dbo:abstract |
Endoxifen, also known as 4-hydroxy-N-desmethyltamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group as well as a protein kinase C (PKC) inhibitor. It is under development for the treatment of estrogen receptor-positive breast cancer and for the treatment of mania in bipolar disorder. It is taken by mouth. Endoxifen is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce endoxifen and afimoxifene (4-hydroxytamoxifen). Currently, endoxifen is approved by Drugs Controller General of India for the acute treatment of manic episode with or without mixed features of Bipolar I disorder. It is manufactured and sold by Intas Pharmaceuticals under the brand name Zonalta. (en) |
dbo:alternativeName |
Zonalta (en) |
dbo:casNumber |
1032008-74-4 (hydrochloride) 112093-28-4 114828-90-9 (E-isomer) |
dbo:chEMBL |
1949791 |
dbo:fdaUniiCode |
46AF8680RC |
dbo:pubchem |
130621 |
dbo:thumbnail |
wiki-commons:Special:FilePath/Endoxifen.svg?width=300 |
dbo:wikiPageExternalLink |
https://adisinsight.springer.com/drugs/800036114 |
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14655 (xsd:nonNegativeInteger) |
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dbo:wikiPageWikiLink |
dbr:Montgomery–Åsberg_Depression_Rating_Scale dbr:Bipolar_disorder dbr:Breast_cancer dbr:Antiestrogen dbr:Lithium_(medication) dbr:Cytochrome_P450 dbr:Valproate dbc:Alcohols dbc:Experimental_drugs dbc:Human_drug_metabolites dbc:Phenol_ethers dbr:Estrogen_(medication) dbr:Oral_administration dbr:Enzyme dbr:Fulvestrant dbr:Aromatase_inhibitor dbr:Clinical_Global_Impression dbr:Prodrug dbr:Protein_kinase_C dbr:Protein_kinase_inhibitor dbc:Hormonal_antineoplastic_drugs dbr:Active_metabolite dbr:Triphenylethylene dbr:Drugs_Controller_General_of_India dbr:Afimoxifene dbc:Triphenylethylenes dbr:Estradiol dbr:Estradiol_(medication) dbr:Estrogen_receptor dbr:Nonsteroidal dbr:Isomer dbc:Selective_estrogen_receptor_modulators dbr:Tamoxifen dbr:Hydrochloride dbr:Affinity_(pharmacology) dbr:Bipolar_I_disorder dbr:CYP2D6 dbr:India dbr:Intas_Pharmaceuticals dbr:Metabolism dbr:Mania dbr:Selective_estrogen_receptor_modulator dbr:Young_Mania_Rating_Scale dbr:Manic_episode dbr:Mixed_episode dbr:N-desmethyltamoxifen dbr:ERα dbr:ERβ |
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25 (xsd:integer) |
dbp:casNumber |
112093 (xsd:integer) |
dbp:casSupplemental |
114828 (xsd:integer) 1032008 (xsd:integer) |
dbp:chembl |
1949791 (xsd:integer) |
dbp:h |
27 (xsd:integer) |
dbp:iupacName |
4 (xsd:integer) |
dbp:n |
1 (xsd:integer) |
dbp:o |
2 (xsd:integer) |
dbp:pdbLigand |
9 (xsd:integer) |
dbp:pubchem |
130621 (xsd:integer) |
dbp:routesOfAdministration |
dbr:Oral_administration |
dbp:smiles |
CCCC3=CC=CC=C3 (en) |
dbp:stdinchi |
1 (xsd:integer) |
dbp:stdinchikey |
MHJBZVSGOZTKRH-UHFFFAOYSA-N (en) |
dbp:synonyms |
4 (xsd:integer) |
dbp:tradename |
Zonalta (en) |
dbp:unii |
46 (xsd:integer) |
dbp:width |
250 (xsd:integer) |
dbp:wikiPageUsesTemplate |
dbt:Drugbox dbt:Estrogen_receptor_modulators dbt:Reflist dbt:Short_description dbt:Cascite dbt:Fdacite |
dcterms:subject |
dbc:Alcohols dbc:Experimental_drugs dbc:Human_drug_metabolites dbc:Phenol_ethers dbc:Hormonal_antineoplastic_drugs dbc:Triphenylethylenes dbc:Selective_estrogen_receptor_modulators |
rdf:type |
owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
rdfs:comment |
Endoxifen, also known as 4-hydroxy-N-desmethyltamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group as well as a protein kinase C (PKC) inhibitor. It is under development for the treatment of estrogen receptor-positive breast cancer and for the treatment of mania in bipolar disorder. It is taken by mouth. (en) |
rdfs:label |
Endoxifen (en) |
owl:sameAs |
yago-res:Endoxifen wikidata:Endoxifen https://global.dbpedia.org/id/2YAXB |
prov:wasDerivedFrom |
wikipedia-en:Endoxifen?oldid=1090500192&ns=0 |
foaf:depiction |
wiki-commons:Special:FilePath/Endoxifen.svg |
foaf:isPrimaryTopicOf |
wikipedia-en:Endoxifen |
is dbo:wikiPageRedirects of |
dbr:Zonalta dbr:Endoxifene dbr:Z-endoxifen dbr:ZONALTA |
is dbo:wikiPageWikiLink of |
dbr:List_of_investigational_sex-hormonal_agents dbr:List_of_selective_estrogen_receptor_modulators dbr:Clomifenoxide dbr:Triphenylethylene dbr:Droloxifene dbr:Nonsteroidal dbr:Norendoxifen dbr:Tamoxifen dbr:Zonalta dbr:C25H27NO2 dbr:Endoxifene dbr:N-Desmethyltamoxifen dbr:Z-endoxifen dbr:ZONALTA |
is foaf:primaryTopic of |
wikipedia-en:Endoxifen |