Preferred Label : Rocbrutinib;
NCIt synonyms : BTKi LP-168; WT/C481 Mutation-specific BTK Inhibitor LP-168; LP-168; BTK Inhibitor LP-168;
NCIt definition : An orally bioavailable inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia
tyrosine kinase), with potential antineoplastic activity. Upon oral administration,
rocbrutinib covalently binds to and inhibits the activity of wild-type (WT) BTK and
non-covalently binds to inhibits the activity of C481 mutated BTK, a resistance mutation
in the BTK active site in which cysteine is substituted for serine at residue 481
(C481S). 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. 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. BTK C481S mutation plays an
important role in resistance to certain BTK inhibitors. This dual activity allows
efficacy against tumor cells expressing WT BTK through covalent binding while simultaneously
preventing the proliferation of tumor cells expressing the most common resistance
mutation to covalent BTK inhibitors through non-covalent binding.;
UNII : KD68L3GRW2;
CAS number : 2485861-07-0;
Molecule name : LP 168; LP168; NWP-775; NWP 775;
NCI Metathesaurus CUI : CL1922154;
Origin ID : C203033;
UMLS CUI : C5908925;
Semantic type(s)
- concept_is_in_subset
- has_target
