Zanubrutinib - Mode of Action

Zanubrutinib (BGB-3111) is a small molecule inhibitor of Bruton’s tyrosine kinase (BTK) that is currently being evaluated in a broad late-stage clinical trials program globally, as a potential monotherapy and in combination with other therapies to treat various B cell malignancies.

BTK is a key component of the B cell receptor (BCR) signaling pathway, and is an important regulator of cell proliferation and cell survival in various B cell malignancies. BTK inhibitors block BCR-induced BTK activation and its downstream signaling, leading to growth inhibition and cell death in certain malignant white blood cells called B cells.

Zanubrutinib is an orally active inhibitor that covalently binds to BTK, resulting in irreversible inactivation of the enzyme.

Zanubrutinib is in pivotal Phase 2 and Phase 3 trials in several B cell malignancies including: Waldenstrom’s macroglobulinemia (WM), treatment-naive mantle cell lymphoma (MCL), both front-line and relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), relapsed/refractory follicular lymphoma, marginal zone lymphoma, and diffuse large B cell lymphoma.