Drug intelligence / Profile preview

zanubrutinib

Development stage
Approved
Lead developer
BeiGene
Modality
Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Fragment-Derived Small Molecules → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

Zanubrutinib is a second-generation, highly selective, irreversible small molecule inhibitor of Bruton's tyrosine kinase (BTK). It is designed to maximize BTK occupancy and minimize off-target kinase inhibition. By inhibiting BTK, zanubrutinib disrupts B-cell receptor signaling pathways that are critical for the survival and proliferation of malignant B cells. This mechanism underlies its efficacy in treating various B-cell malignancies. Zanubrutinib was developed by BeiGene and is marketed under the brand name Brukinsa (百悦泽). It was first approved in the United States in November 2019 for mantle cell lymphoma (MCL) after at least one prior therapy, making it the first Chinese-developed cancer drug approved by the FDA. Subsequent approvals include Waldenström macroglobulinemia (WM), marginal zone lymphoma (MZL), chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), and follicular lymphoma (FL) in combination with obinutuzumab[3][7][9][10]. Clinical trials have demonstrated superior efficacy and improved safety/tolerability compared to first-generation BTK inhibitors such as ibrutinib[6][8].

Brand names
Brukinsa百悦泽
Other names
泽布替尼赞鲁替尼澤佈替尼
02

Targets

BTK (Bruton tyrosine kinase)

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