- High selectivity for MC4R significantly reduces potential for
skin pigmentation
- MC4R is a well-validated target for treating obesity
- Clinical studies with highly selective MC4R agonists
targeted to commence in calendar year 2025
CRANBURY, N.J., Oct. 23,
2024 /PRNewswire/ -- Palatin Technologies, Inc.
(NYSE American: PTN), a biopharmaceutical company developing
first-in-class medicines based on molecules that modulate
the activity of the melanocortin receptor system, presented a
poster titled "Structural Modification Allows the Removal of
Melanocortin Receptor 1 Agonism From Melanocortin Receptor 4
Agonists," at the 19th Annual Peptide Therapeutics
Symposium held October 22-23, 2024 in
person and virtually in La Jolla,
California. John H. Dodd,
Ph.D., lead author and Senior Vice President Research &
Development for Palatin Technologies, presented the poster. A copy
of the poster can be found on Palatin's website www.palatin.com
under Resources.
MC4R plays a significant role in eating behavior and how our
bodies manage energy. Palatin has identified the specific
structural parts of a peptide that are responsible for MC1R
agonism, which causes increased skin pigmentation, found in
nonselective MC4R agonists. Palatin modified these structural parts
to boost and optimize MC4R activity while reducing MC1R activity,
resulting in the discovery of new highly selective MC4R agonists
that significantly reduce the potential for skin pigmentation. An
MC4R agonist with high selectivity for the MC4R would not activate
MC1R and potentially eliminate or significantly reduce skin color
changes.1,2
"These novel highly selective MC4R agonists, which potentially
eliminate adverse effects such as skin pigmentation, represents a
meaningful step forward in MC4R based therapeutics for a variety of
indications, including general obesity, genetically linked obesity,
and weight loss maintenance," said Carl
Spana, Ph.D., President and Chief Executive Officer of
Palatin. "We will combine these peptides with our proprietary
technology for extending biological half-life for once-weekly
dosing. We look forward to beginning clinical development in
calendar 2025."
GLP-1 agonists to treat obesity are highly effective, but data
shows that 67% of patients discontinue use in the first year due to
side effects and a plateau effect. This often results in a rebound
effect with patients gaining significant weight back. Safe,
effective, and consistent treatment and maintenance of weight loss
requires multiple therapeutic options with differing mechanisms of
action. The MC4R pathway plays a key role in the regulation of
energy storage and food intake. MC4R agonists, especially highly
selective MC4R agonists being developed by Palatin, could
potentially play a vital role for treating obesity as monotherapy
and/or combination therapy.
Palatin is currently conducting a Phase 2 clinical trial in
obese patients with the MC4R agonist bremelanotide in combination
with tirzepatide with results expected in 1Q 2025.
About the Peptide Therapeutics Symposium
The Peptide
Therapeutics Symposium was established in 2005 as an annual
scientific meeting that brings together world leaders in peptide
research from academia and the biopharmaceutical industries. The
meeting is focused on advances in core technology pertinent to
peptide-based drug discovery and therapeutic candidate
development.
About Melanocortin 4 Receptor Agonists Effect on
Obesity
Genetic analysis has identified the melanocortin 4
receptor (MC4R) of the paraventricular nucleus of the hypothalamus
as playing a central role in appetite regulation. Genetic mutations
that inhibit signaling in the MC4R pathway lead to hyperphagia,
decreased energy expenditure and early-onset obesity; such
mutations have been identified as the cause of several rare genetic
obesity disorders. Agouti-related peptide is an endogenous
antagonist of the MC4R that works with neuropeptide Y to stimulate
appetite, whereas MC4R agonists such as α- and
β-melanocyte-stimulating hormone promote satiety. Agonism of the
MC4R therefore represents an attractive target for potential
obesity treatments.
About Melanocortin Receptor Agonists
The melanocortin
receptor ("MCR") system has effects on inflammation, immune system
responses, metabolism, food intake, and sexual function. There are
five melanocortin receptors, MC1R through MC5R. Modulation of these
receptors, through use of receptor-specific agonists, which
activate receptor function, or receptor-specific antagonists, which
block receptor function, can have medically significant
pharmacological effects.
Many tissues and immune cells located in the eye (and other
places, for example the gut and kidney) express melanocortin
receptors, empowering our opportunity to directly activate natural
pathways to resolve disease inflammation.
About Obesity
Obesity, which is defined as a body mass
index (BMI) ≥30 kg/m2, represents a rising worldwide public health
concern. Obesity is associated with an increased risk of overall
mortality and serious health conditions, including high blood
pressure, high cholesterol, type 2 diabetes, coronary heart
disease, stroke and certain cancers. Health-related quality of life
is significantly lower among adults with obesity, and obesity is
associated with increased health care resource use and high
economic burden. Safe and effective obesity treatments therefore
remain a critical unmet need. The global increase in the prevalence
of obesity is a public health issue that has severe cost
implications for healthcare systems. In the United States, about 42% of adults live
with obesity, and one out of five teens between the ages of 12-19
live with obesity.
About Palatin
Palatin is a biopharmaceutical company
developing first-in-class medicines based on molecules that
modulate the activity of the melanocortin receptor systems, with
targeted, receptor-specific product candidates for the treatment of
diseases with significant unmet medical need and commercial
potential. Palatin's strategy is to develop products and then form
marketing collaborations with industry leaders to maximize their
commercial potential. For additional information regarding Palatin,
please visit Palatin's website at www.Palatin.com and follow
Palatin on Twitter at @PalatinTech.
Forward-looking Statements
Statements in this press
release that are not historical facts, including statements about
future expectations of Palatin Technologies, Inc., such as
statements about Palatin products in development, clinical trial
results, potential actions by regulatory agencies including the
FDA, regulatory plans, development programs, proposed indications
for product candidates, and market potential for product candidates
are "forward-looking statements" within the meaning of Section 27A
of the Securities Act of 1933, Section 21E of the Securities
Exchange Act of 1934 and as that term is defined in the Private
Securities Litigation Reform Act of 1995. Palatin intends that such
forward-looking statements be subject to the safe harbors created
thereby. Such forward-looking statements involve known and unknown
risks, uncertainties and other factors that could cause Palatin's
actual results to be materially different from its historical
results or from any results expressed or implied by such
forward-looking statements. Palatin's actual results may differ
materially from those discussed in the forward-looking statements
for reasons including, but not limited to, results of clinical
trials, regulatory actions by the FDA and other regulatory and the
need for regulatory approvals, Palatin's ability to fund
development of its technology and establish and successfully
complete clinical trials, the length of time and cost required
to complete clinical trials and submit applications for regulatory
approvals, products developed by competing pharmaceutical,
biopharmaceutical and biotechnology companies, commercial
acceptance of Palatin's products, and other factors discussed in
Palatin's periodic filings with the Securities and Exchange
Commission. Palatin is not responsible for updating events that
occur after the date of this press release.
Palatin Technologies® is a registered trademark of
Palatin Technologies, Inc.
1 Yeo GSH, et al. Mol Metab.
2021;48:101206.
2 Fatima MT, et al. Diabetes Obes Metab.
2022;24(4):583-598.
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