UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy. In LNCaP cells, UT-34 (3-10 μM; 24 hours) treatment inhibits the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM.

Cortexolone 17 alpha-propionate (CB-03-01, Clascoterone) is a topical and peripherally selective androgen antagonist.

Ailanthone is an effective inhibitor of both full-length androgen receptor (AR) (IC50: 69?nM) and constitutively active truncated AR splice variants (IC50: 309?nM).