MLchartDataset catalogue

EGFR mutant-selective inhibitor TRX-221

Term · Oncology and biomedicine · MLC-T-ONC-013262

An orally bioavailable, mutant-selective, fourth-generation epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGFR mutant-selective inhibitor TRX-221 targets, binds to and inhibits the activity of EGFR with selective mutations, including Del19/T790M/C797S, L858R/T790M/C797S, Del19/C797S, L858R/C797S, Del19/T790M, L858R/T790M, Del19, and L858R, thereby preventing 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 tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. TRX-221 is able to cross the blood-brain barrier (BBB). By sparing wild-type (WT) EGFR, TRX-221 may avoid EGFR-related toxicities.

Table 1. Record
IdentifierMLC-T-ONC-013262
FieldOncology and biomedicine
SynonymsEGFR inhibitor TRX-221
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-013262",
  "term": "EGFR mutant-selective inhibitor TRX-221",
  "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 TRX-221 targets, binds to and inhibits the activity of EGFR with selective mutations, including Del19/T790M/C797S, L858R/T790M/C797S, Del19/C797S, L858R/C797S, Del19/T790M, L858R/T790M, Del19, and L858R, thereby preventing 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 tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. TRX-221 is able to cross the blood-brain barrier (BBB). By sparing wild-type (WT) EGFR, TRX-221 may avoid EGFR-related toxicities.",
  "synonyms": [
    "EGFR inhibitor TRX-221"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/egfr-mutant-selective-inhibitor-trx-221/"
}

Record 6,454 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.