– Preclinical data demonstrated PALI-2108 to be safe and well tolerated
– PALI-2108 is orally delivered and colon activated allowing for local activity with low systemic exposure
– Company advancing PALI-2108 for the treatment of moderate-to-severe ulcerative colitis (UC) toward Phase 1 clinical study, expected to commence in 2024
Carlsbad, CA, Jan. 29, 2024 — Palisade Bio, Inc. (Nasdaq: PALI) (“Palisade” or the “Company”), a biopharmaceutical company focused on developing novel therapeutics for serious chronic gastrointestinal (GI) diseases, today announced the presentation of positive preclinical data of its lead asset, PALI-2108 at the Crohn’s & Colitis Congress, which was held on January 25-27, 2024 in Las Vegas, NV.
The preclinical data was presented in a poster titled, Local Bioactivation and Efficacy of PALI-2108: A Promising PDE4 Inhibitor Prodrug for Ulcerative Colitis Treatment. PALI-2108 is the Company’s orally administered, locally acting colon-specific phosphodiesterase-4B (PDE4B) inhibitor prodrug in development for patients affected by moderate-to-severely active ulcerative colitis (UC). The poster is available on the Scientific Publications page of the Company’s website.
Mitchell Jones, M.D., Ph.D., Chief Medical Officer of Palisade Bio, commented, “PALI-2108 continues to demonstrate promise as a novel therapy for UC, with colon-selective bioactivation, an expanded therapeutic window, reduced CNS toxicity, potent PDE4 inhibitory activity, and impressive efficacy in preclinical models. We are pleased with our growing body of evidence, including support for a precision medicine approach and the selection of potential responders, which validate the continued development of this program. We are working diligently to launch our Phase 1 study later this year, and we are eager to continue to gain experience on the potential of this groundbreaking PDE4 inhibitor prodrug therapy. The journey ahead holds great promise for advancing UC treatment, and we are committed to making a meaningful impact for patients.”
The results presented at the Crohn’s and Colitis Foundation include several preclinical studies of PALI-2108, a novel oral PDE4 inhibitor prodrug designed for the treatment of ulcerative colitis (UC). The Company’s research has focused on addressing the limitations of current PDE4 inhibitors, such as CNS toxicity and systemic distribution, which often lead to therapy discontinuation.
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 β-glucuronidase. This feature ensures localized bioactivation, leading to colon-specific distribution with limited systemic exposure, as confirmed by a tissue distribution study. The colon/plasma AUC ratio exceeding 200 further highlights PALI-2108’s preference for the colon.
In addition, the Company’s research demonstrates colon-selective bioactivation in oxazolone colitis-induced mice, negligible plasma levels in duodenal and ileal tissue, and comparable target engagement with other PDE4 inhibitors. As well, a tolerated dose study in dogs revealed no CNS toxicity or emesis over effective doses, addressing a critical concern associated with oral administration.
“PALI-2108 is emerging as a promising candidate for UC therapy, offering localized bioactivation, expanded therapeutic window, and potent PDE4 inhibitory activity. We believe this innovative approach has the potential to revolutionize UC treatment and enhance patient outcomes,” added Dr. Jones.
In summary, results of the Company’s preclinical studies showed that PALI-2108 demonstrated:
- Local bioactivation;
- Colon-specific distribution;
- Similar target engagement to other PDE4 inhibitors;
- Dose-dependent efficacy in a mouse UC model; and
- No systemic toxicity in dogs and large therapeutic window due to local activation.
Inflammatory bowel disease (IBD) represents a multi-billion-dollar market opportunity in need of innovative approaches, with current therapies achieving a clinical remission rate of less than 20% on average.
About Palisade Bio
Palisade Bio is a biopharmaceutical company focused on developing novel therapeutics for serious chronic gastrointestinal diseases. The Company believes that by using a targeted approach with its novel therapeutics it will transform the treatment landscape. For more information, please go to www.palisadebio.com.
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Source: Palisade Bio