HOUSTON and VANCOUVER,
May 15, 2020 /CNW/ - ESSA Pharma Inc.
(Nasdaq: EPIX; TSX-V: 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 Virtual American Urological
Association ("AUA") Annual Meeting.
In an oral poster presentation titled, "The preclinical
characterization and development of EPI-7386, an N-terminal domain
androgen receptor inhibitor for the treatment of prostate cancer",
a more in-depth preclinical characterization of EPI-7386 including
gene expression analyses and the toxicologic profile was presented.
The studies highlight new information about EPI-7386 including:
- In vitro cellular gene expression
analyses demonstrate that EPI-7386:
-
- Inhibits androgen-induced genes with major similarities but
some differences from enzalutamide in a cellular model sensitive to
androgen receptor inhibitors.
- In the same cellular model, the combination of enzalutamide and
EPI-7386 inhibits androgen-induced gene expression more completely
and broadly.
- EPI-7386 shows superiority to enzalutamide in inhibiting
androgen-induced genes in an androgen receptor resistant model, and
in contrast to enzalutamide, also blocks genes induced by the AR-V7
androgen receptor splice variant.
- Toxicology studies evaluating the safety profile of EPI-7386
demonstrate that:
-
- Very high plasma exposures of EPI-7386 were achieved across all
studies.
- The drug was well tolerated at both the low and middle doses,
corresponding to drug plasma exposures 2-5 fold higher than the
efficacious exposures achieved in mouse xenograft models.
- 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
"The breadth of in vitro and in vivo studies
utilized to profile EPI-7386 preclinically demonstrate an
encouraging profile for EPI-7386 across a variety of antiandrogen
sensitive and antiandrogen-resistant cellular models, xenograft and
patient-derived xenograft mouse models, and gene expression
analyses. The favorable toxicologic profile of EPI-7386 observed in
our IND-enabling studies at very high exposures will permit
initiation of the Phase 1 study at a dose of 200 mg per day, which
should allow us to reach biologically relevant blood levels of
EPI-7386 in patients quickly," said Dr. David R. Parkinson, President & Chief
Executive Officer. "We look forward to beginning patient
dosing soon in our initial phase 1 study of EPI-7386 in mCRPC
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 metastatic
castration-resistant prostate cancer ("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, 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 regarding EPI-7386, including those 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.
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