Preferred Label : Nemtabrutinib;
NCIt synonyms : Bruton's Tyrosine Kinase Inhibitor ARQ 531; BTK Inhibitor ARQ 531;
NCIt definition : An orally available reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton
agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon
administration, nemtabrutinib non-covalently binds to and inhibits the activity of
both the wild-type and the C481S mutated form of BTK, a resistance mutation in the
BTK active site in which cysteine is substituted for serine at residue 481. This prevents
the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated
activation of downstream survival pathways. This leads to an inhibition of the growth
of malignant B-cells that overexpress BTK. Compared to other BTK inhibitors, nemtabrutinib
does not require interaction with the BTK C481 site and inhibits the proliferation
of cells harboring the BTK C481S mutation. BTK, a member of the Src-related BTK/Tec
family of cytoplasmic tyrosine kinases, is overexpressed or mutated in B-cell malignancies;
it plays an important role in the development, activation, signaling, proliferation
and survival of B-lymphocytes.;
UNII : JTZ51LIXN4;
CAS number : 2095393-15-8;
Molecule name : ARQ 531; ARQ-531; MK-1026;
NCI Metathesaurus CUI : CL525087;
Origin ID : C138066;
UMLS CUI : C5691143;
Semantic type(s)
- concept_is_in_subset
- has_target
