EPI-001 (original) (raw)
EPI-001 is the first inhibitor of the androgen receptor amino-terminal domain. The single stereoisomer of EPI-001, EPI-002, is a first-in-class drug that the USAN council assigned a new stem class "-aniten" and the generic name "ralaniten". This distinguishes the anitens novel molecular mechanism from anti androgens that bind the C-terminus ligand-binding domain and have the stem class "lutamide" (such as flutamide, nilutamide, bicalutamide, enzalutamide, etc.). EPI-001 and its stereoisomers and analogues were discovered by Marianne Sadar and Raymond Andersen, who co-founded the pharmaceutical company ESSA Pharma Inc (Vancouver, Canada) for the clinical development of anitens for the treatment of castration-resistant prostate cancer (CRPC).
| Property | Value |
|---|---|
| dbo:abstract | EPI-001 is the first inhibitor of the androgen receptor amino-terminal domain. The single stereoisomer of EPI-001, EPI-002, is a first-in-class drug that the USAN council assigned a new stem class "-aniten" and the generic name "ralaniten". This distinguishes the anitens novel molecular mechanism from anti androgens that bind the C-terminus ligand-binding domain and have the stem class "lutamide" (such as flutamide, nilutamide, bicalutamide, enzalutamide, etc.). EPI-001 and its stereoisomers and analogues were discovered by Marianne Sadar and Raymond Andersen, who co-founded the pharmaceutical company ESSA Pharma Inc (Vancouver, Canada) for the clinical development of anitens for the treatment of castration-resistant prostate cancer (CRPC). EPI-001 is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice variants (IC50 for inhibition of AR NTD transactivation ≈ 6 μM). This is different from all currently-used antiandrogens, which, conversely, bind to the C-terminal ligand-binding domain (LBD) of the AR and competitively block binding and activation of the receptor by androgens. Due to its unique mechanism of action, EPI-001 type compounds may prove to be effective in the treatment of advanced prostate cancer resistant to conventional antiandrogens such as enzalutamide. EPI-001's successor, ralaniten acetate (EPI-506), a prodrug of ralaniten (EPI-002), one of the four stereoisomers of EPI-001, was under clinical investigation in a phase I study. EPI-506 was the first drug that directly binds to an intrinsically disordered region to be tested in humans and marks a leap in drug development from folded drug targets. (en) |
| dbo:casNumber | 227947-06-0 |
| dbo:class | dbr:Nonsteroidal_antiandrogen |
| dbo:pubchem | 4166922 |
| dbo:thumbnail | wiki-commons:Special:FilePath/EPI-001.svg?width=300 |
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| dbo:wikiPageLength | 12457 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1094353797 (xsd:integer) |
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| dbp:atcPrefix | None (en) |
| dbp:c | 21 (xsd:integer) |
| dbp:casNumber | 227947 (xsd:integer) |
| dbp:chemspiderid | 3378517 (xsd:integer) |
| dbp:cl | 1 (xsd:integer) |
| dbp:class | dbr:Nonsteroidal_antiandrogen |
| dbp:h | 27 (xsd:integer) |
| dbp:iupacName | 3 (xsd:integer) |
| dbp:o | 5 (xsd:integer) |
| dbp:pubchem | 4166922 (xsd:integer) |
| dbp:smiles | ClCCCOc1cccCC (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | HDTYUHNZRYZEEB-UHFFFAOYSA-N (en) |
| dbp:width | 250 (xsd:integer) |
| dbp:wikiPageUsesTemplate | dbt:Androgen_receptor_modulators dbt:Drugbox dbt:PPAR_modulators dbt:Reflist dbt:Short_description dbt:Cascite dbt:Androgens_and_antiandrogens |
| dcterms:subject | dbc:Glycerols dbc:Abandoned_drugs dbc:Alkylating_agents dbc:Halohydrins dbc:Organochlorides dbc:Triols dbc:Nonsteroidal_antiandrogens dbc:PPAR_agonists dbc:2,2-Bis(4-hydroxyphenyl)propanes |
| gold:hypernym | dbr:Antiandrogen |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 yago:WikicatMolecularFormulas yago:Abstraction100002137 yago:Agent114778436 yago:Antineoplastic102722458 yago:CausalAgent100007347 yago:Communication100033020 yago:CytotoxicDrug103157987 yago:Drug103247620 yago:Formula106816935 yago:Matter100020827 yago:Medicine103740161 yago:Message106598915 yago:MolecularFormula106817173 yago:PhysicalEntity100001930 dbo:Drug yago:Statement106722453 yago:Substance100020090 yago:WikicatExperimentalCancerDrugs |
| rdfs:comment | EPI-001 is the first inhibitor of the androgen receptor amino-terminal domain. The single stereoisomer of EPI-001, EPI-002, is a first-in-class drug that the USAN council assigned a new stem class "-aniten" and the generic name "ralaniten". This distinguishes the anitens novel molecular mechanism from anti androgens that bind the C-terminus ligand-binding domain and have the stem class "lutamide" (such as flutamide, nilutamide, bicalutamide, enzalutamide, etc.). EPI-001 and its stereoisomers and analogues were discovered by Marianne Sadar and Raymond Andersen, who co-founded the pharmaceutical company ESSA Pharma Inc (Vancouver, Canada) for the clinical development of anitens for the treatment of castration-resistant prostate cancer (CRPC). (en) |
| rdfs:label | EPI-001 (en) |
| owl:sameAs | freebase:EPI-001 yago-res:EPI-001 wikidata:EPI-001 dbpedia-sh:EPI-001 dbpedia-sr:EPI-001 https://global.dbpedia.org/id/Xmj2 |
| prov:wasDerivedFrom | wikipedia-en:EPI-001?oldid=1094353797&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/EPI-001.svg |
| foaf:isPrimaryTopicOf | wikipedia-en:EPI-001 |
| is dbo:wikiPageWikiLink of | dbr:Bisphenol_A dbr:Bisphenol_A_diglycidyl_ether dbr:Androgen_receptor dbr:EPI-7386 dbr:Antiandrogen dbr:Nonsteroidal dbr:C21H27ClO5 dbr:N-Terminal_domain_antiandrogen dbr:Selective_PPAR_modulator dbr:Ralaniten dbr:Ralaniten_acetate |
| is foaf:primaryTopic of | wikipedia-en:EPI-001 |
