Drug intelligence / Profile preview

nemtabrutinib

Development stage
Phase 3
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Nemtabrutinib is an orally available, reversible, non-covalent small molecule inhibitor of Bruton's tyrosine kinase (BTK), developed for the treatment of various B-cell malignancies. Unlike earlier BTK inhibitors, nemtabrutinib is effective against both wild-type and C481S mutant forms of BTK, addressing a common resistance mechanism to covalent BTK inhibitors. It works by blocking the action of BTK in malignant B cells, thereby suppressing oncogenic B-cell receptor signaling and inhibiting cancer cell growth and survival. Nemtabrutinib is being investigated in multiple clinical trials for blood cancers including chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), Waldenström’s macroglobulinemia, mantle cell lymphoma, follicular lymphoma, marginal zone lymphoma, and Richter’s transformation[1][3][4][5][6].

Other names
MK-1026MK1026MK 1026ARQ 531ARQ531ARQ-531
02

Targets

BTK (Bruton tyrosine kinase)

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