Fezolinetant

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Fezolinetant is the first NK3 antagonist which has been optimized for use in women’s health, and is being developed for sex-hormone related disorders such as endometriosis, polycystic ovarian syndrome and uterine fibroids. ESN-364 is an oral available small molecule which, due to its unique mechanism of action, allows modulation of the hypothalamic-pituitary gonadal axis with a selective action on hormones relevant to disease. As such, the agent is expected to have greater tolerability than competing products which target GnRH.

Inn NameFezolinetant
Lab CodesESN-364
Chemical Name(4-fluorophenyl)[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-5,6-dihydro-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]methanone
Chemical StructureFezolinetant.png
Molecular FormulaC16H15FN6OS
Cas Registry Number1629229-37-3
New Molecular EntityYes
OriginatorEuroscreen
Mechanism Of ActionNeurokinin-3 (NK-3) receptor antagonist
Who Atc CodesG02 (Other Gynecologicals), G04C (Drugs Used In Benign Prostatic Hypertrophy)
Ephmra CodesG2 (Other Gynaecologicals), G4C (BPH (Benign Prostatic Hypertrophy) Products)
Indication

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