Palisade Bio, Inc. announced that the Canadian Intellectual Property Office (CIPO) has issued a Notice of Allowance for patent application number 3,174,137 titled, ?Gut Microbiota Bioactivated PDE4 Inhibitor Precursors.? This patent covers the composition of PALI-2108, the Company?s orally administered, locally acting colon-specific Phosphodiesterase-4 (PDE4) inhibitor prodrug in development for patients affected by Ulcerative Colitis (UC). The allowed patent claims cover the proprietary composition of PALI-2108.

In preclinical studies, PALI-2108 demonstrated promising outcomes. In a DSS-induced UC mouse model, researchers observed a significant reduction in disease activity index (DAI) score over time compared to the control group. Notably, body weight loss was attenuated in specific dosage groups, showcasing the potential for targeted efficacy.

PALI-2108?s unique design, incorporating a galactose-derived sugar moiety, allows for minimal absorption until cleaved by the colonic bacterium enzyme ß-glucuronidase. This feature ensures localized bioactivation, leading to colon-specific distribution with limited systemic exposure, as confirmed by a tissue distribution study. Palisade continues to advance PALI-2108 for the treatment of moderate-to-severe UC toward a Phase 1 clinical study, expected to be initiated before the end of 2024.