Drug intelligence / Profile preview

tislelizumab + zanubrutinib

Development stage
Unknown
Lead developer
BeiGene
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

Tislelizumab + zanubrutinib is a combination therapy that pairs a PD-1 inhibitor (tislelizumab) with a BTK inhibitor (zanubrutinib). This combination has shown promising efficacy in treating B-cell malignancies, particularly Richter's transformation, which is an aggressive transformation of chronic lymphocytic leukemia (CLL) into diffuse large B-cell lymphoma (DLBCL). **Mechanism of Action:** - Tislelizumab is a humanized IgG4 variant monoclonal antibody that targets PD-1 with high affinity and specificity. It was engineered to minimize binding to Fc-γ receptor on macrophages to prevent macrophage-driven killing of effector T-cells. - Zanubrutinib is a next-generation BTK inhibitor that forms a covalent bond with cysteine 481 in the ATP-binding pocket of BTK, blocking B-cell receptor signaling pathways and inhibiting the proliferation, trafficking, chemotaxis, and adhesion of malignant B cells. The combination potentially creates a synergistic effect by simultaneously targeting immune checkpoint inhibition and B-cell receptor signaling.

Brand names
BrukinsaTevimbra
Other names
BGB-3111BGB3111BGB 3111BGB-A317BGB-A-317BGB-A 317
02

Targets

BTK (Bruton tyrosine kinase)PDCD1 (Programmed cell death protein 1 receptor)

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