A Fast and Clean BTK Inhibitor
Ronen Gabizon, Nir London
Abstract
Bruton's tyrosine kinase (BTK) is a major drug target for B-cell related malignancies; however, existing BTK inhibitors approved for cancer treatment have significant off-targets that limit their use for autoimmune and inflammatory diseases. Remibrutinib (LOU064) is a novel covalent BTK inhibitor that binds an inactive BTK conformation, which affords it unprecedented selectivity. Its optimization led to rapid BTK engagement in vivo and fast clearance, further limiting systemic exposure. Remibrutinib is currently in phase 2 clinical trials for treatment of chronic urticaria and Sjoegren's syndrome.
Topics & Concepts
Bruton's tyrosine kinaseChemistryIn vivoTyrosine kinaseIbrutinibCancer researchPharmacologyImmunologyBiochemistryChronic lymphocytic leukemiaMedicineSignal transductionLeukemiaBiotechnologyBiologyChronic Lymphocytic Leukemia ResearchImmunodeficiency and Autoimmune DisordersChronic Myeloid Leukemia Treatments