UC Candidate Therapy PL-8177 Shows Successful Delivery to Lower GI Tract

UC Candidate Therapy PL-8177 Shows Successful Delivery to Lower GI Tract
Use of an oral, delayed-release formulation of the ulcerative colitis treatment candidate PL-8177 led to targeted delivery to the lower gastrointestinal tract and was well-tolerated, according to top-line results of an open-label study. Palatin Technologies’ PL-8177 binds with high selectivity to the melanocortin receptor 1 (MC1), whose levels are increased on the surface of intestinal cells in inflammatory bowel disease (IBD), kidney inflammation, and rheumatoid arthritis, among other disorders. According to the company, activation of MC1 in the colon and lower gastrointestinal tract with this investigational therapy may reduce chronic inflammatory and immune responses. PL-8177 is a radioactive-labeled (or radiolabeled), polymer-bound compound. Its delayed-release polymer formulation is intended to protect the medication until it reaches the lower gastrointestinal tract. The study included 24 participants divided into six groups of four patients each. Levels of the investigational therapy and its byproduct were measured in blood, urine, and feces samples at different timepoints following treatment with a microdose. The findings revealed that the study’s main aim was achieved, as oral administration led to favorable pharmacokinetics — the compound’s absorption, distribution, metabolism, and excretion in the body — and release of PL-8177 in the lower gastrointestinal tract. A secondary goal was also met, as PL-8177 was not systemically absorbed after oral administration. This was reflected by no detectable levels of the compound or its b
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