- 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.
SOURCE Palatin Technologies, Inc.
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