NCIt definition : An orally available inhibitor of both the steroid 17-alpha-hydroxylase/C17,20 lyase
(CYP17A1 or CYP17) and androgen receptor (AR), with potential anti-androgen and antineoplastic
activities. Upon oral administration, CYP17/AR inhibitor ODM 204 selectively inhibits
the enzymatic activity of CYP17A1 in both the testes and adrenal glands, thereby inhibiting
androgen production. This may both decrease androgen-dependent growth signaling and
inhibit the proliferation of androgen-dependent tumor cells. In addition, ODM 204
binds to ARs in target tissues and inhibits androgen-induced receptor activation and
AR nuclear translocation, which prevents the binding to and transcription of AR-responsive
genes. This leads to an inhibition of growth in AR-expressing prostate cancer cells.
The cytochrome P450 enzyme CYP17A1, which is localized to the endoplasmic reticulum,
exhibits both 17alpha-hydroxylase and 17,20-lyase activities.;
Semantic type(s)