Obesity and Diabetes

Obesity is a multifactorial condition with numerous biochemical components relating to satiety (feeling full), energy utilization and homeostasis. A number of different metabolic and hormonal pathways are being evaluated by companies around the world in efforts to develop better treatments for obesity. Scientific research has established that melanocortin receptors have a role in eating behavior and energy homeostasis, and that melanocortin receptor agonists can decrease food intake and induce weight loss. Our obesity and diabetes program is based on our expertise in developing peptides specific for melanocortin receptors.

Our Lead Obesity and Diabetes Product Candidate

Our lead obesity and diabetes product candidate is a synthetic peptide we developed with the code name PL-8905. PL-8905 is a highly selective melanocortin receptor‐4 receptor (MC4r) agonist, with preclinical toxicology and CMC activities being conducted to support an IND filing and phase 1 clinical studies.

Mutations in the MC4r are one of the most prevalent forms of monogenetic obesity in humans.   The MC4r and associated signaling pathways play a key role in regulating food intake and energy homeostasis.  Extensive academic research supports MC4r as one of the best validated drug targets for obesity.  As part of Palatin’s MC4r agonist program, compound libraries consisting of highly selective MC4r compounds have been developed and a detailed evaluation process was conducted to select potential lead development candidates. In addition, key structure/function relationships have been defined and incorporated into both peptide and oral small molecule compound development.

Palatin has conducted two clinical trials with an MC4r agonist in obese subjects.  These studies provide further validation of MC4r as a target and gave Palatin a better understanding of PK/PD relationships and magnitude of treatment effect.  In both studies significant reductions in food intake and corresponding weight loss occurred, with the results highly instructive in guiding further clinical development of an MC4r agonist.

What is the Development Status of PL-8905?

PL-8905 has demonstrated significant efficacy in preclinical obesity models with positive effects on weight loss and glucose regulation. Animal models have also shown a synergistic effect with GLP-1 in weight loss and glucose regulation.  The drug has demonstrated minimal effect on blood pressure and CNS penetration, with excellent chemical and metabolic stability.