Onapristone (original) (raw)
Onapristone (INN) (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a silent antagonist of the progesterone receptor (PR), in contrast to the related antiprogestogen mifepristone (which is a weak partial agonist of the receptor). Moreover, compared to mifepristone, onapristone has reduced antiglucocorticoid activity, shows little antiandrogenic activity, and has 10- to 30-fold greater potency as an antiprogestogen. The medication was under development for clinical use, for instance in the treatment of breast cancer and as an endometrial contraceptive, but was discontinued during phase III clinical trials in 1995 due to findin
| Property | Value |
|---|---|
| dbo:abstract | Onapristone (INN) (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a silent antagonist of the progesterone receptor (PR), in contrast to the related antiprogestogen mifepristone (which is a weak partial agonist of the receptor). Moreover, compared to mifepristone, onapristone has reduced antiglucocorticoid activity, shows little antiandrogenic activity, and has 10- to 30-fold greater potency as an antiprogestogen. The medication was under development for clinical use, for instance in the treatment of breast cancer and as an endometrial contraceptive, but was discontinued during phase III clinical trials in 1995 due to findings that liver function abnormalities developed in a majority patients. Onapristone has been found to be effective in the treatment of breast cancer. As of 2016, onapristone has re-emerged and is under development for the treatment of prostate cancer, currently in phase II clinical trials. It was also under development for the treatment of endometrial cancer, breast cancer, ovarian cancer, and uterine cancer, but was discontinued for these indications in favor of focusing on prostate cancer. (en) |
| dbo:casNumber | 96346-61-1 |
| dbo:chEMBL | 1908373 |
| dbo:class | dbr:Antiprogestogen |
| dbo:fdaUniiCode | H6H7G23O3N |
| dbo:kegg | D09571 |
| dbo:pubchem | 5311505 |
| dbo:thumbnail | wiki-commons:Special:FilePath/Onapristone.svg?width=300 |
| dbo:wikiPageID | 53979431 (xsd:integer) |
| dbo:wikiPageLength | 7811 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1082622911 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Potency_(pharmacology) dbr:Endometrium dbr:Partial_agonist dbr:Breast_cancer dbr:Antiglucocorticoid dbr:Antiprogestogen dbr:Lilopristone dbr:List_of_investigational_sex-hormonal_agents dbc:Dimethylamino_compounds dbc:Enones dbc:Estranes dbr:Endometrial_cancer dbc:Antiglucocorticoids dbc:Experimental_cancer_drugs dbr:Antiandrogen dbr:Liver dbr:Steroid dbr:Clinical_trial dbr:Progesterone_receptor dbr:Prostate_cancer dbc:1-Ethylcyclopentanols dbr:Aglepristone dbc:Antiprogestogens dbr:Receptor_(biochemistry) dbc:Antineoplastic_drugs dbr:Telapristone dbr:Uterine_cancer dbc:Abortifacients dbr:Mifepristone dbr:Schering_AG dbr:Phases_of_clinical_research dbr:Toripristone dbr:Ovarian_cancer dbr:Synthetic_compound dbr:Silent_antagonist dbr:Hormonal_contraceptive |
| dbp:c | 29 (xsd:integer) |
| dbp:casNumber | 96346 (xsd:integer) |
| dbp:chembl | 1908373 (xsd:integer) |
| dbp:chemspiderid | 4470982 (xsd:integer) |
| dbp:class | dbr:Antiprogestogen |
| dbp:h | 39 (xsd:integer) |
| dbp:iupacName | -11 (xsd:integer) |
| dbp:kegg | D09571 (en) |
| dbp:n | 1 (xsd:integer) |
| dbp:o | 3 (xsd:integer) |
| dbp:pubchem | 5311505 (xsd:integer) |
| dbp:smiles | C[C@@]12C[C@@H]C5=CC=CNC (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | IEXUMDBQLIVNHZ-YOUGDJEHSA-N (en) |
| dbp:synonyms | ZK-89299; ZK-299; AR-18; IVV-1001; 11β--17α-hydroxy-17β--13α-estra-4,9-dien-3-one (en) |
| dbp:unii | H6H7G23O3N (en) |
| dbp:width | 250 (xsd:integer) |
| dbp:wikiPageUsesTemplate | dbt:Drugbox dbt:Glucocorticoid_receptor_modulators dbt:Progesterone_receptor_modulators dbt:Reflist dbt:Short_description dbt:Abbrlink |
| dcterms:subject | dbc:Dimethylamino_compounds dbc:Enones dbc:Estranes dbc:Antiglucocorticoids dbc:Experimental_cancer_drugs dbc:1-Ethylcyclopentanols dbc:Antiprogestogens dbc:Antineoplastic_drugs dbc:Abortifacients |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | Onapristone (INN) (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a silent antagonist of the progesterone receptor (PR), in contrast to the related antiprogestogen mifepristone (which is a weak partial agonist of the receptor). Moreover, compared to mifepristone, onapristone has reduced antiglucocorticoid activity, shows little antiandrogenic activity, and has 10- to 30-fold greater potency as an antiprogestogen. The medication was under development for clinical use, for instance in the treatment of breast cancer and as an endometrial contraceptive, but was discontinued during phase III clinical trials in 1995 due to findin (en) |
| rdfs:label | Onapristone (en) |
| owl:sameAs | yago-res:Onapristone wikidata:Onapristone https://global.dbpedia.org/id/2Y9ah |
| prov:wasDerivedFrom | wikipedia-en:Onapristone?oldid=1082622911&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/Onapristone.svg |
| foaf:isPrimaryTopicOf | wikipedia-en:Onapristone |
| is dbo:wikiPageRedirects of | dbr:ZK-299 dbr:ZK-89,299 dbr:ZK-89299 dbr:ZK299 dbr:ZK89299 dbr:ZK_299 dbr:ZK_89,299 dbr:ZK_89299 |
| is dbo:wikiPageWikiLink of | dbr:Antiprogestogen dbr:Lilopristone dbr:List_of_investigational_sex-hormonal_agents dbr:Progesterone_receptor dbr:Aglepristone dbr:Lonaprisan dbr:Telapristone dbr:Sex-hormonal_agent dbr:Toripristone dbr:Vilaprisan dbr:List_of_drugs:_O–Op dbr:ZK-299 dbr:ZK-89,299 dbr:ZK-89299 dbr:ZK299 dbr:ZK89299 dbr:ZK_299 dbr:ZK_89,299 dbr:ZK_89299 |
| is foaf:primaryTopic of | wikipedia-en:Onapristone |
