Androgen Receptors

TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor.

ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.

AZD-3514 is a potent androgen receptor downregulator with potential anticancer cancer activity.

Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues.

CSRM617 is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice.

ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.