Esperion Therapeutics Announces Publication of Definitive Paper on Bempedoic Acid Mechanism of Action in Nature Communication...
November 28 2016 - 4:30PM
Esperion Therapeutics, Inc. (NASDAQ:ESPR), a pharmaceutical company
focused on developing and commercializing oral therapies for the
treatment of patients with elevated low density lipoprotein
cholesterol (LDL-C), today announced the publication of
“Liver-specific ATP-citrate lyase inhibition by bempedoic acid
decreases LDL-C and attenuates atherosclerosis,” by Stephen L.
Pinkosky et al. in Nature Communications, available at:
http://www.nature.com/articles/ncomms13457. The paper
systematically outlines the experiments and analyses undertaken by
Esperion and its collaborators to fully understand the mechanism of
action for how bempedoic acid reduces LDL-C.
Bempedoic acid is a pro-drug that requires activation to the CoA
form to inhibit adenosine triphosphate (ATP) citrate lyase, an
important enzyme on the cholesterol biosynthesis pathway. The
specific enzyme required for this activation was identified as
acetyl-CoA synthetase long chain 1 (ACSVL1), found in the liver but
not found in skeletal muscle. Since bempedoic acid has no activity
in skeletal muscle there is minimal risk for the muscle-related
adverse events that have been associated with the use of
statins.
Importantly, ATP citrate lyase (ACL) inhibition, mediated by
bempedoic acid, results in decreased cholesterol biosynthesis, up
regulation of LDL receptors, and reduction in LDL-C levels. In
addition, bempedoic acid also reduced the progression of
atherosclerosis in preclinical models.
“We are pleased that the research conducted by our scientific
team on the liver-specific mechanism of action for bempedoic acid
has been recognized in Nature Communications, a journal whose
prestige speaks to the high quality of our science and research.
Bempedoic acid targets ACL, the key differentiating feature of the
molecule and has also been shown to complement the effects of
statins, which target HMG-CoA reductase,” said Tim Mayleben,
president and chief executive officer of Esperion Therapeutics.
“The publication of these results will provide the scientific and
medical communities information to better understand both how
bempedoic acid reduces elevated LDL-C, and why bempedoic acid
appears to be associated with minimal risk for the muscle-related
adverse events that have been associated with the use of
statins.”
About Bempedoic Acid
Bempedoic acid is a first-in-class ACL inhibitor that reduces
cholesterol biosynthesis and lowers elevated levels of LDL-C by
up-regulating the LDL receptor, but with reduced potential for
muscle-related side effects. Completed Phase 1 and 2 studies in
more than 800 patients treated with bempedoic acid have produced
clinically relevant LDL-C lowering results of up to 30 percent as
monotherapy, approximately 50 percent in combination with
ezetimibe, and an incremental 20 to 22 percent when added to stable
statin therapy.
Esperion's Commitment to Patients with
Hypercholesterolemia
In the United States, 78 million people, or more than 20 percent
of the population, have elevated LDL-C; an additional 73 million
people in Europe and 30 million people in Japan also live with
elevated LDL-C. Esperion's mission is to provide patients and
physicians with a new oral therapy to significantly reduce elevated
levels of LDL-C in patients inadequately treated with current
lipid-modifying therapies. Esperion-discovered and developed,
bempedoic acid is an oral LDL-C lowering therapy in Phase 3
development. The Company plans to develop bempedoic acid as a
monotherapy as well as a fixed dose combination (FDC) with
ezetimibe, with a particular focus on patients inadequately treated
with current lipid-modifying therapies. It is estimated that
approximately 5-20 percent of patients who are prescribed statins
are only able to tolerate less than the lowest approved daily
starting dose of their statin ("statin intolerant").
About Esperion Therapeutics
Esperion Therapeutics, Inc. is a pharmaceutical company
focused on developing and commercializing oral therapies for the
treatment of patients with elevated LDL-C. Through scientific and
clinical excellence, and a deep understanding of cholesterol
biology, the team at Esperion is committed to developing new LDL-C
lowering therapies that will make a substantial impact on reducing
global cardiovascular disease; the leading cause of death around
the world. Bempedoic acid, the Company's lead product candidate,
significantly reduces elevated LDL-C levels in patients with
hypercholesterolemia, including patients inadequately treated with
current lipid-modifying therapies. For more information, please
visit www.esperion.com and follow us on Twitter
at https://twitter.com/EsperionInc.
Forward-Looking Statements
This press release contains forward-looking statements that are
made pursuant to the safe harbor provisions of the federal
securities laws, including statements regarding the therapeutic
potential of, and clinical development plan for, bempedoic acid.
Any express or implied statements contained in this press release
that are not statements of historical fact may be deemed to be
forward-looking statements. Forward-looking statements involve
risks and uncertainties that could cause Esperion's actual results
to differ significantly from those projected, including the risks
detailed in Esperion's filings with the Securities and Exchange
Commission. You are cautioned not to place undue reliance on the
forward-looking statements, which speak only as of the date of this
release. Esperion disclaims any obligation or undertaking to update
or revise any forward-looking statements contained in this press
release, other than to the extent required by law.
Media Contact:
Elliot Fox
W2O Group
212.257.6724
efox@w2ogroup.com
Investor Contact:
Mindy Lowe
Esperion Therapeutics, Inc.
734.887.3903
mlowe@esperion.com
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