LA JOLLA, Calif. / Oct 16, 2023 / Business Wire / 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.

About Equillium

Equillium is a clinical-stage biotechnology company leveraging a deep understanding of immunobiology to develop novel therapeutics to treat severe autoimmune and inflammatory disorders with high unmet medical need. The company’s pipeline consists of the following novel first-in-class immunomodulatory assets targeting immuno-inflammatory pathways. EQ101: a tri-specific cytokine inhibitor that selectively targets IL-2, IL-9, and IL-15; currently under evaluation in a Phase 2 proof-of-concept clinical study of patients with alopecia areata. EQ102: a bi-specific cytokine inhibitor that selectively targets IL-15 and IL-21; currently under evaluation in a Phase 1 first-in-human clinical study to include healthy volunteers and celiac disease patients. EQ302, in development as a first-in-class, selective, bi-specific inhibitor of IL-15 and IL-21; currently in pre-clinical development. Itolizumab: a monoclonal antibody that targets the CD6-ALCAM signaling pathway which plays a central role in the modulation of effector T cells; currently under evaluation in a Phase 3 clinical study of patients with acute graft-versus-host disease (aGVHD) and a Phase 1b clinical study of patients with lupus/lupus nephritis. Equillium acquired rights to itolizumab through an exclusive partnership with Biocon Limited and has entered a strategic partnership with Ono Pharmaceutical Co., Ltd. For the development and commercialization of itolizumab under an option and asset purchase agreement.

For more information, visit www.equilliumbio.com.

Forward Looking Statements

Statements contained in this press release regarding matters that are not historical facts are “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995. Forward-looking statements may be identified by the use of words such as “anticipate”, “believe”, “could”, “continue”, “expect”, “estimate”, “may”, “plan”, “outlook”, “future” and “project” and other similar expressions that predict or indicate future events or trends or that are not statements of historical matters. Because such statements are subject to risks and uncertainties, many of which are outside of Equillium’s control, actual results may differ materially from those expressed or implied by such forward-looking statements. Risks that contribute to the uncertain nature of the forward-looking statements include: Equillium’s ability to execute its plans and strategies; risks related to performing clinical and pre-clinical studies; whether the results from clinical and pre-clinical studies will validate and support the safety and efficacy of Equillium’s product candidates. These and other risks and uncertainties are described more fully under the caption "Risk Factors" and elsewhere in Equillium's filings and reports, which may be accessed for free by visiting the Securities and Exchange Commission’s website at www.sec.gov and on Equillium’s website under the heading “Investors.” Investors should take such risks into account and should not rely on forward-looking statements when making investment decisions. All forward-looking statements contained in this press release speak only as of the date on which they were made. Equillium undertakes no obligation to update such statements to reflect events that occur or circumstances that exist after the date on which they were made, except as required by law.