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

General Information of Drug (ID: DM4MTPU)

Drug Name

NBI-42902 Drug Info

Synonyms

352290-60-9; UNII-3FWQ4MD98O; 3FWQ4MD98O; CHEMBL179691; NBI42902; GTPL1187; GTPL1178; SCHEMBL5758034; ZINC6716969; BDBM50162007; NBI 42902; API0005260; 2,4(1H,3H)-Pyrimidinedione, 3-((2R)-2-amino-2-phenylethyl)-1-((2,6-difluorophenyl)methyl)-5-(2-fluoro-3-methoxyphenyl)-6-methyl-; KB-138000; FT-0771447; 3-[(2R)-2-amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione

Indication

Disease Entry	ICD 11	Status	REF
Prostate cancer	2C82.0	Discontinued in Phase 1	[1]

Cross-matching ID

PubChem CID: 11167850
CAS Number: CAS 352290-60-9
TTD Drug ID: DM4MTPU

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Download the Complete Related Drug List

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gonadorelin	DMAQ469	Amenorrhea	GA20.0	Approved	[3]
Relugolix	DMK7IWL	Prostate cancer	2C82.0	Approved	[4]
Ganirelix	DMGMB30	Ovulation dysfunction	5A80	Approved	[5]
Abarelix	DM5WFNP	Prostate cancer	2C82.0	Approved	[6]
Triptorelin	DMTK4LS	Infertility	GB04	Approved	[7]
Leuprorelin acetate	DM15HAT	Prostate cancer	2C82.0	Approved	[8]
Nafarelin	DMAHEFY	Endometriosis	GA10	Approved	[9]
Cetrorelix	DMFD9Q6	Ovarian stimulation	LB45.1	Approved	[10]
Elagolix sodium	DMRDUC0	Endometriosis	GA10	Approved	[11]
Degarelix	DM3O8QY	Prostate cancer	2C82.0	Approved	[12]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gonadotropin-releasing hormone receptor (GNRHR)	TT8R70G	GNRHR_HUMAN	Inhibitor	[2]

------------------------------------------------------------------------------------

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: 1178).
2	Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11;51(23):7478-85.
3	Use of cognitive behavior therapy for functional hypothalamic amenorrhea. Ann N Y Acad Sci. 2006 Dec;1092:114-29.
4	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
5	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.
6	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
7	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.
8	Clinical pipeline report, company report or official report of Takeda (2009).
9	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.
10	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.
11	2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
12	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.