Elinzanetant

Last updated

Elinzanetant
Elinzanetant skeletal.svg
Clinical data
Trade names Lynkuet
Other namesBAY-3427080; GSK-1144814; NT-814
Routes of
administration
Oral administration
ATC code
  • None
Legal status
Legal status
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
CompTox Dashboard (EPA)
Chemical and physical data
Formula C33H35F7N4O3
Molar mass 668.657 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, sold under the brand name Lynkuet, 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. [4] 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. [4] [5]

Contents

Elinzanetant is a non-hormonal, selective, neurokinin 1 (NK-1) and 3 (NK-3) receptor antagonist. [6] By blocking NK-1 and NK-3 receptors signalling, elinzanetant is postulated to normalize neuronal activity involved in thermo- and sleep regulation in the hypothalamus. [6]

Medical uses

Elinzanetant is indicated for the treatment of moderate to severe vasomotor symptoms associated with menopause. [7]

Society and culture

In September 2025, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Lynkuet, intended for the treatment of moderate to severe vasomotor symptoms (hot flushes). [6] The applicant for this medicinal product is Bayer AG. [6]

Names

Elinzanetant is the international nonproprietary name. [8]

Elinzanetant is sold under the brand name Lynkuet.

References

  1. "Details for: Lynkuet". Drug and Health Products Portal. 23 July 2025. Retrieved 28 September 2025.
  2. "Lynkuet product information". Lynkuet . 23 July 2025. Retrieved 28 September 2025.
  3. "MHRA approves elinzanetant to treat moderate to severe vasomotor symptoms (hot flushes) caused by menopause". Medicines and Healthcare products Regulatory Agency (Press release). 8 July 2025. Retrieved 28 September 2025.
  4. 1 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 . hdl: 1854/LU-8758954 . PMID   33724119.
  5. Pawsey S, Mills EG, Ballantyne E, Donaldson K, Kerr M, Trower M, et al. (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.
  6. 1 2 3 4 "Lynkuet EPAR". European Medicines Agency (EMA). 19 September 2025. Retrieved 27 September 2025. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  7. https://www.bayer.com/sites/default/files/lynkuet-pm-en.pdf
  8. World Health Organization (2020). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 84". WHO Drug Information. 34 (3). hdl: 10665/340680 .