Definition

An orally bioavailable, selective estrogen receptor (ER) alpha-targeted chimeric protein degrader, with potential antineoplastic activity. Upon oral administration, ER alpha-targeting chimeric protein degrader AC682 targets ER alpha wild-type and mutants and induces the degradation of ER alpha proteins. This decreases ER alpha protein levels, decreases the expression of ER alpha-target genes and halts ER-mediated signaling. This results in an inhibition of proliferation in ER alpha-overexpressing tumor cells. ER alpha is overexpressed in a variety of cancers and plays a key role in cancer cell proliferation. AC682 is able to cross the blood-brain barrier (BBB).