Elinzanetant
{{Short description|Chemical compound}}
{{Drugbox
| image = Elinzanetant skeletal.svg
| width = 250
| alt =
| tradename =
| pregnancy_AU =
| pregnancy_category =
| routes_of_administration = Oral administration
| class =
| ATC_prefix = None
| ATC_suffix =
| ATC_supplemental =
| legal_AU =
| legal_CA =
| legal_UK =
| legal_US =
| legal_status =
| bioavailability =
| protein_bound =
| metabolism =
| elimination_half-life =
| excretion =
| CAS_number = 929046-33-3
| CAS_supplemental =
| PubChem = 16063568
| IUPHAR_ligand =
| DrugBank =
| ChemSpiderID = 17223178
| UNII = NZW2BOW35N
| KEGG = D12123
| ChEBI =
| ChEMBL =
| synonyms = BAY-3427080; GSK-1144814; NT-814
| IUPAC_name = 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
| C=33 | H=35 | F=7 | N=4 | O=3
| SMILES = CC1=C(C=CC(=C1)F)C2=CC(=NC=C2N(C)C(=O)C(C)(C)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)N4C[C@H]5COCCN5C[C@H]4CO
| StdInChI_Ref =
| StdInChI = 1S/C33H35F7N4O3/c1-19-9-23(34)5-6-26(19)27-13-29(44-16-25-18-47-8-7-43(25)15-24(44)17-45)41-14-28(27)42(4)30(46)31(2,3)20-10-21(32(35,36)37)12-22(11-20)33(38,39)40/h5-6,9-14,24-25,45H,7-8,15-18H2,1-4H3/t24-,25-/m0/s1
| StdInChIKey_Ref =
| StdInChIKey = DWRIJNIPBUFCQS-DQEYMECFSA-N
}}
Elinzanetant (developmental code names BAY-3427080 GSK-1144814, NT-814) is an orally active small-molecule neurokinin/tachykinin NK1 receptor and NK3 receptor antagonist which is under development by Bayer, GlaxoSmithKline, and NeRRe Therapeutics for the treatment of hot flashes and "sex hormone disorders".{{cite web | title = Elinzanetant - Bayer | url = https://adisinsight.springer.com/drugs/800044912 | work = Adis Insight | publisher = Springer Nature Switzerland AG }}{{cite journal | vauthors = Depypere H, Lademacher C, Siddiqui E, Fraser GL | title = Fezolinetant in the treatment of vasomotor symptoms associated with menopause | journal = Expert Opinion on Investigational Drugs | volume = 30 | issue = 7 | pages = 681–694 | date = July 2021 | pmid = 33724119 | doi = 10.1080/13543784.2021.1893305 | doi-access = free | hdl = 1854/LU-8758954 | hdl-access = free }} It has been found to relieve hot flashes in postmenopausal women and to dose-dependently suppress luteinizing hormone, estradiol, and progesterone levels in premenopausal women.{{cite journal | vauthors = Pawsey S, Mills EG, Ballantyne E, Donaldson K, Kerr M, Trower M, Dhillo WS | title = Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women | journal = The Journal of Clinical Endocrinology and Metabolism | volume = 106 | issue = 8 | pages = e3221–e3234 | date = July 2021 | pmid = 33624806 | pmc = 8277204 | doi = 10.1210/clinem/dgab108 }} As of August 2021, elinzanetant is in phase 2 clinical trials for hot flashes and "sex hormone disorders". It was also under development for the treatment of schizophrenia and opioid-related disorders, but development was discontinued for these uses.
See also
References
{{Reflist}}
{{Neurokinin receptor modulators}}
Category:NK3 receptor antagonists
Category:Trifluoromethyl compounds
{{Nervous-system-drug-stub}}