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

General Information of Drug (ID: DM6C8K1)

• Drug Name: [4Aph(CO-NH-OCH3)5]degarelix Drug Info
• Synonyms: CHEMBL407661; [4Aph(CO-NH-OCH3)5]degarelix

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 16155587
  TTD Drug ID: DM6C8K1

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gonadorelin	DMAQ469	Amenorrhea	GA20.0	Approved	[2]
Relugolix	DMK7IWL	Prostate cancer	2C82.0	Approved	[3]
Ganirelix	DMGMB30	Ovulation dysfunction	5A80	Approved	[4]
Abarelix	DM5WFNP	Prostate cancer	2C82.0	Approved	[5]
Triptorelin	DMTK4LS	Infertility	GB04	Approved	[6]
Leuprorelin acetate	DM15HAT	Prostate cancer	2C82.0	Approved	[7]
Nafarelin	DMAHEFY	Endometriosis	GA10	Approved	[8]
Cetrorelix	DMFD9Q6	Ovarian stimulation	LB45.1	Approved	[9]
Elagolix sodium	DMRDUC0	Endometriosis	GA10	Approved	[10]
Degarelix	DM3O8QY	Prostate cancer	2C82.0	Approved	[11]

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	Inhibitor	[1]

References

• [1] Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III. J Med Chem. 2006 Jun 15;49(12):3536-43.
• [2] Use of cognitive behavior therapy for functional hypothalamic amenorrhea. Ann N Y Acad Sci. 2006 Dec;1092:114-29.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [4] 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.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [6] 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.
• [7] Clinical pipeline report, company report or official report of Takeda (2009).
• [8] 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.
• [9] 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.
• [10] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [11] 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.