Encenicline (original) (raw)
エンセニクリン（Encenicline、開発コードMT-4666）は選択的α7ニコチン受容体部分作動薬である。統合失調症等における認識機能障害の治療薬として第III相臨床試験が実施されている。消化器系の重篤な副作用が発生してアルツハイマー型認知症の国際共同治験に米国FDAが実施保留命令を下した事から、同治験への日本からの参加が中止された。日本で進行中の第II相臨床試験は薬剤の投与が終了しており、開発が継続される可能性がある。
| Property | Value |
|---|---|
| dbo:abstract | Encenicline (INN, USAN, code names EVP-6124, MT-4666) is a selective partial agonist of the α7 nicotinic receptor. It was in phase III clinical trials for the treatment of cognitive impairment in schizophrenia, but failed to meet the study endpoints in 2016. FORUM Pharmaceuticals, who currently is subjecting the drug to the FDA approval process, had all studies suspended until further notice in fall of 2015 due to rare, but serious gastrointestinal problems occurring in patients participating in the drug trial, potentially being a consequence of taking the drug. The trials were scheduled to be run until January 2017, but as of December 2016, they appear to still be on hold. There is speculation by FORUM Pharmaceuticals that this may be due to either the increased daily dose given in the phase III trial compared to earlier trials that showed promise. In previous trials, the highest dose given was 2 mg/day, with the most positive of effects having been realized in patients taking the largest dose (2 mg/day). In the phase III trial, all patients were treated with 3 mg/day doses of the drug. FORUM also speculates that the increase of gastrointestinal problems occurring in the phase III trial could be due to the increased demographic risk that elderly (the average age in the study was 75) and those with Alzheimer's disease have in regard to gastrointestinal issues, citing another study they conducted with a younger demographic (in which the average age was 35–40) for the treatment of schizophrenia of 1,500 individuals in which there were zero complains of gastrointestinal problems. (en) エンセニクリン（Encenicline、開発コードMT-4666）は選択的α7ニコチン受容体部分作動薬である。統合失調症等における認識機能障害の治療薬として第III相臨床試験が実施されている。消化器系の重篤な副作用が発生してアルツハイマー型認知症の国際共同治験に米国FDAが実施保留命令を下した事から、同治験への日本からの参加が中止された。日本で進行中の第II相臨床試験は薬剤の投与が終了しており、開発が継続される可能性がある。 (ja) |
| dbo:casNumber | 550999-75-2 |
| dbo:chEMBL | 2151572 |
| dbo:fdaUniiCode | 5FI5376A0X |
| dbo:kegg | D10626 |
| dbo:pubchem | 46196517 |
| dbo:thumbnail | wiki-commons:Special:FilePath/Encenicline.svg?width=300 |
| dbo:wikiPageExternalLink | http://www.forumpharma.com/content/innovation-pipeline/a7-receptor-agonists |
| dbo:wikiPageID | 46398248 (xsd:integer) |
| dbo:wikiPageLength | 5410 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1121012321 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Schizophrenia dbr:Partial_agonist dbr:Bradanicline dbr:International_nonproprietary_name dbc:Chloroarenes dbc:Experimental_drugs dbc:Stimulants dbr:SSR-180,711 dbr:GTS-21 dbr:Phase_III_clinical_trials dbr:Clinical_trial dbr:AR-R17779 dbc:Carboxamides dbc:Nootropics dbr:Alpha-7_nicotinic_receptor dbr:PHA-543,613 dbr:PNU-282,987 dbc:Nicotinic_agonists dbc:Benzothiophenes dbr:TC-1698 dbr:United_States_Adopted_Name dbr:WAY-317,538 dbr:Cognitive_impairment |
| dbp:atcPrefix | None (en) |
| dbp:c | 16 (xsd:integer) |
| dbp:casNumber | 550999 (xsd:integer) |
| dbp:chembl | 2151572 (xsd:integer) |
| dbp:chemspiderid | 28637768 (xsd:integer) |
| dbp:cl | 1 (xsd:integer) |
| dbp:h | 17 (xsd:integer) |
| dbp:iupacName | N-[-1-Azabicyclo[2.2.2]oct-3-yl]-7-chloro-1-benzothiophene-2-carboxamide (en) |
| dbp:kegg | D10626 (en) |
| dbp:n | 2 (xsd:integer) |
| dbp:o | 1 (xsd:integer) |
| dbp:pubchem | 46196517 (xsd:integer) |
| dbp:s | 1 (xsd:integer) |
| dbp:smiles | c1cc2ccCN[C@H]3CN4CCC3CC4 (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | SSRDSYXGYPJKRR-ZDUSSCGKSA-N (en) |
| dbp:unii | 5 (xsd:integer) |
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| dct:subject | dbc:Chloroarenes dbc:Experimental_drugs dbc:Stimulants dbc:Carboxamides dbc:Nootropics dbc:Nicotinic_agonists dbc:Benzothiophenes |
| gold:hypernym | dbr:Agonist |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | エンセニクリン（Encenicline、開発コードMT-4666）は選択的α7ニコチン受容体部分作動薬である。統合失調症等における認識機能障害の治療薬として第III相臨床試験が実施されている。消化器系の重篤な副作用が発生してアルツハイマー型認知症の国際共同治験に米国FDAが実施保留命令を下した事から、同治験への日本からの参加が中止された。日本で進行中の第II相臨床試験は薬剤の投与が終了しており、開発が継続される可能性がある。 (ja) Encenicline (INN, USAN, code names EVP-6124, MT-4666) is a selective partial agonist of the α7 nicotinic receptor. It was in phase III clinical trials for the treatment of cognitive impairment in schizophrenia, but failed to meet the study endpoints in 2016. (en) |
| rdfs:label | Encenicline (en) エンセニクリン (ja) |
| owl:sameAs | freebase:Encenicline yago-res:Encenicline wikidata:Encenicline dbpedia-ja:Encenicline https://global.dbpedia.org/id/uMnk |
| prov:wasDerivedFrom | wikipedia-en:Encenicline?oldid=1121012321&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/Encenicline.svg |
| foaf:isPrimaryTopicOf | wikipedia-en:Encenicline |
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