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Palatin initiates study of bremelanotide for the treatment of obesity

Palatin Technologies has begun a Phase 2 clinical study of bremelanotide for the treatment of obesity. The clinical study will evaluate the safety and efficacy of bremelanotide, a melanocortin 4 receptor (MC4R) agonist, co-administered with tirzepatide (GLP-1/GIP) in patients with obesity. The primary endpoint of the trial is to demonstrate the safety and increased efficacy of the co-administration of bremelanotide with tirzepatide on reducing body weight. Topline data results are expected by the end of calendar year 2024.

"Although GLP-1 agonists are currently the standard of care treatment for obesity, data shows that 67% of patients discontinue use due to side effects and a plateau effect in the first year," said Dr Carl Spana, CEO and President of Palatin. "We believe co-administering an MC4R agonist with a GLP-1 agonist will achieve significant weight loss at lower doses, with improved tolerability and quality of life for these patients. These beliefs are supported by our published preclinical data and multiple clinical studies demonstrating statistically significant effects on reducing food intake and weight loss in obese patients."


The clinical study, titled ‘BMT-801: A Phase II, Randomized, Double-Blind, Placebo-Controlled, Clinical Study Investigating the Safety, Tolerability, and Effectiveness of the Co-Administration of Bremelanotide with Tirzepatide (GLP-1/GIP) for the Treatment of Obesity’, has FDA clearance. The study is designed to enrol up to 60 patients who are actively on tirzepatide at five trial sites in the US. Patients will undergo multiple assessments of safety and efficacy to help profile the effectiveness of bremelanotide in treating general obesity as a stand-alone treatment or in conjunction with GLP-1/GIP therapy.


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.


"The MC4R pathway biology is clear and strong. It regulates hunger, caloric intake, energy expenditure and, consequently, body weight. Obesity has a tremendous adverse impact on patients, their families, and across the medical community,” Spana added. With significant experience and an extensive intellectual property portfolio in the design and development of MC4R agonists, Palatin continues to develop novel and highly selective MC4R agonists, including oral small molecule MC4R agonists, for the potential treatment of multiple metabolic indications, including certain rare genetic diseases of obesity."

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