Preferred Label : Enozertinib;
NCIt synonyms : EGFR/HER2 Inhibitor ORIC-114;
NCIt definition : An orally bioavailable, central nervous system (CNS) penetrating, mutant-selective
covalent inhibitor of epidermal growth factor receptor (EGFR; ErbB1) and human epidermal
growth factor receptor 2 (HER2; EGFR2; ErbB2) alterations, including exon 20 insertion
(Ex20ins) mutations, with potential antineoplastic activity. Upon oral administration,
enozertinib selectively targets, irreversibly binds to and inhibits the activity of
EGFR or HER2 insertions or mutations. This prevents EGFR/HER2-mediated signaling.
This may induce cell death and inhibit tumor growth in EGFR/HER2-overexpressing tumor
cells. Enozertinib is able to penetrate the blood-brain-barrier (BBB) and may therefore
exert its activity against EGFR Ex20ins-driven CNS primary tumors and CNS metastases.
The ErbB receptor tyrosine kinase family is involved in key cellular functions, including
cell growth and survival. EGFR and HER2 alterations constitutively upregulate kinase
activity.;
UNII : DU24UP8R94;
CAS number : 2489185-38-6;
Molecule name : ORIC 114; ORIC-114;
NCI Metathesaurus CUI : CL1792172;
Origin ID : C187334;
UMLS CUI : C5706402;
Semantic type(s)
- concept_is_in_subset
- has_target
