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Chemical compound
Elinzanetant
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Other names | BAY-3427080; GSK-1144814; NT-814 |
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Routes of administration |
Oral administration |
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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
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CAS Number | |
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PubChem
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KEGG | |
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CompTox Dashboard (
EPA) | |
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Formula | C33H35F7N4O3 |
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Molar mass | 668.657 g·mol−1 |
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3D model (
JSmol) | |
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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
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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
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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
- ^
a
b
c
"Elinzanetant - Bayer". Adis Insight. Springer Nature Switzerland AG.
- ^
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.
-
^ 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