tirabrutinib

Tirabrutinib is an orally administered, highly selective, irreversible small molecule inhibitor of Bruton's tyrosine kinase (BTK). It covalently binds to the cysteine residue (Cys481) in the active site of BTK within B cells, thereby blocking B cell receptor signaling and impeding B cell development. This inhibition disrupts downstream pathways such as NF-kappa-B, AKT, and ERK, leading to reduced proliferation and survival of malignant B cells. Tirabrutinib was discovered and developed by Ono Pharmaceutical. It is approved in Japan under the brand name Velexbru for relapsed or refractory primary central nervous system lymphoma (PCNSL), Waldenström's macroglobulinemia, and lymphoplasmacytic lymphoma. The drug is also being investigated for other hematological malignancies and autoimmune disorders including chronic lymphocytic leukemia (CLL), B cell lymphoma, Sjogren's syndrome, pemphigus, rheumatoid arthritis, among others[1][3][4][5][6][7].

Brand names

Velexbru

Other names

tirabrutinib1351636-18-4