Preferred Label : Endoxifen Hydrochloride;
NCIt synonyms : Z-Endoxifen HCl; 4-Hydroxy-N-Desmethyltamoxifen Hydrochloride; Z-Endoxifen Hydrochloride;
NCIt definition : The hydrochloride salt and the z (cis-) stereoisomer of endoxifen with potential antineoplastic
activity. Endoxifen, the active metabolite of tamoxifen, competitively inhibits the
binding of estradiol to estrogen receptors, thereby preventing the receptor from binding
to the estrogen-response element on DNA and thus reducing DNA synthesis. Unlike tamoxifen,
however, which relies on CYP2D6 activity for its conversion to the active metabolite
endoxifen, the direct administration of endoxifen bypasses the CYP2D6 route. As CYP2D6
activity can vary widely among individuals due to genetic CYP2D6 polymorphisms, endoxifen
is therefore theoretically more potent and more uniform in its bioavailability across
patient populations.;
UNII : 308PA1L567;
CAS number : 1032008-74-4;
NCI Metathesaurus CUI : CL428178;
Origin ID : C95713;
UMLS CUI : C2987366;
Semantic type(s)
- concept_is_in_subset
- has_target
