Docirbrutinib

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable, non-covalent inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon oral administration, docirbrutinib non-covalently binds to and inhibits the activity of both wild-type and the C481S mutated form of BTK, a drug 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, 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:** - AS 1763 - AS-1763 - AS1763 - BN 102 - BN-102 - BN102 - BTK Inhibitor AS-1763 - Bruton's Tyrosine Kinase Inhibitor AS-1763 - DOCIRBRUTINIB - Milrebrutinib