Palisade Bio Reports Phase 1a/b Data for Colon-Targeted IBD Drug PALI-2108
Palisade Bio has announced new phase 1a/b clinical trial results for its investigational PDE4 inhibitor prodrug, PALI-2108, designed for treating inflammatory bowel disease. The data demonstrates successful colon-targeted delivery, with delayed activation in the ileocolonic region and high tissue-to-plasma exposure ratios. Key findings indicate that the active metabolite, PALI-0008, achieves steady-state concentrations within 48 hours and maintains levels above the IC90 threshold throughout the dosing interval, supporting a once-daily regimen. The drug showed selective suppression of inflammatory and fibrotic pathways, such as JAK–STAT and NF‑κB, specifically in colonic tissue rather than peripheral blood. Biomarker analysis revealed decreased mucosal PDE4B expression and significant reductions in faecal calprotectin, aligning with previous reports of clinical remission in ulcerative colitis patients. Mitch Jones, President and Chief Medical Officer, emphasized that these pharmacokinetic profiles compare favorably to existing systemic PDE4 inhibitors. These results reinforce the potential of PALI-2108 as a next-generation therapy, highlighting its ability to provide continuous target inhibition with localized activity, thereby minimizing systemic side effects while maximizing therapeutic efficacy in the intestinal mucosa.
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Palisade Bio Reports Phase 1a/b Data for Colon-Targeted IBD Drug PALI-2108
Palisade Bio has announced new phase 1a/b clinical trial results for its investigational PDE4 inhibitor prodrug, PALI-2108, designed for treating inflammatory bowel disease. The data demonstrates successful colon-targeted delivery, with delayed activation in the ileocolonic region and high tissue-to-plasma exposure ratios. Key findings indicate that the active metabolite, PALI-0008, achieves steady-state concentrations within 48 hours and maintains levels above the IC90 threshold throughout the dosing interval, supporting a once-daily regimen. The drug showed selective suppression of inflammatory and fibrotic pathways, such as JAK–STAT and NF‑κB, specifically in colonic tissue rather than peripheral blood. Biomarker analysis revealed decreased mucosal PDE4B expression and significant reductions in faecal calprotectin, aligning with previous reports of clinical remission in ulcerative colitis patients. Mitch Jones, President and Chief Medical Officer, emphasized that these pharmacokinetic profiles compare favorably to existing systemic PDE4 inhibitors. These results reinforce the potential of PALI-2108 as a next-generation therapy, highlighting its ability to provide continuous target inhibition with localized activity, thereby minimizing systemic side effects while maximizing therapeutic efficacy in the intestinal mucosa.
PharmaTimes