Preferred Label : Tolebrutinib;
NCIt synonyms : Bruton's Tyrosine Kinase Inhibitor SAR442168; BTK Inhibitor SAR442168;
NCIt definition : An orally bioavailable, brain-penetrant, selective, small molecule inhibitor of Bruton's
tyrosine kinase (BTK), with potential immunomodulatory and anti-inflammatory activities.
Upon oral administration, tolebrutinib is able to cross the blood-brain barrier and
inhibits the activity of BTK both peripherally and in the central nervous system (CNS).
This prevents the activation of the B-cell antigen receptor (BCR) signaling pathway,
and the resulting immune activation and inflammation. The inhibition of BTK activity
also prevents microglial inflammatory signaling in the CNS, and the resulting immune
activation, neuroinflammation and neurodegeneration. BTK, a cytoplasmic tyrosine kinase
and member of the Tec family of kinases, plays an important role in B lymphocyte development,
activation, signaling, proliferation and survival. In addition to B cells, BTK is
also expressed in innate immune cells, including macrophages and microglia, and plays
an important role in the regulation of microglial inflammatory signaling.;
UNII : 8CZ82ZYY9X;
InChIKey : KOEUOFPEZFUWRF-LJQANCHMSA-N;
CAS number : 1971920-73-6;
Molecule name : SAR 442168; SAR-442168;
NCI Metathesaurus CUI : CL1407319;
Origin ID : C173549;
UMLS CUI : C5420258;
Semantic type(s)
- concept_is_in_subset
- has_target
