BTK inhibitor HMPL-760

{
  "id": "MLC-T-ONC-012149",
  "term": "BTK inhibitor HMPL-760",
  "field": "Oncology and biomedicine",
  "definition": "A third-generation, reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon administration, BTK inhibitor HMPL-760 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 or the C481S mutated form. BTK C481S mutation plays an important role in resistance to certain BTK inhibitors; HMPL-760 may be able to overome this resistance. 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.",
  "synonyms": [
    "Bruton's tyrosine kinase inhibitor HMPL760"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/btk-inhibitor-hmpl-760/"
}