SAN DIEGO, Nov. 15, 2016 /PRNewswire/ -- Viking
Therapeutics, Inc. ("Viking") (NASDAQ: VKTX), a clinical-stage
biopharmaceutical company focused on the development of novel,
first-in-class or best-in-class therapies for metabolic and
endocrine disorders, today announced additional data from its
previously completed Phase 1b clinical trial of VK2809 in subjects
with mild hypercholesterolemia. Data from an analysis of the
study participants' atherogenic protein levels demonstrated that
subjects experienced statistically significant reductions in
lipoprotein(a) [Lp(a)] and apolipoprotein B-100 (apo B).
These results were highlighted in a poster presentation on
November 14 at the American Heart
Association (AHA) Scientific Sessions 2016, in New Orleans, LA.
VK2809 is a novel, orally available small molecule thyroid
receptor agonist that possesses selectivity for liver tissue, as
well as the beta receptor subtype, suggesting promising therapeutic
potential in this patient population. Previously reported
data have demonstrated that treatment with VK2809 leads to rapid
reductions in plasma LDL cholesterol (LDL-C) and triglycerides in
subjects with mild hypercholesterolemia. The new results
presented at AHA outline VK2809's effect on additional proteins
associated with cardiovascular disease (CVD).
The study was a randomized, double-blind, placebo-controlled
Phase 1b trial designed to evaluate the safety, tolerability and
pharmacokinetics of a range of VK2809 doses in 56 subjects with
elevated serum cholesterol (n = 6 per drug-treated cohort).
Following 14 days of VK2809 treatment, subjects experienced
statistically significant placebo-adjusted, least square mean
reductions in both Lp(a) and apo B across a range of doses.
Reductions in apo B ranged from 20.2% at 5 mg (p = 0.0008) to 39.6%
at 40 mg (p < 0.0001); reductions in Lp(a) ranged from 31.6% at
5 mg (p = 0.12) to 54.9% at 20 mg (p = 0.002). Comparable
results were obtained with or without least square mean
adjustments, which account for covariates in patient
characteristics.
The therapeutic importance of reducing atherogenic proteins has
been highlighted in scientific literature. A report published
in the Mayo Clinic Proceedings stated that Lp(a) was an
independent, causal, risk factor for atherosclerosis, and that
epidemiologic data show a continuous association between Lp(a) and
CVD that is multiplied when both LDL-C and Lp(a) are
elevated.1 Similarly, determination of apo B
levels has been characterized as superior to any other cholesterol
index to identify increased risk of CVD and assess the efficacy of
lipid-lowering treatment.2 Thus, robust reductions
of both Lp(a) and apo B, as demonstrated by VK2809 in this study,
may add to the benefits of LDL-lowering therapy by further
improving a patient's cardiovascular risk profile.
"These data support the promise of thyroid beta-targeted
approaches for the treatment of cardiovascular and other metabolic
diseases. We previously reported results showing VK2809's
ability to rapidly reduce plasma LDL-C and triglycerides by up to
41% and 79%, respectively, following just 14 days of treatment,"
said Brian Lian, Ph.D., chief
executive officer of Viking. "Today's announcement highlights
the added benefit of VK2809 on reducing key proteins associated
with elevated cardiovascular risks. The combined benefits
from reducing both LDL-C and atherogenic proteins suggest a
differentiated therapeutic profile, which may result in improved
long-term benefits for patients with lipid or other metabolic
abnormalities, including fatty liver disease. We look forward
to the results of our ongoing Phase 2 trial of VK2809 in patients
with hypercholesterolemia and fatty liver disease, which we expect
to complete in 1H17."
Treatment with VK2809 was shown to be safe and well-tolerated at
all doses studied in this trial. No serious adverse events
were reported and no treatment- or dose-related trends were
observed for abnormal vital signs, electrocardiograms, cardiac
rhythm or physical examination assessments. Consistent with
liver-targeted thyroid receptor activation, mild, asymptomatic
elevations in liver enzymes and decreased thyroid hormone levels
were observed at higher doses. Metabolically, VK2809 was not
eliminated intact through the kidneys, and less than 3% of the
administered dose was eliminated through the kidneys as the drug's
active metabolite, VK2809A.
Viking previously announced top-line data from the Phase 1b
trial which demonstrated clinically and statistically significant
placebo-adjusted reductions in LDL-C ranging from 15.2% at the 5.0
mg dose (p=0.026) to 41.2% at the 20 mg dose (p<0.0001).
