Trilostane (original) (raw)
Trilostane, sold under the brand names Modrenal and Vetoryl among others, is a medication which has been used in the treatment of Cushing's syndrome, Conn's syndrome, and postmenopausal breast cancer in humans. It was withdrawn for use in humans in the United States in the 1990s but was subsequently approved for use in veterinary medicine in the 2000s to treat Cushing's syndrome in dogs. It is taken by mouth.
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| dbo:abstract | Trilostan ist der generische Name einer zur Stoffklasse der Steroide zählenden chemischen Verbindung, die in der Tiermedizin zur Behandlung einer hypophysenabhängigen Nebennierenüberfunktion eingesetzt wird. Trilostan hemmt das 3β-Hydroxysteroid-Dehydrogenase-Enzymsystems und damit kompetitiv die Synthese verschiedener Steroidhormone (z. B. Kortisol und Aldosteron) in der Nebennierenrinde, ist selbst aber hormonell inaktiv. Der Arzneistoff ist gut verträglich und wirkt sehr sicher, schnell und reversibel. Die Nebenwirkungen sind deutlich geringer als bei Mitotan. Die Biotransformation erfolgt in der Leber. Die Plasmahalbwertszeit beträgt acht Stunden. Es wird zur Behandlung des Cushing Syndroms bei Hunden (Canines Cushing-Syndrom) und Pferden (Equines Cushing-Syndrom, ECS) sowie der Alopecia X bei einigen Hunderassen eingesetzt. (de) Trilostane, sold under the brand names Modrenal and Vetoryl among others, is a medication which has been used in the treatment of Cushing's syndrome, Conn's syndrome, and postmenopausal breast cancer in humans. It was withdrawn for use in humans in the United States in the 1990s but was subsequently approved for use in veterinary medicine in the 2000s to treat Cushing's syndrome in dogs. It is taken by mouth. (en) トリロスタン（Trilostane）は、ヒトのクッシング症候群、コン症候群、閉経後乳癌などの治療に使用されてきた医薬品である。米国では1990年代にヒトへの使用が中止されたが、その後、2000年代にイヌのクッシング症候群の治療薬として獣医学的に使用が承認された。日本では2021年現在でもヒトへの使用が認められている。投与方法は、経口投与である。 (ja) Il trilostano è un inibitore della steroidogenesi adrenocorticale. Il farmaco inibisce l'enzima progesterone reduttasi, essenziale per la produzione di glicocorticoidi e di mineralcorticoidi, bloccando in modo competitivo e reversibile la conversione dei D5-3b-idrossisteroidi, ad esempio il pregnenolone, biologicamente inattivi, a D4-3-chetosteroidi, ad esempio il progesterone biologicamente attivi, sia nella corteccia surrenale che in altri tessuti. Il trilostano sembra essere più efficace in soggetti con ipercortisolismo piuttosto che in individui con normale attività adrenocorticale. Il farmaco determinerebbe anche una inibizione della 3 beta-idrossisteroido deidrogenasi. Nel paziente con sindrome di Cushing il trilostano generalmente riduce la secrezione, la concentrazione plasmatica e l'escrezione urinaria di cortisolo e inibisce la risposta adrenocorticale alla stimolazione da corticotropina (ACTH). Durante il trattamento con il farmaco è possibile si verifichi un aumento, dovuto ad un meccanismo di feed-back, delle concentrazioni plasmatiche di ACTH con conseguente stimolazione della steroidogenesi surrenalica. Questo meccanismo in alcuni soggetti può determinare un annullamento della inibizione della sintesi di cortisolo. (it) Trilostan (łac. Trilostanum) – organiczny związek chemiczny z grupy steroidów. Stosowany jako lek z grupy inhibitorów syntezy hormonów kory nadnerczy. (pl) |
| dbo:alternativeName | Desopan, Modrastane, Modrenal, Trilox, Vetoryl, Winstan (en) |
| dbo:casNumber | 13647-35-3 |
| dbo:chEBI | 32260 |
| dbo:chEMBL | 1200907 |
| dbo:drugbank | DB01108 |
| dbo:fdaUniiCode | L0FPV48Q5R |
| dbo:kegg | D01180 |
| dbo:pubchem | 656583 |
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| dbp:atcSuffix | CA01 (en) |
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| dbp:casNumber | 13647 (xsd:integer) |
| dbp:chebi | 32260 (xsd:integer) |
| dbp:chembl | 1200907 (xsd:integer) |
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| dbp:drugbank | DB01108 (en) |
