Elinzanetant
Clinical data
Other namesBAY-3427080; GSK-1144814; NT-814
Routes of
administration		Oral administration
Identifiers
  • 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)
  • 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=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

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]

See also

References

  1. ^ a b c "Elinzanetant - Bayer". Adis Insight. Springer Nature Switzerland AG.
  2. ^ a b 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. hdl:1854/LU-8758954. 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.

External links

Neurokinin receptor modulators
Categories