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Fezolinetant

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Fezolinetant, Veozah, Neurokinin 3 Receptor Antagonist

  • See Also
  1. Hot Flashes
  2. Neurokinin 1 Receptor Antagonist
  • Indications
  1. Refractory Vasomotor Symptoms of Menopause (Hot Flashes)
    1. Second-line option when hormonal therapy is contraindicated
  • Contraindications
  1. Cirrhosis
  2. Severe renal Impairment (including end-stage renal disease)
  • Mechanism
  1. Neurokinin 3 Receptor Antagonist
    1. Small molecule NK3 Receptor Antagonist
    2. Blocks neurokinin B (NKB) at the infundibular nucleus of the Hypothalamus
  2. Neurokinin B (NKB) regulates temperarture
    1. Blockade can decrease Vasomotor Symptoms of Menopause (Hot Flashes)
  • Medications
  1. Fezolinetant (Veozah)
    1. Cost: $550 per month when released in 2023
  • Dosing
  1. Fezolinetant (Veozah) 45 mg orally daily (with or without food)
    1. Obtain baseline hepatic panel prior to starting, then in 3, 6 and 9 months
    2. Stop periodically to assess continued need
  • Adverse Effects
  1. Common
    1. Diarrhea
    2. Abdominal discomfort
    3. Insomnia
  2. Serious
    1. Liver Injury
      1. Transient transaminase increase >3x upper limit of normal (2% of patients)
      2. Obtain baseline hepatic panel prior to starting, then in 3, 6 and 9 months
      3. Stop medication if transaminases increase >2x upper limit normal
  • Efficacy
  1. Fezolinetant 45 mg daily reduces Hot Flashes by 2 to 3 per day
  2. Less effective than hormonal therapy for Vasomotor Symptoms of Menopause
  3. Similar to SNRIs, SSRIs and Gabapentin in hot flash reduction
  4. Was not studied in women age >65 years prior to release
  • Drug Interactions
  1. CYP1A2 Inhibitors (e.g. Allopurinol, Omeprazole, Fluvoxamine, Cimetidine)
    1. Increase Fezolinetant levels
  • Resources
  1. Fezolinetant (Veozah)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cae9f798-24f9-4580-a4fc-e6c710cbda3c
  • References
  1. Crespo (2024) Am Fam Physician 109(3): 273-4 [PubMed]
  2. Modi (2019) Neuroendocrinology 109(3):242-8 +PMID: 30504731 [PubMed]