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- Q21099001 subject Q7335338.
- Q21099001 subject Q8493060.
- Q21099001 subject Q8878420.
- Q21099001 subject Q8971959.
- Q21099001 subject Q9052323.
- Q21099001 abstract "Sufugolix (INN, BAN) (developmental code name TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively). It was under development by Takeda for the treatment of endometriosis and uterine leiomyoma and reached phase II clinical trials for both of these indications, but was subsequently discontinued.[1] It seems to have been supplanted by relugolix (TAK-385), which is also under development by Takeda for the treatment of these conditions and has a more favorable drug profile (including reduced cytochrome P450 inhibition and improved in vivo GnRHR antagonistic activity) in comparison.Oral administration of sufugolix at a dose of 30 mg/kg to castrated male cynomolgus monkeys resulted in nearly complete suppression of luteinizing hormone levels. The duration of action was more than 24 hours, indicating a long half-life of the drug. The suppressive effects of sufugolix on gonadotropin and sex hormone levels are rapidly reversible with discontinuation.Unlike various other GnRHR antagonists, sufugolix has been elucidated to be a non-competitive or insurmountable/trapping antagonist of the GnRHR.".
- Q21099001 atcPrefix "H01".
- Q21099001 atcSuffix "CC02".
- Q21099001 casNumber "308831-61-0".
- Q21099001 iupacName "1-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea".
- Q21099001 pubchem "3038517".
- Q21099001 thumbnail Sufugolix_structure.png?width=300.
- Q21099001 wikiPageExternalLink 800017215.
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- Q21099001 wikiPageWikiLink Q21099000.
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- Q21099001 wikiPageWikiLink Q725307.
- Q21099001 wikiPageWikiLink Q7335338.
- Q21099001 wikiPageWikiLink Q824258.
- Q21099001 wikiPageWikiLink Q8493060.
- Q21099001 wikiPageWikiLink Q8878420.
- Q21099001 wikiPageWikiLink Q8971959.
- Q21099001 wikiPageWikiLink Q899107.
- Q21099001 wikiPageWikiLink Q9052323.
- Q21099001 wikiPageWikiLink Q918753.
- Q21099001 wikiPageWikiLink Q9635.
- Q21099001 atcPrefix "H01".
- Q21099001 atcSuffix "CC02".
- Q21099001 casNumber "308831".
- Q21099001 iupacName "1".
- Q21099001 pubchem "3038517".
- Q21099001 type ChemicalSubstance.
- Q21099001 type Drug.
- Q21099001 type ChemicalObject.
- Q21099001 type Thing.
- Q21099001 type Q8386.
- Q21099001 comment "Sufugolix (INN, BAN) (developmental code name TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively).".
- Q21099001 label "Sufugolix".
- Q21099001 depiction Sufugolix_structure.png.