BTK degrader ABBV-101

{
  "id": "MLC-T-ONC-012136",
  "term": "BTK degrader ABBV-101",
  "field": "Oncology and biomedicine",
  "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.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/btk-degrader-abbv-101/"
}