NCIt definition : An orally available selective androgen receptor (AR)-targeted protein degrader, using
the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic
activity. Bavdegalutamide is composed of an AR ligand attached to an E3 ligase recognition
moiety. Upon oral administration, bavdegalutamide targets and binds to the AR ligand
binding domain. E3 ligase is recruited to the AR by the E3 ligase recognition moiety
and the AR target protein is tagged by ubiquitin. This causes ubiquitination and degradation
of AR by the proteasome. This prevents the expression of AR target genes and halts
AR-mediated signaling. This results in an inhibition of proliferation in AR-overexpressing
tumor cells. In addition, the degradation of the AR protein releases the ARV-110 is
released and can bind to additional AR target proteins. AR plays a key role in the
proliferation of castration-resistant prostate cancer cells (CRPC).;