Cytochrome P450

CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.

Talarozole R enantiomer inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase.

Phortress, also known as NSC-710305 and 5F-DF-203-L-lysinamide, is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.

EMT inhibitor-2 inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.

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

Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51.

Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.