Preferred Label : CYP17/CYP11B2 Inhibitor LAE001;
NCIt related terms : CFG-920;
NCIt definition : An orally bioavailable, non-steroidal, potent, reversible, dual inhibitor of cytochrome
P450 17 (CYP17 or CYP17A1) and CYP11B2, with potential antiandrogen and antineoplastic
activities. Upon oral administration, LAE001 inhibits the enzymatic activity of CYP17A1
in both the testes and adrenal glands, thereby inhibiting androgen production. This
may decrease androgen-dependent growth signaling and may inhibit cell proliferation
of androgen-dependent tumor cells. LAE001 also inhibits the enzymatic activity of
CYP11B2, thereby inhibiting aldosterone production. This may reduce the elevated aldosterone
levels resulting from CYP17 inhibition and androgen deprivation, leading to a reduction
in mineralocorticoid side effects including cardiovascular complications. The cytochrome
P450 enzyme CYP17A1, localized to the endoplasmic reticulum, exhibits both 17alpha-hydroxylase
and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that
produces steroidal hormones. The cytochrome P450 enzyme CYP11B2, aldosterone synthase,
is an enzyme that plays a key role in aldosterone biosynthesis.;
UNII : UP0K5026VB;
CAS number : 1260006-20-9;
Molecule name : LAE-001; CFG 920; CFG-920; LAE 001;
NCI Metathesaurus CUI : CL437136;
Origin ID : C102855;
UMLS CUI : C5417776;
Semantic type(s)
- concept_is_in_subset
- has_target
