Preferred Label : Vecabrutinib;
NCIt definition : An orally available second-generation, reversible inhibitor of Bruton's tyrosine kinase
(BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity.
Upon administration, vecabrutinib non-covalently binds to and inhibits the activity
of both 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, SNS-062
does not require interaction with the BTK C481 site and inhibits the proliferation
of cells harboring the BTK C481S mutation. Other irreversible BTK inhibitors covalently
bind to the C481 site to inhibit BTK's activity; the C481S mutation prevents that
binding. 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.;
UNII : PQ7O0OB5GU;
InChIKey : QLRRJMOBVVGXEJ-XHSDSOJGSA-N;
CAS number : 1510829-06-7;
Molecule name : BSK-4841; SNS 062; FP-182; SNS-062; BIIB-062;
NCI Metathesaurus CUI : CL523719;
Origin ID : C136416;
UMLS CUI : C4682414;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
