HOUSTON and VANCOUVER, BC,
June 22, 2020 /CNW/ - ESSA Pharma
Inc. (Nasdaq: EPIX); (TSXV: EPI), a clinical-stage pharmaceutical
company focused on developing novel therapies for the treatment of
prostate cancer, today presented new preclinical data on ESSA's
clinical candidate, EPI-7386, at the 2020 American Association for
Cancer Research ("AACR") Virtual Annual Meeting
II.
In an oral poster presentation titled, "Preclinical development
of the second-generation N-terminal domain androgen receptor
inhibitor, EPI-7386, for the treatment of prostate cancer", a
robust preclinical characterization of EPI-7386 including androgen
receptor (AR) binding, gene expression analyses and the toxicologic
profile was presented. The studies highlight new information about
EPI-7386 including:
- Full-length AR target engagement by EPI-7386 was confirmed
in a cellular thermal shift assay.
- In vitro cellular gene expression analyses
demonstrate that EPI-7386:
-
- Inhibits AR transcriptional activity similar to enzalutamide
but with a few notable qualitative and quantitative differences in
an enzalutamide-sensitive cellular model.
- In the same cellular model, combination treatment of EPI-7386
with enzalutamide displays broader and deeper inhibition of
AR-associated transcriptional activity than higher doses of each
single agent alone.
- Shows superior activity to enzalutamide in an AR-V7-driven
cellular model by modulating both AR-FL and AR-V7-driven gene
expression.
- Toxicology studies evaluating the safety profile of EPI-7386
demonstrate that:
-
- Very high plasma exposures of EPI-7386 were achieved across all
studies.
- Tolerability in 28-days tox studies in rats and dogs at AUC ≤
2,000,000 ng*hr/mL, with activity seen on androgen-sensitive target
organs in dogs.
- The highest doses tested were characterized as the HNSTD
(highest non-severely toxic dose) and only exhibited body weight
loss and reduced food consumption. The drug plasma exposures
achieved at this high dose were 7-10 fold higher than the
efficacious exposures achieved in mouse xenograft models.
- The starting clinical dose of EPI-7386 will be 200 mg given
once-daily
"Our latest transcriptomic analyses add to the breadth of
preclinical data supporting the development of EPI-7386 broadly in
prostate cancer. With the favorable toxicologic profile of EPI-7386
observed in our IND-enabling studies at very high exposures, we
will initiate dosing at 200 mg per day, which potentially could
allow us to efficiently reach biologically relevant blood levels of
EPI-7386 in patients," said Dr. David R.
Parkinson, President & Chief Executive Officer.
"We will soon begin dosing patients in our Phase 1 monotherapy
study of EPI-7386 in castration-resistant prostate cancer patients
whose tumors are progressing on current anti-androgens.".
About ESSA Pharma Inc.
ESSA is a clinical-stage
pharmaceutical company focused on developing novel and proprietary
therapies for the treatment of castration-resistant prostate cancer
in patients whose disease is progressing despite treatment with
current therapies. ESSA's proprietary "aniten" compounds bind to
the N-terminal domain of the androgen receptor ("AR"), inhibiting
AR driven transcription and the AR signaling pathway in a unique
manner which bypasses the drug resistance mechanisms associated
with current anti-androgens. The Company is currently conducting a
phase 1 study of EPI-7386 in patients with mCRPC who are failing
current standard-of-care therapies. For more information, please
visit www.essapharma.com and follow us on Twitter under
@ESSAPharma.
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 generally represents a
transition to the lethal variant of the disease, mCRPC, and most
patients ultimately succumb to the illness. The treatment of mCRPC
patients has evolved rapidly over the past five years. Despite
these advances, additional treatment options are needed to improve
clinical outcomes in patients, particularly those who fail existing
treatments including abiraterone or enzalutamide, or those who have
contraindications to receive those drugs. Over time, patients with
mCRPC generally experience continued disease progression, worsening
pain, leading to substantial morbidity and limited survival rates.
In both in vitro and in vivo animal studies, ESSA's novel approach
to blocking the androgen pathway has been shown to be effective in
blocking tumor growth when current therapies are no longer
effective.
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
that preclinical data support the development of EPI-7386 broadly
in prostate cancer, the timing and enrollment of a Phase 1 study of
EPI-7386, future presentations with respect to EPI-7386
and the content thereof, and other statements surrounding the
Company's clinical evaluation 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 Annual Report on Form 20-F dated December 19, 2019 under the heading "Risk
Factors", a copy of which is available on ESSA's profile on the
SEDAR website at www.sedar.com, ESSA's profile on EDGAR at
www.sec.gov, and as otherwise disclosed from time to time on ESSA's
SEDAR profile. 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 Canadian and United
States securities laws. Readers are cautioned against
attributing undue certainty to forward-looking statements.
Neither TSX Venture Exchange nor its Regulation Services
Provider (as that term is defined in the policies of the TSX
Venture Exchange) accepts responsibility for the adequacy or
accuracy of this release.
View original
content:http://www.prnewswire.com/news-releases/essa-pharma-presents-therapeutic-potential-of-epi-7386-at-the-2020-american-association-for-cancer-research-virtual-annual-meeting-ii-301080763.html
SOURCE ESSA Pharma Inc