Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD).
Elacestrant (RAD-1901) inhibits ERα expression in MCF-7 cells (IC50=0.6 nM).
Elacestrant (RAD-1901) induces the degradation of ER, inhibits ER-mediated signaling and growth of ER+ breast cancer cell lines in vitro and in vivo, and significantly inhibits tumor growth of multiple PDX models.
