Equillium Announces Preclinical Data From New Orally Deliverable Multi-Cytokine Inhibitor In Presentation At The 18th Annual Peptide Therapeutics Symposium

Author: Benzinga Newsdesk | October 16, 2023 08:16am

Equillium Inc. (NASDAQ:EQ), a clinical-stage biotechnology company focused on developing novel therapeutics to treat severe autoimmune and inflammatory disorders, today announced a presentation at the 18th Annual Peptide Therapeutics Symposium highlighting EQ302, a second generation orally deliverable multi-cytokine inhibitor in development to target IL-15 and IL-21. The symposium, bringing together leaders in peptide research from academia and industry to focus on advances in core technology pertinent to peptide-based drug discovery and therapeutic candidate development, is taking place October 16 and 17 at the Scripps Seaside Forum in San Diego, California.

Title: Peptide Stapling for Better Stability & Oral Delivery

Presenting Author: Adrian J. Giovannone, Ph.D., Associate Director, Translational Science & Early Development at Equillium

Date and Time: Live for the entire conference beginning at 9:30 am PT on Monday, October 16

The presentation outlines the origins of EQ302 from its parent peptide, EQ102, which was originally modeled from the D-helix of the IL-2 family of cytokines and binds directly to CD132 to inhibit the signaling of IL-15 and IL-21. Stable peptide derivatives of EQ102, including EQ302, are being developed by adding hydrocarbon staples to confer proteolytic resistance and increase stability in the gastrointestinal (GI) tract while retaining cytokine inhibitory properties​, making it a potential candidate for clinical testing in a variety of GI diseases via oral administration.

EQ302 was administered to mice via oral delivery in a pre-clinical formulation designed to enhance permeability of the intestine. Following oral administration to mice challenged with human IL-15, small intestinal tissue was harvested and shown to contain significant amounts of EQ302. To demonstrate the local efficacy of the peptide, IL-15-induced Interferon-gamma (IFNγ) levels within the intestinal tissue were measured and shown to be significantly decreased in EQ302-treated animals versus vehicle control animals.

The data illustrates that:

• Adding hydrocarbon staples to a peptide can confer increased stability in the GI tract while retaining its cytokine inhibitory properties​.
• Utilizing a pre-clinical formulation for enhanced epithelial permeability, EQ302 achieved meaningful concentration levels for localized cytokine inhibition in the small intestine.
• EQ302 delivered to mice via oral gavage can inhibit IL-15-induced IFNγ transcription locally in the GI tract indicating potential utility for Celiac Disease and inflammatory bowel disease.​

The oral presentation is available on the Presentations page of Equillium's website, under the Multi-Cytokine Inhibition tab.

About Multi-Cytokine Platform and EQ101, EQ102 & EQ302

Our proprietary multi-cytokine platform generates rationally designed composite peptides that selectively block key cytokines at the shared receptor level targeting pathogenic cytokine redundancies and synergies while preserving non-pathogenic signaling. This approach is expected to avoid the broad immuno-suppression and off-target safety liabilities that may be associated with other therapeutic classes, such as Janus kinase inhibitors. Many immune-mediated diseases are driven by the same combination of dysregulated cytokines, and we believe identifying the key cytokines for these diseases will allow us to target and develop customized treatment strategies for multiple autoimmune and inflammatory diseases.

Current platform assets include EQ101, a first-in-class, selective, tri-specific inhibitor of IL-2, IL-9, and IL-15 for intravenous and subcutaneous delivery; EQ102, a first-in-class, selective, bi-specific inhibitor of IL-15 and IL-21 for subcutaneous delivery; EQ302, in development as a first-in-class, selective, bi-specific inhibitor of IL-15 and IL-21 for oral delivery.

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