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

General Information of Drug (ID: DMC6EFI)

• Drug Name: Elinzanetant Drug Info
• Synonyms: Elinzanetant; 929046-33-3; NT-814; UNII-NZW2BOW35N; BAY3427080; Elinzanetant [INN]; Elinzanetant [USAN]; NZW2BOW35N; BAY-3427080; N-[6-[(7S,9aS)-7-(hydroxymethyl)-3,4,6,7,9,9a-hexahydro-1H-pyrazino[2,1-c][1,4]oxazin-8-yl]-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethylpropanamide; 2-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-N-(4-(4-FLUORO-2-METHYLPHENYL)-6-((7S,9AS)-7-(HYDROXYMETHYL)HEXAHYDROPYRAZINO(2,1-C)(1,4)OXAZIN-8(1H)-YL)-3-PYRIDINYL)-N,2-DIMETHYLPROPANAMIDE; 2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide; Elinzanetant [USAN:INN]; ELINZANETANT [WHO-DD]; SCHEMBL303180; CHEMBL4802157; GTPL12691; DTXSID101337049; NT814; EX-A6225; WHO 10952; AKOS040756249; Compound A [WO2021094247A1]; MS-31047; Example 34 [WO2007028654A1]; HY-109171; CS-0116361; 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]pyridin-3-yl}-N,2-dimethylpropanamide; BENZAMIDE, 3-(5-METHYL-2-TBENZENEACETAMIDE, N-(4-(4-FLUORO-2-METHYLPHENYL)-6-((7S,9AS)-HEXAHYDRO-7-(HYDROXYMETHYL)PYRAZINO(2,1-C)(1,4)OXAZIN-8(1H)-YL)-3-PYRIDINYL)-N,.ALPHA.,.ALPHA.-TRIMETHYL-3,5-BIS(TRIFLUOROMETHYL)-; Benzamide, 3-(5-methyl-2-tbenzeneacetamide, N-(4-(4-fluoro-2-methylphenyl)-6-((7S,9aS)-hexahydro-7-(hydroxymethyl)pyrazino(2,1-C)(1,4)oxazin-8(1H)-yl)-3-pyridinyl)-N,alpha,alpha-trimethyl-3,5-bis(trifluoromethyl)-

Indication

Disease Entry	ICD 11	Status	REF
Hot flushes	GA30	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 16063568
  TTD Drug ID: DMC6EFI

Molecule-Related Drug Atlas

Drug(s) Targeting Neuromedin-K receptor (TACR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fezolinetant	DMHDQZD	Hot flushes	GA30	Approved	[3]
Senktide	DMOH8LD	Epilepsy	8A60-8A68	Phase 2	[4]
AZD2624	DMZLGQV	Multiple sclerosis	8A40	Phase 2	[5]
Talnetant	DMQKZDT	Schizophrenia	6A20	Phase 2	[6]
GSK1144814	DMK3S9J	Alcohol dependence	6C40.2	Phase 1	[7]
Osanetant	DMMT4PB	Schizoaffective disorder	6A21	Discontinued in Phase 2b	[6]
CS-003	DM1AEVT	Chronic obstructive pulmonary disease	CA22	Discontinued in Phase 2	[8]
SSR-146977	DMR9JA8	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[9]
SB222200	DM6X0PZ	Schizoaffective disorder	6A21	Preclinical	[10]
neurokinin A	DM9UXRP	Discovery agent	N.A.	Investigative	[11]

Drug(s) Targeting Substance-P receptor (TACR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aprepitant	DM053KT	Depression	6A70-6A7Z	Approved	[12]
Selegiline	DM6034S	Major depressive disorder	6A70.3	Approved	[13]
Rolapitant	DM8XP26	Chemotherapy-induced nausea	MD90	Approved	[14]
Netupitant	DMEKAYI	Chemotherapy-induced nausea	MD90	Phase 3	[14]
Serlopitant	DM5VH6U	Prurigo nodularis	EC91.0	Phase 3	[15]
LY-686017	DM7WORZ	Atopic dermatitis	EA80	Phase 3	[16]
CP-122721	DMSWLM5	Major depressive disorder	6A70.3	Phase 2	[17]
FR139317	DMEL5SV	Hypertension	BA00-BA04	Phase 2	[13]
VOFOPITANT HYDROCHLORIDE	DMQMYP5	Vomiting	MD90	Phase 2	[18]
LY-2590443	DM81UJW	Migraine	8A80	Phase 2	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Neuromedin-K receptor (TACR3)	TTBPGLU	NK3R_HUMAN	Antagonist	[2]
Substance-P receptor (TACR1)	TTZPO1L	NK1R_HUMAN	Antagonist	[2]

References

• [1] ClinicalTrials.gov (NCT05099159) A Double-blind, Randomized, Placebo-controlled Multicenter Study to Investigate Efficacy and Safety of Elinzanetant for the Treatment of Vasomotor Symptoms Over 26 Weeks in Postmenopausal Women. U.S.National Institutes of Health.
• [2] Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3221-e3234.
• [3] Fezolinetant for treatment of moderate-to-severe vasomotor symptoms associated with menopause (SKYLIGHT 1): a phase 3 randomised controlled study. Lancet. 2023 Apr 1;401(10382):1091-1102.
• [4] Implication of nigral tachykinin NK3 receptors in the maintenance of hypertension in spontaneously hypertensive rats: a pharmacologic and autoradiographic study. Br J Pharmacol. 2003 Feb;138(4):554-63.
• [5] The selective neurokinin 3 antagonist AZD2624 does not improve symptoms or cognition in schizophrenia: a proof-of-principle study.J Clin Psychopharmacol.2014 Apr;34(2):199-204.
• [6] Pharmacological characterization of senktide-induced tail whips. Neuropharmacology. 2010 Jan;58(1):259-67.
• [7] Pharmacokinetics and central nervous system effects of the novel dual NK1 /NK3 receptor antagonist GSK1144814 in alcohol-intoxicated volunteers.Br J Clin Pharmacol.2013 May;75(5):1328-39.
• [8] Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
• [9] Biochemical and pharmacological activities of SSR 146977, a new potent nonpeptide tachykinin NK3 receptor antagonist. Can J Physiol Pharmacol. 2002 May;80(5):482-8.
• [10] Evidence for mediation of nociception by injection of the NK-3 receptor agonist, senktide, into the dorsal periaqueductal gray of rats. Psychopharmacology (Berl). 2009 May;204(1):13-24.
• [11] Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor. Eur J Pharmacol. 2001 Feb 16;413(2-3):143-50.
• [12] Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46.
• [13] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [14] Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.
• [15] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [16] Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498.
• [17] A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
• [18] Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58.
• [19] 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. (Target id: 360).