Preferred Label : Transdermal 4-Hydroxytestosterone;
NCIt synonyms : Transdermal 4-OHT; Transdermal CR1447;
NCIt definition : A transdermal formulation containing 4-hydroxytestosterone (4-OHT), a steroidal aromatase
inhibitor (AI) and androgen receptor (AR) antagonist, with potential antineoplastic
activity. 4-OHT is largely converted into 4-hydroxyandrostenedione (4-OHA) and irreversibly
binds to and inhibits aromatase, thereby blocking the conversion of androstenedione
to estrone, and testosterone to estradiol. This may inhibit tumor cell proliferation
in estrogen-dependent tumor cells. In addition, 4-OHT binds to the AR and may inhibit
AR-mediated tumor cell growth. Aromatase, a cytochrome P-450 enzyme, is overexpressed
in a variety of cancer cells; it plays a key role in estrogen biosynthesis. Compared
to oral 4-OHT, the transdermal formulation allows for continuous release of 4-OHT
into the bloodstream and prevents first pass metabolism by the liver.;
NCI Metathesaurus CUI : CL471813;
Origin ID : C114103;
UMLS CUI : C3827794;
Semantic type(s)
- concept_is_in_subset
