Palisade Bio announced the successful completion of its analysis to determine the effects of bioactivated PALI-2108 on TNF-alpha production in a whole blood assay. PALI-2108 is Palisade’s orally administered, locally acting, colon-specific phosphodiesterase-4 inhibitor prodrug in development for patients affected by UC. Findings from the study demonstrated that PALI-2108 exhibited efficacy in inhibiting TNF-alpha production induced by LPS in this ex-vivo peripheral whole blood assay. Pre-treatment of human whole blood samples with bioactivated PALI-2108 resulted in a significant reduction in LPS-induced TNF-alpha production compared to non-pretreated samples. Specifically, the Company’s proprietary PDE4 inhibitor, shown to be released by the local bioconversion of PALI-2108 prodrug in the colon, demonstrated a mean IC50 for TNF-alpha inhibition of 0.022 microM, compared to 0.41 microM for apremilast, showcasing its potent anti-inflammatory activity. The study was conducted in collaboration with Paraza Pharma, Inc based in Montreal, QC.
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