Pebezertinib - CISMeF

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;

Details

Origin ID

C187042;

UMLS CUI

C5667102;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
concept_is_in_subset
- FDA Established Names and Unique Ingredient Identifier Codes Terminology [NCIt concept]
- 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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