About: Metapristone

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An Entity of Type : dul:ChemicalObject, within Data Space : wasabi.inria.fr associated with source document(s)

Metapristone (developmental code name RU-42633; also known as desmethylmifepristone) is the major metabolite of mifepristone (RU-486, RU-38486) and a selective progesterone receptor modulator (SPRM) which itself was never marketed. It is formed from mifepristone in the liver by the enzyme CYP3A4 via monodemethylation, and circulates at concentrations higher than those of mifepristone. The metabolite retains partial but considerable affinity for the progesterone receptor (PR) and the glucocorticoid receptor (GR) (RBA = 21% and 61% of that of mifepristone for the human forms of these receptors, respectively). On the basis of actions that are apparently independent of its hormonal activity, metapristone is being researched as a potential cancer metastatic chemopreventive agent.

Attributes	Values
type	Thing drug chemical substance drug Chemical object
label	Metapristone
comment	Metapristone (developmental code name RU-42633; also known as desmethylmifepristone) is the major metabolite of mifepristone (RU-486, RU-38486) and a selective progesterone receptor modulator (SPRM) which itself was never marketed. It is formed from mifepristone in the liver by the enzyme CYP3A4 via monodemethylation, and circulates at concentrations higher than those of mifepristone. The metabolite retains partial but considerable affinity for the progesterone receptor (PR) and the glucocorticoid receptor (GR) (RBA = 21% and 61% of that of mifepristone for the human forms of these receptors, respectively). On the basis of actions that are apparently independent of its hormonal activity, metapristone is being researched as a potential cancer metastatic chemopreventive agent.
sameAs	Metapristone Metapristone Metapristone
topic	dbr:Monodemethylmifepristone dbr:Monodesmethylmifepristone dbr:Demethylmifepristone dbr:Desmethylmifepristone Mifepristone dbr:C28H33NO2 dbr:N-Demethylmifepristone dbr:N-Desmethylmifepristone dbr:N-demethylmifepristone dbr:N-desmethylmifepristone dbr:R-42,633 dbr:R-42633 dbr:R42633 dbr:RU-42,633 dbr:RU-42633 dbr:RU42633 dbr:RU_42,633 dbr:RU_42633 dbr:R_42,633 dbr:R_42633 wikipedia-en:Metapristone dbr:Metapristone#this
depiction
described by	https://covidontheweb.inria.fr:4443/about/id/entity/http/dbpedia.org/resource/Category:Antiprogestogens https://covidontheweb.inria.fr:4443/about/id/entity/http/dbpedia.org/resource/Metabolite https://covidontheweb.inria.fr:4443/about/id/entity/http/dbpedia.org/resource/Enzyme
subject	dbc:Alkyne_derivatives Experimental cancer drugs Antiprogestogens Human drug metabolites Abortifacients Anilines Antiglucocorticoids dbc:Selective_progesterone_receptor_modulators dbc:Estranes
dbo:wikiPageID	57740433(xsd:integer)
dbo:wikiPageRevisionID	1065441412(xsd:integer)
dbo:wikiPageWikiLink	dbr:Metastatic Cancer Liver Glucocorticoid receptor dbc:Alkyne_derivatives enzyme Progesterone receptor CYP3A4 dbr:Chemopreventive metabolite Mifepristone Demethylation Experimental cancer drugs Antiprogestogens Human drug metabolites dbr:Selective_progesterone_receptor_modulator dbr:Affinity_(pharmacology) Abortifacients Anilines Antiglucocorticoids dbc:Selective_progesterone_receptor_modulators dbc:Estranes
is primary topic of	wikipedia-en:Metapristone
wasDerivedFrom	wikipedia-en:Metapristone?oldid=1065441412&ns=0
dbo:abstract	Metapristone (developmental code name RU-42633; also known as desmethylmifepristone) is the major metabolite of mifepristone (RU-486, RU-38486) and a selective progesterone receptor modulator (SPRM) which itself was never marketed. It is formed from mifepristone in the liver by the enzyme CYP3A4 via monodemethylation, and circulates at concentrations higher than those of mifepristone. The metabolite retains partial but considerable affinity for the progesterone receptor (PR) and the glucocorticoid receptor (GR) (RBA = 21% and 61% of that of mifepristone for the human forms of these receptors, respectively). On the basis of actions that are apparently independent of its hormonal activity, metapristone is being researched as a potential cancer metastatic chemopreventive agent.
dbo:thumbnail	wiki-commons:Special:FilePath/Metapristone.svg?width=300
dbp:c	28(xsd:integer)
dbp:h	33(xsd:integer)
dbp:n	1(xsd:integer)
dbp:width	225(xsd:integer)
dbp:casNumber	104004(xsd:integer)
dbp:chembl	1608(xsd:integer)
dbp:chemspiderid	8246002(xsd:integer)
dbp:iupacName	-17(xsd:integer)
dbp:o	2(xsd:integer)
dbp:pubchem	10070462(xsd:integer)
dbp:smiles	CC#C[C@@]1O
dbp:stdinchi	1(xsd:integer)
dbp:stdinchikey	IBLXOBHABOVXDY-WKWWZUSTSA-N
dbp:synonyms	RU-42633; Desmethylmifepristone; 17β-Hydroxy-11β-[4-phenyl]-17α-estra-4,9-dien-3-one
dbp:unii	K1P8OGJ86J
dbo:casNumber	104004-96-8
dbo:chEMBL	1608
dbo:fdaUniiCode	K1P8OGJ86J
dbo:pubchem	10070462
dbo:wikiPageLength	5523(xsd:integer)
dbp:wikiPageUsesTemplate	dbt:Drugbox dbt:Abbrlink dbt:Progesterone_receptor_modulators dbt:Reflist dbt:Genito-urinary-drug-stub dbt:Glucocorticoid_receptor_modulators dbt:Antineoplastic-drug-stub

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