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- Sufugolix 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.".
- Sufugolix atcPrefix "H01".
- Sufugolix atcSuffix "CC02".
- Sufugolix casNumber "308831-61-0".
- Sufugolix 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".
- Sufugolix pubchem "3038517".
- Sufugolix thumbnail Sufugolix_structure.png?width=300.
- Sufugolix wikiPageExternalLink 800017215.
- Sufugolix wikiPageID "48188949".
- Sufugolix wikiPageLength "6620".
- Sufugolix wikiPageOutDegree "33".
- Sufugolix wikiPageRevisionID "685470036".
- Sufugolix wikiPageWikiLink Bioavailability.
- Sufugolix wikiPageWikiLink British_Approved_Name.
- Sufugolix wikiPageWikiLink Castration.
- Sufugolix wikiPageWikiLink Category:Amines.
- Sufugolix wikiPageWikiLink Category:GnRH_antagonists.
- Sufugolix wikiPageWikiLink Category:Organofluorides.
- Sufugolix wikiPageWikiLink Category:Pyrimidines.
- Sufugolix wikiPageWikiLink Category:Ureas.
- Sufugolix wikiPageWikiLink Clinical_trial.
- Sufugolix wikiPageWikiLink Crab-eating_macaque.
- Sufugolix wikiPageWikiLink Cytochrome_P450.
- Sufugolix wikiPageWikiLink Elagolix.
- Sufugolix wikiPageWikiLink Endometriosis.
- Sufugolix wikiPageWikiLink Enzyme_inhibition.
- Sufugolix wikiPageWikiLink Gonadotropin.
- Sufugolix wikiPageWikiLink Gonadotropin-releasing_hormone_antagonist.
- Sufugolix wikiPageWikiLink Gonadotropin-releasing_hormone_receptor.
- Sufugolix wikiPageWikiLink Half-life.
- Sufugolix wikiPageWikiLink IC50.
- Sufugolix wikiPageWikiLink International_nonproprietary_name.
- Sufugolix wikiPageWikiLink Ligand_(biochemistry).
- Sufugolix wikiPageWikiLink Luteinizing_hormone.
- Sufugolix wikiPageWikiLink Mouth.
- Sufugolix wikiPageWikiLink Non-competitive_antagonist.
- Sufugolix wikiPageWikiLink Pharmacodynamics.
- Sufugolix wikiPageWikiLink Phases_of_clinical_research.
- Sufugolix wikiPageWikiLink Receptor_antagonist.
- Sufugolix wikiPageWikiLink Relugolix.
- Sufugolix wikiPageWikiLink Sex_steroid.
- Sufugolix wikiPageWikiLink Small_molecule.
- Sufugolix wikiPageWikiLink Takeda.
- Sufugolix wikiPageWikiLink Uterine_fibroid.
- Sufugolix wikiPageWikiLinkText "Sufugolix".
- Sufugolix wikiPageWikiLinkText "sufugolix".
- Sufugolix atcPrefix "H01".
- Sufugolix atcSuffix "CC02".
- Sufugolix c "36".
- Sufugolix casNumber "308831".
- Sufugolix chemspiderid "2302081".
- Sufugolix f "2".
- Sufugolix h "31".
- Sufugolix inchi "InChI=1S/C36H31F2N5O4S/c1-4121-28-31-334336423448-3224-16-18-2539-3540-47-2/h3-19H,20-22H2,1-2H3,".
- Sufugolix inchikey "UCQSBGOFELXYIN-UHFFFAOYSA-N".
- Sufugolix iupacName "1".
- Sufugolix molecularWeight "667.724246".
- Sufugolix n "5".
- Sufugolix o "4".
- Sufugolix pubchem "3038517".
- Sufugolix routesOfAdministration Mouth.
- Sufugolix s "1".
- Sufugolix smiles "CNCC2=CC6=CC=CNCNOC".
- Sufugolix synonyms "TAK-013".
- Sufugolix wikiPageUsesTemplate Template:Drugbox.
- Sufugolix wikiPageUsesTemplate Template:Genito-urinary-drug-stub.
- Sufugolix wikiPageUsesTemplate Template:Gonadotropins_and_GnRH.
- Sufugolix wikiPageUsesTemplate Template:Peptidergics.
- Sufugolix wikiPageUsesTemplate Template:Reflist.
- Sufugolix wikiPageUsesTemplate Template:Systemic-hormonal-drug-stub.
- Sufugolix subject Category:Amines.
- Sufugolix subject Category:GnRH_antagonists.
- Sufugolix subject Category:Organofluorides.
- Sufugolix subject Category:Pyrimidines.
- Sufugolix subject Category:Ureas.
- Sufugolix hypernym Antagonist.
- Sufugolix type ChemicalSubstance.
- Sufugolix type Drug.
- Sufugolix type ChemicalObject.
- Sufugolix type Thing.
- Sufugolix type Q8386.
- Sufugolix 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).".
- Sufugolix label "Sufugolix".
- Sufugolix sameAs Q21099001.
- Sufugolix sameAs Q21099001.
- Sufugolix wasDerivedFrom Sufugolix?oldid=685470036.
- Sufugolix depiction Sufugolix_structure.png.
- Sufugolix isPrimaryTopicOf Sufugolix.