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elinzanetant   Click here for help

GtoPdb Ligand ID: 12691

Synonyms: BAY-3427080 | BAY3427080 | Compound A [WO2021094247A1] | Example 34 [WO2007028654A1] | Lynkuet® | NT-814 | NT814
Approved drug
elinzanetant is an approved drug
Compound class: Synthetic organic
Comment: Elinzanetant (BAY3427080) is a dual NK1R/NK3R antagonist [6]. It was initially developed for use in the treatment of psychotic disorders [1], but has subsequently been repositioned to manage vasomotor symptoms of the menopause [5].
2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 7
Hydrogen bond donors 1
Rotatable bonds 9
Topological polar surface area 68.61
Molecular weight 668.65
XLogP 2.98
No. Lipinski's rules broken 1

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)

SMILES / InChI / InChIKey
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Canonical 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
Isomeric 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
InChI Key DWRIJNIPBUFCQS-DQEYMECFSA-N

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)

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Summary of Clinical Use Click here for help
Elinzanetant (BAY3427080) was progressed to clinical studies to evaluate its potential to treat vasomotor symptoms of the menopause (hot flushes/flashes, night sweats), and for women undergoing endocrine-based breast cancer therapy [2]. First approval was issued by the UK's MHRA in July 2025, to treat moderate to severe menopausal hot flushes and night sweats [3]. FDA approval for these symptoms followed in October 2025. Elinzanetant is also authorised for prescription in Australia, Canada and Switzerland.

Contraindicated in patients taking strong cytochrome P450 3A4 (CYP3A4) inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, diltiazem, erythromycin, and verapamil) as these may reduce clearance of elinzanetant (daily dosage can be halved if required). CYP3A4 inducers (e.g., rifampicin, carbamazepine, phenobarbital, St. John's Wort) are likely to reduce elinzanetant exposure and efficacy.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03596762 A Study of BAY3427080 (NT-814) in the Treatment of Moderate to Severe Post-menopausal Vasomotor Symptoms Phase 2 Interventional Bayer The SWITCH-1 study. Positive results (decrease in VMS in postmenopausal women) were published in March 2023. 7
NCT02865538 Evaluation of the Pharmacokinetics and Safety of BAY3427080 (NT-814) in Post-Menopausal Women With Vasomotor Symptoms Phase 1/Phase 2 Interventional Bayer The RELENT-1 study. 8
NCT05042362 A Study to Learn More About How Well Elinzanetant Works and How Safe it is for the Treatment of Vasomotor Symptoms (Hot Flashes) That Are Caused by Hormonal Changes Over 26 Weeks in Women Who Have Been Through the Menopause Phase 3 Interventional Bayer OASIS-1 study 4
NCT05099159 A Study to Learn More About How Well Elinzanetant Works and How Safe it is for the Treatment of Vasomotor Symptoms (Hot Flashes) That Are Caused by Hormonal Changes Over 26 Weeks in Women Who Have Been Through the Menopause (OASIS-2) Phase 3 Interventional Bayer OASIS-2 study 4
NCT05030584 A Study to Learn More About How Well Elinzanetant Works and How Safe it is for the Treatment of Vasomotor Symptoms (Hot Flashes) That Are Caused by Hormonal Changes Over 52 Weeks in Women Who Have Been Through the Menopause Phase 3 Interventional Bayer OASIS-3 study
NCT05587296 A Study to Learn More About How Well Elinzanetant Works and How Safe it is Compared to Placebo for the Treatment of Hot Flashes Caused by Anti-cancer Therapy in Women With, or at High Risk for Developing Hormone-receptor Positive Breast Cancer Phase 3 Interventional Bayer OASIS-4 study 2