It is a selective melanocortin 1 receptor (MC1r) agonist peptide, which means that it is a short chain of amino acids (the building blocks of a protein) that binds to MC1r found on the cell membrane. MC1r is a hormonal receptor that plays an important role in the anti-inflammatory response.
How PL-8177 works
When PL-8177 binds to MC1r, it activates the receptor to start a cascade of events in the cell that helps reduce an inflammatory response. In many inflammatory diseases, including IBD, MC1r is upregulated, which means that the body’s cells make more of these receptors. Their abundance also makes the cells more sensitive to MC1r agonists like PL-8177.
Treatments that reduce inflammation by activating MC1r could hold an advantage over those that target other receptors, such as the glucocorticosteroid receptors. While glucocorticosteroids, such as prednisone, have powerful anti-inflammatory effects, they also have many side effects. Because medications like PL-8177 work via a different mechanism, they are not expected to have the same side effects.
Preclinical studies conducted by Palatin showed that it reduces the inflammatory response in animal models of IBD and similar diseases.
PL-8177 in clinical trials
Palatin Technologies announced in January 2018 that the U.S. Food and Drug Administration (FDA) had accepted an investigational new drug application for PL-8177 for the treatment of ulcerative colitis, a form of IBD. This means that the company can now proceed with clinical trials to test PL-8177 as a treatment for this disease.
The company expects to begin a Phase 1 trial of a single dose and multiple ascending doses of PL-8177, administered as an under-the-skin injection, later this year.
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