ibrutinib + zanubrutinib

Ibrutinib and zanubrutinib are small molecule inhibitors of Bruton's tyrosine kinase (BTK) used in the treatment of B-cell malignancies, including Waldenström's macroglobulinemia. Ibrutinib is a first-generation irreversible BTK inhibitor, while zanubrutinib is a next-generation, more selective irreversible BTK inhibitor designed to minimize off-target effects. In the context of the BLOOD-dose platform trial (specifically the BELLIS domain) led by Anne Louise Tølbøll Sørensen, these agents are being evaluated to determine if reduced-dose regimens are non-inferior in safety and effectiveness compared to standard-dose treatments for patients with Waldenström's macroglobulinemia. Both drugs work by forming a covalent bond with a cysteine residue in the BTK active site, thereby blocking B-cell receptor signaling and inhibiting the proliferation of malignant B cells.

Other names

BTK inhibitors