Fezolinetant

Fezolinetant, sold under the brand name Veozah among others, is a medication used for the treatment of hot flashes (vasomotor symptoms) due to menopause. It is a small-molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist which is under development by for the treatment of sex hormone-related disorders. It is taken by mouth. It is developed by Astellas Pharma which acquired it from Ogeda (formerly Euroscreen) in April 2017.

Fezolinetant
Clinical data
Trade namesVeozah, Veoza
Other namesESN-364
AHFS/Drugs.comMonograph
MedlinePlusa623051
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding51%
MetabolismCYP1A2, (CYP2C9, CYP2C19 to lesser extent)
MetabolitesES259564
Elimination half-life9.6h
ExcretionUrine 76.9%, feces 14.7%
Identifiers
  • (4-fluorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC16H15FN6OS
Molar mass358.40 g·mol−1
3D model (JSmol)
  • C[C@@H]1C2=NN=C(N2CCN1C(=O)C3=CC=C(C=C3)F)C4=NC(=NS4)C
  • InChI=1S/C16H15FN6OS/c1-9-13-19-20-14(15-18-10(2)21-25-15)23(13)8-7-22(9)16(24)11-3-5-12(17)6-4-11/h3-6,9H,7-8H2,1-2H3/t9-/m1/s1
  • Key:PPSNFPASKFYPMN-SECBINFHSA-N

The most common side effects include abdominal pain, diarrhea, insomnia, back pain, hot flush and elevated hepatic transaminases.

Fezolinetant was approved for medical use in the United States in May 2023, and in the European Union in December 2023. Fezolinetant is the first neurokinin 3 (NK3) receptor antagonist approved by the US Food and Drug Administration (FDA) to treat moderate to severe hot flashes from menopause. The FDA considers it to be a first-in-class medication.

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