Preferred Label : BTK Degrader ABBV-101;
NCIt definition : An orally bioavailable, targeted degrader of Bruton's tyrosine kinase (BTK; Bruton
agammaglobulinemia tyrosine kinase) comprised of an E3 ubiquitin ligase binding moiety
conjugated, via a linker, to a BTK-binding moiety, with potential antineoplastic activity.
Upon oral administration of BTK degrader ABBV-101, the BTK-targeting moiety targets
and binds to BTK, and the E3 ligase-binding moiety targets and binds to E3 ubiquitin
ligase. This catalyzes ubiquitination and proteasome-mediated degradation 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.;
Molecule name : ABBV 101; ABBV-101;
NCI Metathesaurus CUI : CL1907333;
Origin ID : C200056;
chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
