Drug intelligence / Profile preview

zanubrutinib + thiotepa

Development stage
Unknown
Lead developer
BeiGene
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Zanubrutinib + thiotepa is an investigational combination regimen consisting of zanubrutinib, a second-generation small molecule Bruton's tyrosine kinase (BTK) inhibitor, and thiotepa, an alkylating agent. Zanubrutinib selectively inhibits BTK, a key enzyme in the B-cell receptor signaling pathway that promotes survival and proliferation of malignant B cells. Thiotepa is a cytotoxic chemotherapy agent that cross-links DNA strands to induce cell death and has high central nervous system (CNS) penetration. This combination is being studied primarily for the treatment of primary CNS lymphoma (PCNSL), aiming to improve remission rates by combining targeted therapy with cytotoxic chemotherapy[2][1]. The regimen may be used as induction or consolidation therapy, including in patients undergoing autologous stem cell transplantation with thiotepa-based conditioning[2][4].

Brand names
Brukinsa (zanubrutinib)Tepylute (thiotepa)
02

Targets

DNABTK (Bruton tyrosine kinase)CYP3A4 (Cytochrome P450 3A4)

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