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- Relugolix abstract "Relugolix (INN) (developmental code name TAK-385) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.12 nM) that is under development for clinical use by Takeda. It is currently in phase II clinical trials for the treatment of endometriosis, uterine leiomyoma, and prostate cancer.A single oral administration of relugolix at a dose of 3 mg/kg has been found to suppress luteinizing hormone levels for more than 24 hours in castrated cynomolgus monkeys, indicating a long duration of action. The drug (80–160 mg/day) has been found to reduce testosterone levels to sustained castrate levels in men with once-daily chronic administration. Lower dosages (10–40 mg/day) are being studied in the treatment of endometriosis and uterine leiomyoma to achieve partial sex hormone suppression. The reasoning behind partial suppression for these conditions is to reduce the incidence and severity of menopausal symptoms such as hot flushes and to avoid bone mineral density changes caused by estrogen deficiency that can eventually lead to osteoporosis.".
- Relugolix atcPrefix "H01".
- Relugolix atcSuffix "CC02".
- Relugolix casNumber "737789-87-6".
- Relugolix iupacName "1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea".
- Relugolix pubchem "10348973".
- Relugolix thumbnail Relugolix_structure.png?width=300.
- Relugolix wikiPageExternalLink 800028257.
- Relugolix wikiPageID "48188195".
- Relugolix wikiPageLength "6671".
- Relugolix wikiPageOutDegree "33".
- Relugolix wikiPageRevisionID "697285446".
- Relugolix wikiPageWikiLink Bioavailability.
- Relugolix wikiPageWikiLink Bone_density.
- Relugolix wikiPageWikiLink Castration.
- Relugolix wikiPageWikiLink Category:Amines.
- Relugolix wikiPageWikiLink Category:GnRH_antagonists.
- Relugolix wikiPageWikiLink Category:Ketones.
- Relugolix wikiPageWikiLink Category:Organofluorides.
- Relugolix wikiPageWikiLink Category:Pyridazines.
- Relugolix wikiPageWikiLink Category:Pyrimidines.
- Relugolix wikiPageWikiLink Category:Ureas.
- Relugolix wikiPageWikiLink Clinical_trial.
- Relugolix wikiPageWikiLink Crab-eating_macaque.
- Relugolix wikiPageWikiLink Elagolix.
- Relugolix wikiPageWikiLink Endometriosis.
- Relugolix wikiPageWikiLink Estrogen.
- Relugolix wikiPageWikiLink Gonadotropin-releasing_hormone_receptor.
- Relugolix wikiPageWikiLink Hot_flash.
- Relugolix wikiPageWikiLink IC50.
- Relugolix wikiPageWikiLink International_nonproprietary_name.
- Relugolix wikiPageWikiLink Luteinizing_hormone.
- Relugolix wikiPageWikiLink Menopause.
- Relugolix wikiPageWikiLink Mouth.
- Relugolix wikiPageWikiLink Osteoporosis.
- Relugolix wikiPageWikiLink Pharmacodynamics.
- Relugolix wikiPageWikiLink Phases_of_clinical_research.
- Relugolix wikiPageWikiLink Prostate_cancer.
- Relugolix wikiPageWikiLink Receptor_antagonist.
- Relugolix wikiPageWikiLink Sex_steroid.
- Relugolix wikiPageWikiLink Small_molecule.
- Relugolix wikiPageWikiLink Sufugolix.
- Relugolix wikiPageWikiLink Takeda.
- Relugolix wikiPageWikiLink Testosterone.
- Relugolix wikiPageWikiLink Uterine_fibroid.
- Relugolix wikiPageWikiLinkText "Relugolix".
- Relugolix wikiPageWikiLinkText "relugolix".
- Relugolix atcPrefix "H01".
- Relugolix atcSuffix "CC02".
- Relugolix c "29".
- Relugolix casNumber "737789".
- Relugolix chemspiderid "8524431".
- Relugolix f "2".
- Relugolix h "27".
- Relugolix inchi "InChI=1S/C29H27F2N7O5S/c1-3614-19-24-263829372744-2516-8-10-1732-2835-43-4/h5-13H,14-15H2,1-4H3,".
- Relugolix inchikey "AOMXMOCNKJTRQP-UHFFFAOYSA-N".
- Relugolix iupacName "1".
- Relugolix molecularWeight "623.630386".
- Relugolix n "7".
- Relugolix o "5".
- Relugolix pubchem "10348973".
- Relugolix routesOfAdministration Mouth.
- Relugolix s "1".
- Relugolix smiles "CNCC1=CC5=CC=CNCNOC".
- Relugolix synonyms "TAK-385".
- Relugolix wikiPageUsesTemplate Template:Drugbox.
- Relugolix wikiPageUsesTemplate Template:Genito-urinary-drug-stub.
- Relugolix wikiPageUsesTemplate Template:Gonadotropins_and_GnRH.
- Relugolix wikiPageUsesTemplate Template:Peptidergics.
- Relugolix wikiPageUsesTemplate Template:Reflist.
- Relugolix wikiPageUsesTemplate Template:Systemic-hormonal-drug-stub.
- Relugolix subject Category:Amines.
- Relugolix subject Category:GnRH_antagonists.
- Relugolix subject Category:Ketones.
- Relugolix subject Category:Organofluorides.
- Relugolix subject Category:Pyridazines.
- Relugolix subject Category:Pyrimidines.
- Relugolix subject Category:Ureas.
- Relugolix hypernym Antagonist.
- Relugolix type ChemicalSubstance.
- Relugolix type Drug.
- Relugolix type ChemicalObject.
- Relugolix type Thing.
- Relugolix type Q8386.
- Relugolix comment "Relugolix (INN) (developmental code name TAK-385) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.12 nM) that is under development for clinical use by Takeda.".
- Relugolix label "Relugolix".
- Relugolix sameAs Q21099000.
- Relugolix sameAs Q21099000.
- Relugolix wasDerivedFrom Relugolix?oldid=697285446.
- Relugolix depiction Relugolix_structure.png.
- Relugolix isPrimaryTopicOf Relugolix.