Fezolinetant Chemical Properties

Boiling point:

623.0±65.0 °C(Predicted)

Density 

1.56±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:20.0(Max Conc. mg/mL);55.8(Max Conc. mM)

pka

-0.28±0.40(Predicted)

form 

Solid

color 

White to yellow

InChI

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

InChIKey

PPSNFPASKFYPMN-SECBINFHSA-N

SMILES

C(N1CCN2C(C3SN=C(C)N=3)=NN=C2[C@H]1C)(C1=CC=C(F)C=C1)=O

Fezolinetant Usage And Synthesis

Uses

Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

Definition

ChEBI: Fezolinetant is a triazolopyrazine that is 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine substituted by 3-methyl-1,2,4-thiadiazol-5-yl, 4-fluorobenzoyl and methyl groups at positions 3, 7, and 8R, respectively. It is a prescription medicine used to reduce moderate to severe vasomotor symptoms due to menopause. It has a role as a neurokinin-3 receptor antagonist. It is a member of monofluorobenzenes, a triazolopyrazine, a member of thiadiazoles, a member of benzamides and a tertiary carboxamide.

Mechanism of action

Fezolinetant is an oral non-hormonal therapy that is an NK3R antagonist. It works by binding to and blocking the activity of NK3 receptors, which play a role in the regulation of body temperature in the brain.

Side effects

The common side effects of Fezolinetant include abdominal pain, diarrhoea, insomnia, back pain, hot flushes and elevated liver transaminases.

in vivo

IC 50

NK3