Preferred Label : Pebezertinib;
NCIt synonyms : EGFR Ex20ins Inhibitor BLU-451; EGFR Inhibitor BLU-451; EGFR Exon 20 Insertion Inhibitor BLU-451;
NCIt definition : An orally bioavailable, central nervous system (CNS) penetrating, mutant-selective
covalent inhibitor of epidermal growth factor receptor (EGFR) exon 20 insertion (Ex20ins)
activating mutations, with potential antineoplastic activity. Upon oral administration,
pebezertinib selectively targets, irreversibly binds to and inhibits the activity
of EGFR Ex20ins and some other oncogenic point mutations. This prevents EGFR Ex20ins-mediated
signaling. This may induce cell death and inhibit tumor growth in EGFR Ex20ins-overexpressing
tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumors, plays a key
role in tumor cell proliferation and tumor vascularization. Pebezertinib 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. Pebezertinib does not inhibit
the activity of wild-type (WT) EGFR. EGFR Ex20ins are oncogenic driver mutations that
constitutively upregulate kinase activity.;
UNII : G8G5AU5GLJ;
CAS number : 2769954-39-2;
Molecule name : LNG 451; BLU 451; LNG-451; BLU-451;
NCI Metathesaurus CUI : CL1779252;
Origin ID : C187042;
UMLS CUI : C5667102;
Semantic type(s)
- concept_is_in_subset
- has_target
