GB7208 / Gossamer Bio - LARVOL DELTA

Bruton's tyrosine kinase inhibition reduces disease severity in a model of secondary progressive autoimmune demyelination. (PubMed, Acta Neuropathol Commun) - "We show that late in the course of disease, EAE severity could not be reduced with a potent relapse inhibitor, FTY720 (fingolimod), indicating that disease was relapse-independent. We show similar efficacy with two small molecule inhibitors, including a novel, highly selective, central nervous system-penetrant BTK inhibitor, GB7208. These results suggest that through lymphoid and myeloid cell regulation, BTK inhibition reduced neurodegeneration and disease progression during secondary progressive EAE."

Journal • CNS Disorders • Immunology • Inflammation • Multiple Sclerosis • ARG1 • CD86 • IL1B • MRC1

A CNS-Penetrant BTK Inhibitor Modulates Multiple Pathogenic Pathways Implicated in Multiple Sclerosis (ACTRIMS Forum 2023) - "CNS-penetrant BTKis, such as GB7208, have the ability to inhibit multiple inflammatory mechanisms within the CNS compartment relevant to MS pathogenesis and may have the potential to impact PIRA."

CNS Disorders • Inflammation • Inflammatory Arthritis • Multiple Sclerosis • Rheumatology • Solid Tumor

GB7208 is a novel, highly potent and selective CNS-penetrant BTK inhibitor for neuroinflammatory and neurodegenerative diseases (ECTRIMS 2022) - "GB7208 has been designed as an orally available, selective, irreversible small molecule BTKi optimized for best-in-class potency, selectivity, and brain exposure. The pharmacologic features of GB7208 support further investigation in neuroinflammatory/neurodegenerative diseases such as MS, where BTK is a critical signaling node contributing to activation and function of pathogenic B cells and microglia within the CNS."

CNS Disorders • Immunology • Multiple Sclerosis • EGFR

GB7208 is a CNS-penetrant BTK inhibitor demonstrating potent activity on pathogenic pathways implicated in Multiple Sclerosis (ECTRIMS 2022) - "GB7208 is a CNS-penetrant BTK inhibitor that potently inhibits multiple mechanisms relevant to MS pathogenesis."

CNS Disorders • Immunology • Inflammatory Arthritis • Multiple Sclerosis • Solid Tumor