Palisade Bio announces data from two ex vivo studies of PALI-2108

Palisade Bio (PALI) announced the presentation of data from two translational studies demonstrating the ex vivo bioactivation of PALI-2108 in stool samples and whole blood. This orally administered, colon-specific phosphodiesterase-4 inhibitor prodrug is in development for patients with ulcerative colitis. The poster titled “Colonic Bioactivation and Potent TNFalpha Inhibition of PALI-2108 in Human Clinical Studies: A Promising PDE4 Inhibitor Prodrug for the Oral Treatment of Ulcerative Colitis.” Key Highlights: PALI-2108 was successfully bioactivated into its active form, PALI-0008, in stool samples from both normal healthy volunteers and UC patients, achieving a high conversion rate of 90.1% at 24 hours. PALI-0008 demonstrated significant inhibition of TNFalpha production in human whole blood, with an IC50 of 0.022 muM, indicating strong potency. PALI-0008 exhibited approximately a 20-fold higher potency in reducing TNFalpha production compared to apremilast, underscoring its potential efficacy. The microbiome study revealed consistent levels of beta-glucuronidase across different species and conditions, supporting the activation mechanism of PALI-2108. The consistent abundance of this enzyme suggests that PALI-2108 could be effective across diverse patient populations, including those with UC.