NCIt definition : An orally bioavailable, non-covalent inhibitor of Bruton's tyrosine kinase (BTK; Bruton
agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon
oral administration, docirbrutinib non-covalently binds to and inhibits the activity
of both wild-type and the C481S mutated form of BTK, a drug 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 or the C481S mutated form.
BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is
overexpressed in B-cell malignancies; it plays an important role in the development,
activation, signaling, proliferation and survival of B-lymphocytes.;
Semantic type(s)