zanubrutinib + methotrexate + rituximab

This investigational combination therapy consists of zanubrutinib, a second-generation Bruton tyrosine kinase (BTK) inhibitor; rituximab, a CD20-directed monoclonal antibody; and high-dose methotrexate (HD-MTX), a folate antimetabolite chemotherapy agent. The regimen is being evaluated in a Phase II clinical trial (NCT05398224) led by Peking University Cancer Hospital for the treatment of secondary central nervous system lymphoma (SCNSL) in patients with diffuse large B-cell lymphoma (DLBCL). Zanubrutinib is specifically included for its high blood-brain barrier permeability, which is critical for treating CNS involvement. The therapy functions by simultaneously inhibiting B-cell receptor signaling via BTK, inducing B-cell lysis through CD20 targeting, and disrupting DNA synthesis in rapidly dividing malignant cells via dihydrofolate reductase inhibition.

Brand names

RituxanMabThera

Other names

Z-R-MTXZanubrutinib + HD-MTX + RituximabZanubrutinib plus High-Dose Methotrexate and Rituximab