Orally bioavailable ANITACâ„¢
degraders can eliminate full length, mutant and splice variant
forms of AR that are expressed in castration-resistant prostate
cancer (CRPC) patients
ANITAC degraders inhibit AR-dependent
transcription and reduce viability of AR-dependent prostate cancer
cells
Data to be presented at the 2022 American
Association for Cancer Research Annual Meeting
SOUTH
SAN FRANCISCO, CALIFORNIA and VANCOUVER, BC, April 8,
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 first generation of androgen receptor (AR) ANITen
bAsed Chimera (ANITACâ„¢) N-terminal domain (NTD) degraders at the
2022 American Association for Cancer Research (AACR) Annual
Meeting.
"We look forward to presenting our first preclinical data
demonstrating the potential of ESSA's ANITAC degraders as a new
approach to AR pathway inhibition. The NTD is a promising target
for the suppression of AR biology which is responsible for driving
most prostate cancers, but due to the intrinsically disordered
nature of the NTD region of AR, it has been generally considered
undruggable. Through their unique ability to bind to the NTD of AR,
ANITACs have the ability to inhibit NTD-mediated AR transcription
while also degrading AR protein including resistant forms of AR
which are commonly associated with castration-resistant prostate
cancer," said Dr. David. R. Parkinson, Chief Executive Officer,
ESSA Pharma Inc. "Our bifunctional degraders leverage ESSA's deep
scientific expertise and success in targeting the AR NTD with a new
treatment modality aimed at suppressing AR biology by eliminating
the AR protein itself. We look forward to providing further updates
this year from this exciting new preclinical program."
The preclinical results demonstrate that ANITAC degraders
utilize the ubiquitin proteasome system and can degrade many forms
of AR including full length, mutant and splice variants which are
often expressed in CRPC patients. Specifically, the ANITAC
degraders show robust potency in inhibiting AR transcriptional
activity driven by AR-FL, AR-V7, or AR-V567es. In addition, the
orally bioavailable ANITAC degraders exhibit high potency in
inhibiting AR-dependent transcription and reducing viability of
AR-dependent prostate cancer cells.
Poster presentation details are as follows:
Title: Androgen receptor (AR) N-Terminal Domain
degraders can degrade AR full length and AR splice variants in CRPC
preclinical models
Authors: Nan Hyung Hong, et al.
Abstract
Number: 429
Session Title: Protein Degraders and Proteasome
Inhibitors
Session Date and Time: Sunday, April
10, 2022 | 1:30 p.m. - 5:00 p.m.
ET
Location: New Orleans Convention Center, Exhibit Halls
D-H, Poster Section 26
The poster is available to 2022 AACR Annual Meeting attendees
and in the Science 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 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 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.
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 the potential of ESSA's ANITAC degraders as a new
approach to AR pathway inhibition, NTD being a promising target for
the suppression of AR biology, the potential benefits of ANITAC
degraders, the anticipated timeline for providing further updates
on preclinical programs, the ability of ANITAC degraders to
utilize the ubiquitin proteasome system and degrade many forms of
AR, inhibit AR-dependent transcription and reduce viability of
AR-dependent prostate cancer cells and other statements surrounding
the Company's clinical evaluation of ANITAC degraders.
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 February 3, 2022 under the heading "Risk
Factors", a copy of which is available on ESSA's profile on EDGAR
at www.sec.gov, and as otherwise disclosed from time to
time on ESSA's SEDAR profile www.sedar.com.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.
View original
content:https://www.prnewswire.com/news-releases/essa-pharma-announces-the-presentation-of-preclinical-data-for-its-first-generation-of-androgen-receptor-n-terminal-domain-degraders-301520601.html
SOURCE ESSA Pharma Inc