Definition

An orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, rintodestrant specifically targets and binds to the estrogen receptor alpha (ERalpha; ERa; ESR1) and induces a conformational change that promotes ERalpha degradation and downregulation. This prevents ERalpha-mediated signaling and inhibits both the growth and survival of ERalpha-expressing cancer cells.