About: Z-Endoxifen Hydrochloride     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Z-Endoxifen Hydrochloride
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Z-Endoxifen Hydrochloride
NCI_META_CUI
  • CL428178
PDQ_Open_Trial_Search_ID
  • 693335
PDQ_Closed_Trial_Search_ID
  • 693335
FULL_SYN
  • 4-Hydroxy-N-Desmethyltamoxifen HydrochlorideSNNCI
  • Z-Endoxifen HydrochloridePTNCI
  • Z-Endoxifen HClSYNCI
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.NCI
code
  • C95713
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