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bexirestrant

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.
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Synonym:selective estrogen receptor degrader SCO-120
SERD SCO-120
Code name:SCO 120
SCO-120
SCO120
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