Fezolinetant

Fezolinetant

• developed for the treatment of moderate-to-severe vasomotor symptoms associated with menopause
  
• is a nonhormonal, selective neurokinin 3 receptor antagonist that blocks neurokinin B binding on the kisspeptin/neurokinin B/dynorphin neurons in the hypothalamus to moderate neuronal activity in the thermoregulatory center
  
• is a once-daily oral nonhormonal therapy
  
• a review (n=2168;5 RCTs) found fezolinetant is effective in lowering moderate-to-severe vasomotor symptom frequency (pooled mean difference of 2.62 [95% CI 1.84-3.41] episodes per day versus placebo) and was associated with improvement in sleep quality (3)
  
• possible adverse effects of fezolinetant include diarrhoea, insomnia, abdominal pain and an increase in alanine transaminase (4)

Reference:

1. Neal-Perry G, Cano A, Lederman S, Nappi RE, Santoro N, Wolfman W, English M, Franklin C, Valluri U, Ottery FD. Safety of Fezolinetant for Vasomotor Symptoms Associated With Menopause: A Randomized Controlled Trial. Obstet Gynecol. 2023 Apr 1;141(4):737-747
2. Wright AC, Beaudoin FL, McQueen RB, Yeung K, Moradi A, Herron-Smith S, Gutierrez E, Lin GA, Pearson SD. The effectiveness and value of fezolinetant for moderate-to-severe vasomotor symptoms associated with menopause: A summary from the Institute for Clinical and Economic Review's Midwest Public Advisory Council. J Manag Care Spec Pharm. 2023 Jun;29(6):692-698.
3. Bonga KN et al. Efficacy and Safety of Fezolinetant for the Treatment of Menopause-Associated Vasomotor Symptoms: A Meta-analysis. Obstetrics & Gynecology ():10.1097/AOG.0000000000005508, January 16, 2024.
4. Fezolinetant for menopausal vasomotor symptomsDrug and Therapeutics Bulletin 2024;62:118-124