Elinzanetant

Elinzanetant
Clinical data
Other names	BAY-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	929046-33-3;
PubChem CID	16063568;
ChemSpider	17223178;
UNII	NZW2BOW35N;
KEGG	D12123;
Chemical and physical data
Formula	C33H35F7N4O3
Molar mass	668.657 g·mol−1
3D model (JSmol)	Interactive image;
	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;

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]

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.

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

v t e Neurokinin receptor modulators
NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Elinzanetant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant
NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant
NK₃	Agonists: Neurokinin B Senktide Antagonists: Elinzanetant Fezolinetant Osanetant Pavinetant SB-218,795 SB-222,200 Talnetant

Clinical data

Other names	BAY-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	929046-33-3
PubChem CID	16063568
ChemSpider	17223178
UNII	NZW2BOW35N
KEGG	D12123
Chemical and physical data
Formula	C₃₃H₃₅F₇N₄O₃
Molar mass	668.657 g·mol⁻¹
3D model (JSmol)	Interactive image
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