Preferred Label : Transdermal 17beta-Estradiol Gel BHR-200;
NCIt definition : A proprietary, transdermal, hydroalcoholic gel formulation containing 17beta-estradiol,
with potential antineoplastic activity. Upon topical administration, 17beta-estradiol
exerts its antineoplastic effect(s) through as of yet not fully elucidated mechanism(s)
of action(s). This formulation may induce feedback inhibition via the hypothalamic-pituitary-gonadal
axis feedback loop, block the secretion of luteinizing hormone (LH) and prevent the
release of testosterone from Leydig cells in the testes, thus suppressing testosterone
secretion. In addition, 17beta-estradiol inhibits enzymes involved in steroidogenesis,
thereby further inhibiting androgen production. Since testosterone is required to
sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent
prostate cancer cell proliferation. In addition, 17beta-estradiol prevents bone loss,
and suppresses andropause symptoms, such as hot flashes, which appear during androgen-deprivation
therapy (ADT) where the standard of care is the use of gonadotrophin releasing hormone
(GnRH) analogs. Compared to oral estrogens, the topical gel formulation lowers the
risk of cardiovascular side effects.;
Molecule name : BHR-200;
Origin ID : C120308;
UMLS CUI : C3896903;
Semantic type(s)
- chemical_or_drug_is_metabolized_by_enzyme
- concept_is_in_subset
