EGFR mutant-selective inhibitor BLU-701

{
  "id": "MLC-T-ONC-013254",
  "term": "EGFR mutant-selective inhibitor BLU-701",
  "field": "Oncology and biomedicine",
  "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.",
  "synonyms": [
    "EGFR inhibitor BLU-701",
    "EGFR TKI BLU-701"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/egfr-mutant-selective-inhibitor-blu-701/"
}