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Multi-Cytokine Inhibitor Platform

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 provides multi-cytokine inhibition at the receptor level and is expected to avoid the broad immuno-suppression and off-target safety liabilities of JAK 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 diseases.

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Most MABs are targeted against one cytokine and do not address the disease pathology adequately if more than one cytokine is implicated in the disease process. JAK inhibitors lack specificity and inhibit the JAK/STAT signaling pathway that is utilized by all the cytokines regardless of their involvement in the disease. As the result, this class of compounds are often associated with serious side effects. Our peptides selectively block multiple disease driving cytokines while maintaining the healthy immune balance through the normal function of other family members.

cytokine diagram

Equillium's Multi-Cytokine Inhibitors Block the Pockets in the Common Receptor

EQ101 is a first-in-class, tri-specific inhibitor of IL-2, IL-9 and IL-15, three inflammatory cytokines implicated in multiple diseases. It selectively blocks those three key pathogenic cytokines while preserving non- pathogenic signaling related to IL-4, IL-7 and IL-21 and has demonstrated clinical proof-of-concept as a novel cytokine inhibitor through a completed Phase 1/2 study in cutaneous T cell lymphoma (CTCL), a dermato-oncology indication. EQ101 achieved its primary objective of safety and tolerability and showing clinically meaningful improvements in SWAT scores (modified severity-weighted assessment tool).

EQ101 was also shown to be well tolerated with a favorable safety profile with no drug-related SAEs and no dose-limiting toxicities. It is now Phase 2 ready in alopecia areata, a dermatological autoimmune disorder, and is Phase 2/3 ready in CTCL with open U.S. INDs for each indication, with an orphan designation for CTCL in the U.S. and Europe. EQ101 is currently formulated for intravenous administration, with subcutaneous formulation development underway. Equillium is planning to initially focus development of EQ101 in patients suffering from alopecia areata, where there are currently no drugs approved.

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EQ102 is a first-in-class, selective inhibitor of IL-15 and IL-21. It has undergone substantial translational work supporting its potential use as a treatment for various gastrointestinal diseases and is Phase 1 ready for a study planned to include a proof-of-concept evaluation in patients with celiac disease, an immune disorder related to gluten exposure. The high degree of selectivity for IL-15 and IL-21 inhibition aligns well with the demonstrated key involvement of these two cytokines that work synergistically in driving the pathology in celiac disease and other inflammatory gut and hepatic disorders.

EQ102 is currently formulated for subcutaneous administration where it is positioned to address an unmet need in patients experiencing symptoms despite attempts to maintain a gluten-free diet.