EYD-001 / EydisBio - LARVOL DELTA

Design and development of small molecule kinase inhibitors targeting TAK1 for inflammatory diseases | Poster Board #1190 (ACS-Fall 2026) - "The optimized compounds demonstrated strong TAK1 inhibition, outperforming the known inhibitor Takinib and Tuspetinib. In macrophage-based assays, the lead candidates effectively suppressed pro-inflammatory cytokines, including TNF-α and IL-6, with submicromolar IC50 values, showing markedly improved activity compared to the reference inhibitor HS-276. Following evaluation of pharmacokinetic properties and safety profiles, including cardiotoxicity assessment, these compounds are being advanced for in vivo validation in an arthritis mouse model. Overall, these findings highlight imidazothiadiazole-based TAK1 inhibitors as promising candidates for the development of new anti-inflammatory therapeutics"

Cardiovascular • Immunology • Inflammation • IL6 • TNFA

Design and development of small molecule kinase inhibitors targeting TAK1 for inflammatory diseases | Poster Board #1755 (ACS-Fall 2026) - "The optimized compounds demonstrated strong TAK1 inhibition, outperforming the known inhibitor Takinib and Tuspetinib. In macrophage-based assays, the lead candidates effectively suppressed pro-inflammatory cytokines, including TNF-α and IL-6, with submicromolar IC50 values, showing markedly improved activity compared to the reference inhibitor HS-276. Following evaluation of pharmacokinetic properties and safety profiles, including cardiotoxicity assessment, these compounds are being advanced for in vivo validation in an arthritis mouse model. Overall, these findings highlight imidazothiadiazole-based TAK1 inhibitors as promising candidates for the development of new anti-inflammatory therapeutics"

Cardiovascular • Immunology • Inflammation • IL6 • TNFA

Pharmacological inhibition of transforming growth factor-beta-activated kinase 1 (TAK1) in a murine model of metabolic dysfunction-associated steatotic liver disease (EASL 2026) - "TAK1 inhibition by HS-276 was well tolerated in a murine model of MASLD, contrasting our previous findings from genetic models. Our data suggest an attenuation of liver injury and favourable metabolic effects, highlighting the potential of TAK1 inhibition for the treatment of MASLD."

Preclinical • Fibrosis • Hepatology • Immunology • Inflammation • Liver Failure • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Respiratory Diseases • Scleroderma • Systemic Sclerosis

Molecular Dynamics Study of the Binding of Cationic, Anionic, and Neutral Luminescent Conjugated Ligands to the Alzheimer Folds of Aβ(1-42) and Tau Fibrils. (PubMed, Chembiochem) - "The binding of the anionic ligands (multiple localized negative charges) to fibrils is primarily driven by Coulombic forces, whereas the binding of the neutral HS-276 and cationic bTVBT4 (single delocalized positive charge) is governed by Lennard-Jones interactions. This highlights the influence of charges on binding, providing insights for the design of future ligands targeting Aβ(1-42) and tau fibrils."

Journal • Alzheimer's Disease • CNS Disorders

Pharmacological inhibition of transforming growth factor-β activated kinase 1 (TAK1) prevents chemotherapy induced peripheral neuropathy (CIPN). (PubMed, J Pain) - "In the paclitaxel and oxaliplatin CIPN mouse model, administration of HS-276 significantly reduced mechanical allodynia comparable to gabapentin. PERSPECTIVE: This manuscript demonstrates the therapeutic potential of TAK1-targeted therapies for the treatment of chemotherapy-induced peripheral neuropathy (CIPN). This new treatment has the potential to protect CIPN patients from development of debilitating and dose-limiting CIPN-associated pain, and allow patients to remain on life-saving chemotherapeutic treatments for longer."

IO biomarker • Journal • Neuralgia • Oncology • Pain • Peripheral Neuropathic Pain • IL1B • IL6 • TLR4

A Dual Inhibitor of TAK1 and MAP4K2, NG25, Suppresses Cytokine-driven Inflammation in Juvenile Idiopathic Arthritis Synovial Fibroblasts (ACR Convergence 2025) - "The efficacy of NG25 was further compared with different TAK1 inhibitors (5Z-7-oxozeaenol (5Z), takinib, or HS-276). Our preliminary findings delineate NG25's potential anti-inflammatory and anti-chemotactic activities in JIASFs. These findings lay a foundation for testing the efficacy of NG25 in animal models of JIA."

Idiopathic Arthritis • Immunology • Inflammation • Rheumatology • CDH11 • CXCL5 • CXCL8 • ICAM1 • IFNG • IL1B • IL6 • LY6G6D • MMP3 • PDPN • PTGS2 • TNFA • VCAM1

Inhibition of TAK1 as a novel analgesic for chemotherapy induced peripheral neuropathy (NeuPSIG 2025) - "Furthermore, in the paclitaxel mouse model of CIPN, orally administered EYD-001 was able to prevent the onset of mechanical allodynia, with effects comparable to those observed with gabapentin. These findings underscore the potential of TAK1 inhibitors as a novel therapeutic approach for CIPN. The development of small molecule TAK1 inhibitors for the treatment of CIPN could provide a new class of drugs with improved efficacy and safety profiles compared to current treatments improving the quality of life for individuals undergoing neurotoxic chemotherapies."

CNS Disorders • Pain • TGFB1 • TLR4

Effect of compounds targeting different mechanisms on LPS-induced neuroinflammation (Neuroscience 2024) - "These included HS-276 (TAK1), GSK2982772 (RIPK1), MCC950 (NLRP3), CA-4948 (IRAK4), Tofacitinib citrate (JAK), Psilocybin (5HT2A), and TAK-242 (TLR4). Our data show that TAK-242 inhibits the LPS-induced increase in cytokine mRNA and protein expression in a similar manner to Dexa. TAK-242 is a TLR4 inhibitor which is a known receptor for LPS so this response further validates this in vivo LPS model as a useful approach for testing the efficacy of novel anti-inflammatory agents against neuroinflammation but may only be useful for agents either targeting TLR-4 or its immediate downstream components."

Alzheimer's Disease • CNS Disorders • Parkinson's Disease • IFNG • IL1B • IL6 • IRAK4 • NLRP3 • RIPK1 • TLR4 • TNFA

EydisBio Receives FDA Orphan Drug Designation for TAK1 Inhibitor for the Treatment of Systemic Sclerosis (PRNewswire) - "EydisBio, Inc. is pleased to announce that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation to EYD-001, its highly selective and potent, orally bioavailable TAK1 inhibitor for the treatment of systemic sclerosis."

Orphan drug • Immunology • Systemic Sclerosis