Bexirestrant

{
  "id": "MLC-T-ONC-011999",
  "term": "Bexirestrant",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, bexirestrant specifically targets and binds to both wild-type and mutant forms of the estrogen receptor (ER; ERalpha), including the somatic mutations Y537S and D538G. This induces a conformational change that results in ER degradation. This prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells. Somatic mutations in the ER gene ESR1, especially Y537S and D538G, have been associated with acquired antiestrogen drug resistance.",
  "synonyms": [
    "SERD SCO-120",
    "selective estrogen receptor degrader SCO-120"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/bexirestrant/"
}