Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMB2C0E)

• Drug Name: Elagolix Drug Info
• Synonyms: Elagolix; 834153-87-6; UNII-5B2546MB5Z; NBI-56418; 5B2546MB5Z; NBI56418; NBI 56418; Elagolix [USAN:INN]; Orilissa; ELA gOLIX; Elagolix (USAN/INN); SCHEMBL1642523; GTPL8362; CHEMBL1208155; DTXSID40232348; ABT-620; 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6-dioxopyrimidin-1-yl]-1-phenylethyl]amino]butanoic acid; EX-A1765; BCP08827; ZINC49888891; CS-5329; SB16700; DB11979; compound 10b [PMID 19006286]; HY-14789; AN-27202; D09335; Z-3253; 153E876; Butanoic acid, 4-(((1R)-2-(5-(2-flu

Indication

Disease Entry	ICD 11	Status	REF
Uterine fibroids	2E86.0	Phase 3	[1] , [2]

• Cross-matching ID:
  PubChem CID: 11250647
  CAS Number: CAS 834153-87-6
  TTD Drug ID: DMB2C0E

Molecule-Related Drug Atlas

Drug(s) Targeting Gonadotropin-releasing hormone receptor (GNRHR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gonadorelin	DMAQ469	Hypothalamic hypogonadism	5A61.2	Approved	[4]
Relugolix	DMK7IWL	Prostate cancer	2C82.0	Approved	[5]
Ganirelix	DMGMB30	Ovulation dysfunction	5A80	Approved	[6]
Abarelix	DM5WFNP	Prostate cancer	2C82.0	Approved	[7]
Triptorelin	DMTK4LS	Solid tumour/cancer	2A00-2F9Z	Approved	[8]
Leuprorelin acetate	DM15HAT	Prostate cancer	2C82.0	Approved	[9]
Nafarelin	DMAHEFY	Endometriosis	GA10	Approved	[10]
Cetrorelix	DMFD9Q6	Ovarian stimulation	LB45.1	Approved	[11]
Elagolix sodium	DMRDUC0	Endometriosis	GA10	Approved	[12]
Degarelix	DM3O8QY	Prostate cancer	2C82.0	Approved	[13]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gonadotropin-releasing hormone receptor (GNRHR)	TT8R70G	GNRHR_HUMAN	Antagonist	[3]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8362).
• [2] ClinicalTrials.gov (NCT01620528) A Clinical Study to Evaluate the Safety and Efficacy of Elagolix in Subjects With Moderate to Severe Endometriosis-Associated Pain. U.S. National Institutes of Health.
• [3] Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain. Womens Health (Lond Engl). 2015 Jan;11(1):19-28.
• [4] Use of cognitive behavior therapy for functional hypothalamic amenorrhea. Ann N Y Acad Sci. 2006 Dec;1092:114-29.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [6] Age attenuates testosterone secretion driven by amplitude-varying pulses of recombinant human luteinizing hormone during acute gonadotrope inhibiti... J Clin Endocrinol Metab. 2007 Sep;92(9):3626-32.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [8] Regulation of GnRH I receptor gene expression by the GnRH agonist triptorelin, estradiol, and progesterone in the gonadotroph-derived cell line alphaT3-1. Endocrine. 2006 Aug;30(1):139-44.
• [9] Clinical pipeline report, company report or official report of Takeda (2009).
• [10] Reversible downregulation of endocrine and germinative testicular function (hormonal castration) in the dog with the GnRH-agonist azagly-nafarelin ... Theriogenology. 2009 Apr 15;71(7):1037-45.
• [11] Gonadotropin releasing hormone analogs induce apoptosis by extrinsic pathway involving p53 phosphorylation in primary cell cultures of human prostatic adenocarcinomas. Prostate. 2009 Jul 1;69(10):1025-33.
• [12] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [13] Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II. J Med Chem. 2005 Jul 28;48(15):4851-60.