Efgitasialase alfa

– E-688/HLX316 is the first tumor-targeted human sialidase to enter clinical trials, designed to restore both innate and adaptive anti-tumor immunity by removing immunosuppressive sialoglycans – – Trial is being conducted in China by strategic partner Shanghai Henlius Biotech – WALTHAM, Mass.--(BUSINESS WIRE)--Palleon Pharmaceuticals, the first company to translate glycan editing science into clinical-stage therapeutics for immune modulation, today announced the first patient has been dosed in a Phase 1 clinical trial of E-688/HLX316, a first-in-class B7-H3-targeted sialidase. The study is being conducted in China by strategic collaborator Shanghai Henlius Biotech in patients with tumors prone to B7-H3 overexpression and hypersialylation, with an initial focus on platinum-resistant ovarian cancer. This milestone marks the clinical translation of a fundamentally new mechanism — glycan editing for immune modulation — grounded in the pioneering glycobiology research of Nobel laureate Carolyn Bertozzi. Tumor hypersialylation, the upregulation of sialic acid-containing glycans on the surface of cancer cells, can suppress anti-tumor immunity by activating sialic acid-dependent immune regulatory pathways. This axis of immune evasion is present across many solid tumors and correlates with poor clinical outcomes in dozens of published studies. "E-688/HLX316 is designed to enzymatically remove sialic acid from tumor cell surfaces at the site of B7-H3 overexpression, unmasking tumors to the immune system in a durable, mechanistically distinct way. This first-in-human trial is a critical step toward validating glycan editing for immune modulation as a new therapeutic paradigm across hypersialylated solid tumors,” said Jim Broderick, M.D., Chief Executive Officer and Founder of Palleon. "The protocol includes a planned expansion into platinum-resistant ovarian cancer, where high B7-H3 expression and hypersialylation provide a compelling biological rationale for this approach." About E-688/HLX316 E-688/HLX316 is generated from Palleon's EAGLE (Enzyme-Antibody Glycan-Editing) platform and combines a human sialidase enzyme with a targeting arm directed at B7-H3, a tumor antigen broadly overexpressed across solid tumors and associated with aggressive disease biology and poor prognosis. By enzymatically removing sialic acid from tumor cell surfaces, E-688/HLX316 restores immune recognition through glycan-binding receptor pathways, disrupts the immunosuppressive tumor microenvironment, and is designed to generate durable anti-tumor immune responses — activating both innate and adaptive immunity through a mechanism distinct from existing checkpoint therapies. In preclinical studies, E-688/HLX316 demonstrated tumor surface desialylation lasting more than seven days in vivo and showed improved anti-tumor activity relative to anti-PD-1 monotherapy in humanized tumor models. Phase 1 Trial Design The Phase 1 first-in-human trial will evaluate safety, tolerability, pharmacokinetics and pharmacodynamics, and preliminary anti-tumor activity of E-688/HLX316 monotherapy, comprising a Phase 1a dose escalation in B7-H3+ advanced solid tumors and Phase 1b dose expansion in platinum-resistant ovarian cancer. Palleon and Henlius intend to expand the program into additional solid tumor indications characterized by high B7-H3 expression and hypersialylation. About Palleon Pharmaceuticals Palleon Pharmaceuticals is pioneering glycan editing for immune modulation, a new approach to the treatment of autoimmune disease and cancer. Co-founded on the glycobiology research of Carolyn Bertozzi (2022 Nobel Laureate in Chemistry), Palleon's pipeline includes E-602 (Phase 2, membranous nephropathy) and E-688/HLX316 (Phase 1, advanced solid tumors). Contacts Media Contact Lauren Crociati Ten Bridge Communications lcrociati@tenbridgecommunications.com

E-688/HLX316 activates both innate and adaptive anti-tumor immunity through tumor-targeted enzymatic desialylation Initiation of a first-in-human clinical trial of E-688/HLX316 is underway in China, following IND approval granted to strategic collaborator Henlius by the National Medical Products Administration (NMPA) WALTHAM, Mass.--(BUSINESS WIRE)--Palleon Pharmaceuticals today presented preclinical data and announced the initiation of a human clinical trial for E-688/HLX316, a first-in-class B7-H3 targeted sialidase, in an oral presentation at the American Association for Cancer Research (AACR) Annual Meeting “New Drugs on the Horizon” session. The presentation, titled “ E-688/HLX316: A First-in-Class B7-H3 Targeted Sialidase for Boosting Innate and Adaptive Anti-Tumor Immunity” introduces the first ever tumor-targeted enzymatic desialylation agent to enter the clinic. Tumor hypersialylation — the upregulation of sialic acid-containing glycans on the surface of cancer cells — activates several sialic acid-dependent immune regulatory pathways that suppress anti-tumor immunity. This axis of immune evasion is present across the majority of solid tumors and correlates with poor clinical outcomes in dozens of published studies. Conventional antibodies and small molecules cannot effectively disrupt this redundant glycan-mediated immunosuppression. Palleon’s engineered human sialidase overcomes this challenge by enzymatically removing sialic acid from the tumor surface, broadly neutralizing sialic acid-mediated immune suppression. Palleon’s first-generation sialidase, E-602, established human proof-of-mechanism and a favorable tolerability pro a previous clinical trial and is now in Phase 2 development in autoimmunity. This early clinical experience helped define the additional design requirements needed for the oncology clinical setting: durable tumor-localized desialylation and direct tumor cell killing. E-688/HLX316 was engineered to satisfy both conditions, and preclinical data confirm that it extends tumor surface desialylation to more than seven days in vivo and outperforms anti-PD-1 as a single agent in humanized tumor models, enhancing both innate and adaptive anti-tumor immunity. “Tumor hypersialylation is now an addressable axis of immune evasion that is independent of PD-1/L1 biology,” said Jim Broderick, M.D., CEO and Founder of Palleon Pharmaceuticals. “Our first-generation clinical experience identified the attributes of an effective oncology sialidase and informed the design of E-688/HLX316. The preclinical package confirms the approach works as intended.” E-688/HLX316 is being evaluated in a first-in-human monotherapy trial in platinum-resistant ovarian cancer in China led by Palleon’s strategic collaborator Henlius. Palleon’s clinical roadmap includes a systematic expansion into other large cancer populations characterized by high B7-H3 expression and hypersialylation, including lung and prostate cancer. About Palleon Pharmaceuticals Palleon Pharmaceuticals is a clinical-stage biotherapeutics company developing first-in-class engineered sialidase therapies for the treatment of cancer and autoimmune disease. Co-founded on the glycobiology research of Carolyn Bertozzi (2022 Nobel laureate in Chemistry), Palleon is the first company to translate this science into human therapeutics targeting cell surface sialoglycans. Palleon’s platform has generated two clinical programs: E-602 (Phase 2, membranous nephropathy) and E-688/HLX316 (first-in-human, platinum-resistant ovarian cancer). Contacts Media Contact Lauren Crociati Ten Bridge Communications lcrociati@tenbridgecommunications.com