targets and Cancer Therapeutics –
VANCOUVER, Canada and
HOUSTON, Texas, Oct. 7, 2021 /CNW/ - 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 characterizing the mechanism of action of EPI-7386, ESSA's
lead product candidate for the treatment of prostate cancer. The
data include the results of nuclear magnetic resonance (NMR)
studies which confirm the binding of the compound to the N-terminal
domain (NTD) of the androgen receptor (AR), a region not currently
targeted by other antiandrogen therapies. Data were presented in a
virtual video poster format at the 2021 American Association for
Cancer Research (AACR), National Cancer Institute (NCI), and
European Organisation for Research and Treatment of Cancer (EORTC)
Virtual International Conference on Molecular Targets and Cancer
Therapeutics, taking place virtually from October 7-10, 2021.
The virtual poster presentation, titled, "Comprehensive
preclinical characterization of the mechanism of action of
EPI-7386, an androgen receptor N-terminal domain inhibitor," will
be presented and available for viewing starting October 7, 2021 at 9:00
a.m. ET.
The preclinical data confirm EPI-7386's target engagement with
the NTD of the AR through multiple studies:
- Three separate orthogonal NMR approaches confirm that EPI-7386
binds to the Tau5 region of the NTD
- Cellular thermal shift assays (CETSA) confirm engagement of
EPI-7386 with both full length AR (AR-FL) and AR-V567es, a splice
variant lacking the ligand-binding domain (LBD)
- Gene expression driven by the AR splice variant, AR-V567es, can
be inhibited by EPI-7386 whereas enzalutamide and darolutamide,
which bind to the LBD, cannot inhibit AR-V567es-driven gene
expression
- Chromatin immunoprecipitation sequencing (ChIP-Seq) data
indicate that EPI-7386 inhibits androgen-induced changes at the AR
cistrome and when combined with enzalutamide, can completely
abrogate genome-wide androgen-induced AR binding
"We are excited by the data presented today, which support
ESSA's novel approach to prostate cancer by definitively
demonstrating that EPI-7386 binds to the N-terminal domain of the
androgen receptor—the primary driver of prostate cancer growth,"
said Dr. David R. Parkinson, M.D.,
President and Chief Executive Officer of ESSA Pharma Inc. "Through
this unique mechanism of AR inhibition, EPI-7386 can inhibit
AR-driven biology in both full length and splice variant-driven
prostate cancer models. Additionally, the data demonstrate that the
combination of EPI-7386 with enzalutamide results in complete
inhibition of genome-wide androgen-induced AR binding, supporting
the rationale for our upcoming Phase 1/2 combination trials of
EPI-7386 with approved antiandrogens in patients with metastatic
castration-resistant prostate cancer."
The poster is available on the 2021 AACR-NCI-EORTC Virtual
International Conference website and on the "Events &
Presentations" section of the Company's website at
www.essapharma.com.
About ESSA Pharma Inc.
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.
About EPI-7386
EPI-7386 is an investigational,
highly-selective, oral, small molecule inhibitor of the N-terminal
domain of the androgen receptor. EPI-7386 is currently being
studied in a Phase 1 clinical trial (NCT04421222) in men with
metastatic castration-resistant prostate cancer ("mCRPC") whose
tumors have progressed on current standard-of-care therapies. The
Phase I clinical trial of EPI-7386 began in Q3 of 2020 following
FDA allowance of the IND and Health Canada acceptance. The U.S. FDA
has granted Fast Track designation to EPI-7386 for the treatment of
adult male patients with mCRPC resistant to standard-of-care
treatment. ESSA retains all rights to EPI-7386 worldwide.
About Prostate Cancer
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
castration-resistant prostate cancer ("mCRPC"). The treatment of
mCRPC patients has evolved rapidly over the past 10 years. Despite
these advances, many patients with mCRPC fail or develop resistance
to existing treatments, leading to continued disease progression
and limited survival rates.
Forward-Looking Statement Disclaimer
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 preclinical data characterizing the mechanism of action
of EPI-7386 supporting ESSA's novel approach to prostate cancer,
EPI-7386's ability to inhibit AR-driven biology in both full length
and splice variant driven prostate cancer models, and the data
supporting the rationale for the Company's upcoming Phase 1/2
combination trials of EPI-7386.
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 16, 2021 under the heading "Risk Factors",
a copy of which is available on ESSA's profile on EDGAR at
www.sec.gov.com 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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SOURCE ESSA Pharma Inc