Preferred Label : 17beta-Hydroxysteroid Dehydrogenase Type 5 Inhibitor ASP9521;
NCIt synonyms : 17bHSD5 Inhibitor ASP9521; (4-(2-Hydroxy-2-methylpropyl)piperidin-1-yl)(5-methoxy-1H-indol-2-yl)methanone;
NCIt related terms : ASP-9521;
NCIt definition : A selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase
type 5 (17bHSD5, aldo-keto reductase 1C3; AKR1C3), with potential antineoplastic activity.
Upon administration, ASP9521 selectively binds to and inhibits the activity of 17bHSD5.
This prevents the conversion of the adrenal androgens dehydroepiandrosterone and androstenedione
into 5-androstenediol and testosterone. By blocking testosterone production, ASP9521
may inhibit the growth of testosterone-dependent cancers such as castration-resistant
prostate cancer (CRPC). 17bHSD5, expressed both in normal prostate tissue and in prostate
cancer (PC), plays a crucial role in persistent production of androgens despite castration;
its expression is associated with increased malignancy of PC.;
UNII : AA79G37CPR;
CAS number : 1126084-37-4;
Molecule name : ASP 9521; ASP9521;
Origin ID : C133224;
UMLS CUI : C4045761;
Semantic type(s)
- concept_is_in_subset
