Preferred Label : BTK Inhibitor GB5121;
NCIt definition : An orally bioavailable, central nervous system (CNS)-penetrating, irreversible covalent
inhibitor of Bruton's tyrosine kinase (BTK), with potential antineoplastic activity.
Upon oral administration, BTK inhibitor GB5121 selectively targets, irriversibly binds
to and inhibits the activity of BTK and prevents the activation of the B-cell antigen
receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated
activation of downstream survival pathways. This leads to an inhibition of the growth
of malignant B cells that overexpress BTK. 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 B-lymphocyte development, activation, signaling, proliferation
and survival. GB5121 is able to penetrate the blood-brain-barrier (BBB) and may thereby
treat BTK-driven CNS tumors and metastasis.;
Molecule name : GB 5121; GB-5121;
NCI Metathesaurus CUI : CL1779202;
Origin ID : C187046;
UMLS CUI : C5667107;
Semantic type(s)
- concept_is_in_subset
- has_target
