EGFR Mutant-selective Inhibitor BLU-701

Preferred Label : EGFR Mutant-selective Inhibitor BLU-701;

NCIt synonyms : EGFR Inhibitor BLU-701; EGFR TKI BLU-701;

NCIt definition : An orally bioavailable, mutant-selective, fourth-generation epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGFR mutant-selective inhibitor BLU-701 targets, reversibly binds to and inhibits the activity of the activating/ sensitizing mutations EGFR exon 19 deletion (ex19del) and L858R, and the C797S resistance EGFR mutations, including the resistance double mutants ex19del/C797S and L858R/C797S. This prevents EGFR mutant-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR mutant-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumors, plays a key role in tumor cell proliferation and tumor vascularization. BLU-701 is able to penetrate the blood-brain-barrier (BBB) and could exert its activity against CNS metastases in EGFR-driven tumors. BLU-701 does not inhibit the activity of wild-type (WT) EGFR.;

Molecule name : BLU 701; BLU-701;

NCI Metathesaurus CUI : CL1778244;

Details

Origin ID

C185863;

UMLS CUI

C5667029;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
concept_is_in_subset
- CTRP Agent Terminology [NCIt concept]
- CTRP 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 19 Deletion Mutation [NCIt concept]
- EGFR NP_005219.2:p.C797S [NCIt concept]
- EGFR NP_005219.2:p.L858R [NCIt concept]

Keyword's position in hierarchy(ies) :

You can consult :

recommendations
documents concerning education
documents for patients