EGFR Exon 20 Insertion Inhibitor BLU-451

Preferred Label : EGFR Exon 20 Insertion Inhibitor BLU-451;

NCIt synonyms : EGFR Ex20ins Inhibitor BLU-451; EGFR 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, EGFR Ex20ins inhibitor BLU-451 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. BLU-451 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. BLU-451 does not inhibit the activity of wild-type (WT) EGFR. EGFR Ex20ins are oncogenic driver mutations that constitutively upregulate kinase activity.;

Molecule name : LNG 451; BLU 451; LNG-451; BLU-451;

NCI Metathesaurus CUI : CL1779252;

Details

Origin ID

C187042;

UMLS CUI

C5667102;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
concept_is_in_subset
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_target
- EGFR Exon 20 Insertion Mutation [NCIt concept]
- Epidermal Growth Factor Receptor [NCIt concept]

Keyword's position in hierarchy(ies) :

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