In addition, subjects experienced placebo-adjusted reductions in
triglycerides ranging from 34.8% at 5.0 mg dose (p=0.052) to 78.6%
at the 40 mg dose (p=0.0001).
The company recently initiated a Phase 2 clinical trial of
VK2809 in patients with primary hypercholesterolemia and
non-alcoholic fatty liver disease. The Phase 2 clinical
trial is a randomized, double-blind, placebo-controlled, parallel
group study designed to evaluate the efficacy, safety and
tolerability of VK2809 in approximately 80 patients with elevated
LDL-C and non-alcoholic fatty liver disease.
References:
1Mayo Clinic Proceedings, November 2013; 88(11): 1294-1311.
2J. Intern. Med., March
2006; 259(3): 247-258.
About VK2809
VK2809 is an orally available, tissue and
receptor-subtype selective agonist of the thyroid beta receptor in
Phase 2 development for the treatment of patients with
hypercholesterolemia and fatty liver disease. VK2809 belongs
to a family of novel prodrugs which are cleaved in vivo to
release potent thyromimetics. Selective activation of the TRß
receptor in liver tissue is believed to favorably affect
cholesterol and lipoprotein levels via multiple mechanisms,
including increasing the expression of low-density lipoprotein
(LDL) receptors and increasing mitochondrial fatty acid
oxidation.
In a Phase 1b study in patients with mild hypercholesterolemia,
treatment with VK2809 resulted in placebo-adjusted reductions in
low-density lipoprotein that exceeded 40% at high doses.
Patients also experienced significant reductions in triglycerides,
as well as the atherogenic proteins lipoprotein-a and
apolipoprotein B. Consistent with its liver- and
receptor-selective mechanism of action, treatment with VK2809 has
also demonstrated rapid reduction of liver fat in animal models of
hepatic steatosis. Further animal data have shown that VK2809
has additive cholesterol lowering activity in combination with
statins. These characteristics suggest a highly
differentiated therapeutic profile relative to existing oral
options for patients with hypercholesterolemia and fatty liver
disease, such as nonalcoholic steatohepatitis (NASH). The
potential markets for these indications are significant. In
the U.S., approximately 33% of adults, or 71 million people, have
elevated LDL cholesterol. Additionally, NASH is becoming
recognized as a leading cause of cirrhosis and liver failure and
affects an estimated 6 to 15 million Americans.
About Viking Therapeutics, Inc.
Viking Therapeutics,
Inc. is a clinical-stage biopharmaceutical company focused on the
development of novel, first-in-class or best-in-class therapies for
metabolic and endocrine disorders. The company's research and
development activities leverage its expertise in metabolism to
develop innovative therapeutics designed to improve patients'
lives. Viking has exclusive worldwide rights to a portfolio
of five therapeutic programs in clinical trials or preclinical
studies, which are based on small molecules licensed from Ligand
Pharmaceuticals Incorporated. The company's clinical programs
include VK5211, an orally available, non-steroidal selective
androgen receptor modulator, or SARM, in Phase 2 development for
the treatment and prevention of lean body mass loss in patients who
have undergone hip fracture surgery, VK2809, a small molecule
thyroid beta agonist in Phase 2 development for
hypercholesterolemia and fatty liver disease, and VK0612, a
first-in-class, orally available drug candidate in Phase 2
development for type 2 diabetes. Viking is also developing
novel and selective agonists of the thyroid beta receptor for
adrenoleukodystrophy, as well as two earlier-stage programs
targeting metabolic diseases and anemia.
Forward-Looking Statements
This press release
contains forward-looking statements regarding Viking Therapeutics,
including statements about Viking's expectations regarding its
development activities, timelines and milestones, as well as the
company's goals and plans regarding VK2809. Forward-looking
statements are subject to risks and uncertainties that could cause
actual results to differ materially and reported results should not
be considered as an indication of future performance. These risks
and uncertainties include, but are not limited to: risks associated
with the success, cost and timing of Viking's product candidate
development activities and clinical trials; and risks regarding
regulatory requirements, among others. These forward-looking
statements speak only as of the date hereof. Viking disclaims
any obligation to update these forward-looking statements.
Follow Viking on Twitter @Viking_VKTX.
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SOURCE Viking Therapeutics, Inc.