TOK-001 (Galeterone) is a potent 17α-hydroxylase/17,20-lyase (CYP17) inhibitor with IC50 of 300 nM.
TOK-001 (Galeterone) also shown to be potent pure AR antagonist.
TOK-001 (Galeterone) inhibits the growth of DHT-stimulated LNCaP and LAPC4 prostate cancer cells with IC50 <10 uM.
TOK-001 (Galeterone) causes marked down-regulation of AR protein expression, more efficacious than castration in the LAPC4 xenograft model.
