Elinzanetant

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".[1][2] 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.[2][3] As of August 2021, elinzanetant is in phase 2 clinical trials for hot flashes and "sex hormone disorders".[1] It was also under development for the treatment of schizophrenia and opioid-related disorders, but development was discontinued for these uses.[1]

Elinzanetant
Clinical data
Other namesBAY-3427080; GSK-1144814; NT-814
Routes of
administration		Oral administration
Identifiers
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
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC33H35F7N4O3
Molar mass668.657 g·mol−1
3D model (JSmol)
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
InChI
  • InChI=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
  • Key:DWRIJNIPBUFCQS-DQEYMECFSA-N

See also

References
  1. "Elinzanetant - Bayer". Adis Insight. Springer Nature Switzerland AG.
  2. Depypere H, Lademacher C, Siddiqui E, Fraser GL (July 2021). "Fezolinetant in the treatment of vasomotor symptoms associated with menopause". Expert Opinion on Investigational Drugs. 30 (7): 681–694. doi:10.1080/13543784.2021.1893305. PMID 33724119.
  3. Pawsey S, Mills EG, Ballantyne E, Donaldson K, Kerr M, Trower M, Dhillo WS (July 2021). "Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women". The Journal of Clinical Endocrinology and Metabolism. 106 (8): e3221–e3234. doi:10.1210/clinem/dgab108. PMC 8277204. PMID 33624806.
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