spebrutinib

Spebrutinib is an orally bioavailable, covalent, small-molecule inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), a cytoplasmic tyrosine kinase involved in B-cell receptor and Fc receptor signaling pathways. By irreversibly binding to the ATP-binding site of BTK (notably at Cys 481), spebrutinib blocks BTK activity, leading to inhibition of B-cell activation, proliferation, and survival. This mechanism disrupts downstream signaling critical for both innate and adaptive immune responses. Spebrutinib was developed for potential use in B-cell malignancies such as chronic lymphocytic leukemia and diffuse large B-cell lymphoma, as well as autoimmune diseases like rheumatoid arthritis. The drug was originally discovered by Avila Therapeutics and later acquired by Celgene; however, its development has been terminated and it is no longer in active clinical pipelines[1][3][5].

Other names

spebrutinibN-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide