First Patient Dosed in Phase 2 Study of Palatin's Bremelanotide with Tirzepatide for Obesity Treatment

Palatin Technologies, Inc., a biopharmaceutical firm specializing in innovative medicines that target the melanocortin receptor system, has commenced patient dosing for their clinical study BMT-801. This Phase II trial is a randomized, double-blind, placebo-controlled study that aims to assess the safety, tolerance, and efficacy of combining Bremelanotide with Tirzepatide (a GLP-1/GIP) for obesity treatment. The study is registered under ClinicalTrials.gov Identifier: NCT06565611.

Carl Spana, Ph.D., the President and CEO of Palatin, expressed enthusiasm about the initiation of patient dosing and the interest shown by both patients and physicians in this study. He noted that addressing obesity effectively will require diverse therapeutic options employing various mechanisms of action. The MCR4 pathway is crucial in energy storage and food intake regulation, making MCR4 agonists significant in future combination therapies. Palatin is advancing its novel long-acting peptide and small molecule compounds as potential components of these combinations.

Dr. Spana highlighted the rapid growth and effectiveness of GLP-1 agonists in obesity treatment. However, he pointed out that 67% of patients discontinue their use within the first year due to side effects and a plateau in effectiveness, often leading to weight regain. Emerging data suggest that combining an MCR4 agonist with incretin therapies like Tirzepatide may produce enhanced weight loss effects with better-tolerated doses.

The BMT-801 study will enroll up to 60 patients across four sites in the United States. The primary objective is to demonstrate the safety and improved efficacy of co-administering Bremelanotide with Tirzepatide for weight reduction. Initially, patients will receive Tirzepatide-only for four weeks to confirm eligibility before being randomized into one of four treatment regimens. Multiple safety and efficacy assessments will be conducted to evaluate Bremelanotide's effectiveness in treating general obesity, both as a stand-alone treatment and in combination with GLP-1/GIP therapy.

Enrollment for the Phase II study is expected to be completed by the third quarter of 2024, with topline results anticipated in the first quarter of 2025.

Melanocortin 4 receptor (MCR4) agonists have shown promise in obesity treatment. Genetic studies have identified MCR4 in the hypothalamus as a central player in appetite regulation. Mutations in the MCR4 pathway can lead to overeating, reduced energy expenditure, and early-onset obesity. These mutations are linked to several rare genetic obesity disorders. MCR4 agonists, like α- and β-melanocyte-stimulating hormones, promote satiety by countering the appetite-stimulating effects of endogenous antagonists, such as Agouti-related peptide and neuropeptide Y. Targeting MCR4 is, therefore, a promising strategy for obesity treatments.

The melanocortin receptor (MCR) system affects various physiological processes, including inflammation, immune responses, metabolism, food intake, and sexual function. There are five known melanocortin receptors (MCR1 through MCR5). Modulating these receptors with specific agonists or antagonists can have significant medical effects. Many tissues and immune cells express melanocortin receptors, which allows for the activation of natural pathways to resolve disease inflammation.

Obesity, defined as a BMI of 30 kg/m² or higher, is a growing global health issue. It is associated with increased mortality and various serious health conditions such as hypertension, high cholesterol, type 2 diabetes, coronary heart disease, stroke, and certain cancers. Obesity reduces the quality of life and places a significant economic burden on healthcare systems. In the United States, about 42% of adults and one in five teens (ages 12-19) are affected by obesity.

Palatin Technologies focuses on developing first-in-class medicines that modulate the melanocortin receptor systems, targeting diseases with significant unmet medical needs and commercial potential. Their strategy involves developing products and forming marketing collaborations with industry leaders to maximize commercial success.