NCIt definition : An orally bioavailable androgen receptor (AR) antagonist with potential antineoplastic
activity. Upon oral administration, proxalutamide binds to AR in target tissues, inhibits
androgen-induced receptor activation, and facilitates the formation of inactive complexes
that cannot translocate to the nucleus. This prevents binding to and transcription
of AR-responsive genes that regulate prostate cancer cell proliferation. In addition,
proxalutamide induces AR downregulation, thereby further preventing AR-mediated signaling.
This ultimately leads to an inhibition of growth in AR-expressing prostate cancer
cells. AR is overexpressed in prostate cancer and plays a key role in prostate cancer
cell proliferation.;