EGFR mutant-selective inhibitor BBT-176
Term · Oncology and biomedicine · MLC-T-ONC-013253
A fourth-generation, orally bioavailable, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGFR mutant-selective inhibitor BBT-176 targets, binds to, and inhibits the activity of EGFR with C797S triple mutations including Del19/T790M/C797S and L858R/T790M/C797S, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-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. BBT-176 inhibits EGFR with C797S mutations, which prevents covalent bond formation with third-generation EGFR inhibitors leading to drug resistance. BBT-176 may have enhanced anti-tumor effects in tumors with C797S-mediated resistance when compared to other EGFR tyrosine kinase inhibitors.
| Identifier | MLC-T-ONC-013253 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | epidermal growth factor receptor mutant-selective inhibitor BBT-176; mutant-selective EGFR inhibitor BBT-176 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-013253",
"term": "EGFR mutant-selective inhibitor BBT-176",
"field": "Oncology and biomedicine",
"definition": "A fourth-generation, orally bioavailable, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGFR mutant-selective inhibitor BBT-176 targets, binds to, and inhibits the activity of EGFR with C797S triple mutations including Del19/T790M/C797S and L858R/T790M/C797S, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-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. BBT-176 inhibits EGFR with C797S mutations, which prevents covalent bond formation with third-generation EGFR inhibitors leading to drug resistance. BBT-176 may have enhanced anti-tumor effects in tumors with C797S-mediated resistance when compared to other EGFR tyrosine kinase inhibitors.",
"synonyms": [
"epidermal growth factor receptor mutant-selective inhibitor BBT-176",
"mutant-selective EGFR inhibitor BBT-176"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/egfr-mutant-selective-inhibitor-bbt-176/"
}
Record 6,444 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.