Resverlogix Announces New Research Findings Highlighting the Safety of BD2-selective BET Inhibitors
June 08 2022 - 6:12AM
Resverlogix Corp. ("Resverlogix") (TSX:RVX) today announced the
publication of an article entitled “Breaking boundaries: Pan BETi
disrupt 3D chromatin structure, BD2-selective BETi are strictly
epigenetic transcriptional regulators” in the journal Biomedicine
& Pharmacotherapy. The article uncovers a clear mechanism for
the improved safety, and reduced off-target effects, seen with
BD2-selective BET inhibitors in comparison with non-selective BET
inhibitors.
The article is published online HERE.
“This research helps us better understand the important
differences between selective and non-selective BET inhibition as
therapeutic strategies,” said Dr. Ewelina Kulikowski, Senior Vice
President, Research & Development, and the senior author of the
article. “BD2-selective inhibitors, such as apabetalone, can
inhibit the expression of disease-causing genes without disrupting
the fundamental functions of cells.”
Publication Highlights Include:
- A new role for BET protein BRD4 was discovered, in maintaining
the higher order structure of chromatin at topologically
associating domain (TAD) boundaries
- Maintaining the structure of TAD boundaries is critical for the
basic functioning of cells, and disrupting the boundaries can lead
to cell death
- As a result of differing interactions with BRD4, non-selective
BET inhibitors disrupt TAD boundaries, while BD2-selective BET
inhibitors do not
- These findings contribute to a potential mechanism underlying
the differences in clinical safety outcomes observed between
BD2-selective and non-selective BET inhibitors
Other Recent Publications
Another article, entitled “Inhibition of epigenetic reader
proteins by apabetalone counters inflammation in activated innate
immune cells from Fabry disease patients receiving enzyme
replacement therapy”, was recently published in the journal
Pharmacology Research & Perspectives. The article details the
beneficial impacts of apabetalone treatment on inflammatory
pathways in immune cells from Fabry disease patients. These
findings suggest that apabetalone is a promising therapeutic
candidate for the rare disorder. The article is available online
HERE.
About Apabetalone
Apabetalone (RVX-208), is a first-in-class, small molecule,
therapeutic candidate with an epigenetic mechanism of action.
It is a BD2 (bromodomain) selective BET (bromodomain
and extra-terminal) inhibitor that works in preventing
and treating disease progression by regulating the expression
of disease-causing genes.
Due to the extensive role for BET proteins in the human body,
apabetalone, can simultaneously target multiple disease-related
biological processes while maintaining a well-described safety
profile – leading to a new way to treat chronic disease.
Apabetalone received Breakthrough Therapy Designation from the US
Food and Drug Administration (FDA) and is the only drug of its
class with an established safety record in human clinical trials,
with well over 4200 patient-years of safety data across 10 clinical
trials.
COVID-19:
Studies – published in prestigious scientific journals
(including Cell) – demonstrate that apabetalone has the potential
to act against COVID-19 with a unique dual-mechanism: first by
preventing viruses from entering the cells and replicating; and
second by averting excessive inflammatory reactions that can cause
severe and lasting organ damage. The investigational treatment
could potentially reduce the severity and duration of COVID-19.
Apabetalone’s unique dual-mechanism also means that it has the
potential to show efficacy against new COVID-19 variants and may
even help fight other viruses.
Resverlogix has partnered with EVERSANA™, the pioneer of next
generation commercial services to the global life sciences
industry, to support the rapid commercialization of apabetalone for
COVID-19 in Canada and the United States. EVERSANA™ is currently
leading clinical outreach and advocacy for apabetalone in the
Canadian market.
Cardiology:
Apabetalone is the first therapy of its kind to receive
Breakthrough Therapy Designation from the US Food and Drug
Administration (FDA) – for a major cardiovascular indication –
following the ground-breaking findings from the BETonMACE Phase 3
study. Data from BETonMACE showed apabetalone can potentially
prevent major adverse cardiac events among high-risk cardiovascular
disease patients who also have type 2 diabetes mellitus.
About Resverlogix
Founded in 2001, Resverlogix is a Calgary based late-stage
biotechnology company and the world leader in epigenetics, or gene
regulation, with the goal of developing first-in-class therapies
for the benefit of patients with chronic disease.
Resverlogix is developing a new class of epigenetic therapies
designed to regulate the expression of disease-causing genes. We
aim to improve patients’ lives by restoring biological functions –
altered by serious illnesses such as cardiovascular disease – back
to a healthier state.
The Company’s clinical program is focused on evaluating the lead
epigenetic candidate apabetalone for the treatment of
cardiovascular disease and associated comorbidities, and
COVID-19.
Resverlogix common shares trade on the Toronto Stock Exchange
(TSX:RVX).
Follow us: Twitter: @Resverlogix_RVX. LinkedIn:
https://www.linkedin.com/company/resverlogix-corp-/
Forward Looking Statements:
This news release may contain certain forward-looking
information as defined under applicable Canadian securities
legislation, that are not based on historical fact, including
without limitation statements containing the words "believes",
"anticipates", "plans", "intends", "will", "should", "expects",
"continue", "estimate", "forecasts" and other similar expressions.
In particular, this news release includes forward looking
information related to the potential role of apabetalone in the
treatment of patients with COVID-19, cardiovascular disease and
associated comorbidities and other chronic diseases. Our actual
results, events or developments could be materially different from
those expressed or implied by these forward-looking statements. We
can give no assurance that any of the events or expectations will
occur or be realized. By their nature, forward-looking statements
are subject to numerous assumptions and risk factors including
those discussed in our Annual Information Form and most recent
MD&A which are incorporated herein by reference and are
available through SEDAR at www.sedar.com. The forward-looking
statements contained in this news release are expressly qualified
by this cautionary statement and are made as of the date hereof.
The Company disclaims any intention and has no obligation or
responsibility, except as required by law, to update or revise any
forward-looking statements, whether as a result of new information,
future events or otherwise.
For further information please contact:
Investor RelationsEmail:
ir@resverlogix.comPhone:
403-254-9252www.resverlogix.com
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