| dbp:eliminationHalfLife | 4320.0 (dbd:second) |
| dbp:h | 27 (xsd:integer) |
| dbp:iupacName | -515 (xsd:integer) |
| dbp:iupharLigand | 6850 (xsd:integer) |
| dbp:kegg | D01180 (en) |
| dbp:legalUsComment | Veterinary use (en) |
| dbp:metabolism | dbr:Liver |
| dbp:metabolites | 17 (xsd:integer) |
| dbp:n | 1 (xsd:integer) |
| dbp:o | 3 (xsd:integer) |
| dbp:pubchem | 656583 (xsd:integer) |
| dbp:routesOfAdministration | dbr:Oral_administration |
| dbp:smiles | N#C\C4=C[C@H]5O[C@]35[C@]C4 (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | KVJXBPDAXMEYOA-CXANFOAXSA-N (en) |
| dbp:synonyms | WIN-24,540; 4α,5-Epoxy-3,17β-dihydroxy-5α-androst-2-ene-2-carbonitrile (en) |
| dbp:tradename | Desopan, Modrastane, Modrenal, Trilox, Vetoryl, Winstan (en) |
| dbp:unii | L0FPV48Q5R (en) |
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| dct:subject | dbc:Cholesterol_side-chain_cleavage_enzyme_inhibitors dbc:Androgens_and_anabolic_steroids dbc:Androstanes dbc:Antiestrogens dbc:Oxidoreductase_inhibitors dbc:Nitriles dbc:Withdrawn_drugs dbc:11β-Hydroxylase_inhibitors dbc:3β-Hydroxysteroid_dehydrogenase_inhibitors |
| gold:hypernym | dbr:Inhibitor |
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| rdfs:comment | Trilostane, sold under the brand names Modrenal and Vetoryl among others, is a medication which has been used in the treatment of Cushing's syndrome, Conn's syndrome, and postmenopausal breast cancer in humans. It was withdrawn for use in humans in the United States in the 1990s but was subsequently approved for use in veterinary medicine in the 2000s to treat Cushing's syndrome in dogs. It is taken by mouth. (en) トリロスタン（Trilostane）は、ヒトのクッシング症候群、コン症候群、閉経後乳癌などの治療に使用されてきた医薬品である。米国では1990年代にヒトへの使用が中止されたが、その後、2000年代にイヌのクッシング症候群の治療薬として獣医学的に使用が承認された。日本では2021年現在でもヒトへの使用が認められている。投与方法は、経口投与である。 (ja) Trilostan (łac. Trilostanum) – organiczny związek chemiczny z grupy steroidów. Stosowany jako lek z grupy inhibitorów syntezy hormonów kory nadnerczy. (pl) Trilostan ist der generische Name einer zur Stoffklasse der Steroide zählenden chemischen Verbindung, die in der Tiermedizin zur Behandlung einer hypophysenabhängigen Nebennierenüberfunktion eingesetzt wird. Trilostan hemmt das 3β-Hydroxysteroid-Dehydrogenase-Enzymsystems und damit kompetitiv die Synthese verschiedener Steroidhormone (z. B. Kortisol und Aldosteron) in der Nebennierenrinde, ist selbst aber hormonell inaktiv. Der Arzneistoff ist gut verträglich und wirkt sehr sicher, schnell und reversibel. Die Nebenwirkungen sind deutlich geringer als bei Mitotan. (de) Il trilostano è un inibitore della steroidogenesi adrenocorticale. Il farmaco inibisce l'enzima progesterone reduttasi, essenziale per la produzione di glicocorticoidi e di mineralcorticoidi, bloccando in modo competitivo e reversibile la conversione dei D5-3b-idrossisteroidi, ad esempio il pregnenolone, biologicamente inattivi, a D4-3-chetosteroidi, ad esempio il progesterone biologicamente attivi, sia nella corteccia surrenale che in altri tessuti. Il trilostano sembra essere più efficace in soggetti con ipercortisolismo piuttosto che in individui con normale attività adrenocorticale. Il farmaco determinerebbe anche una inibizione della 3 beta-idrossisteroido deidrogenasi. (it) |
| rdfs:label | Trilostan (de) Trilostano (it) トリロスタン (ja) Trilostan (pl) Trilostane (en) |
| owl:sameAs | freebase:Trilostane http://www4.wiwiss.fu-berlin.de/drugbank/resource/drugs/DB01108 yago-res:Trilostane wikidata:Trilostane dbpedia-de:Trilostane dbpedia-it:Trilostane dbpedia-ja:Trilostane dbpedia-pl:Trilostane dbpedia-sh:Trilostane dbpedia-sr:Trilostane https://global.dbpedia.org/id/547oE |
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| is dbo:wikiPageRedirects of | dbr:Desopan dbr:ATC_code_H02CA01 dbr:ATCvet_code_QH02CA01 dbr:Modrastane dbr:Modrenal dbr:Vetoryl dbr:Trilox dbr:Winstan |
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| is owl:differentFrom of | dbr:Stanozolol |
| is foaf:primaryTopic of | wikipedia-en:Trilostane |
