Pharm

Neurokinin 3 Receptor Antagonist

search

Neurokinin 3 Receptor Antagonist, Fezolinetant, Veozah

  • 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
  • Mechanism
  1. Neurokinin 3 Receptor Antagonist
  2. Blocks neurokinin B (NKB) at the infundibular nucleus of the Hypothalamus
  3. Neurokinin B (NKB) regulates temperarture and its blockade can decrease Vasomotor Symptoms of Menopause (Hot Flashes)
  • Efficacy
  1. Fezolinetant 45 mg daily reduces Hot Flashes by 2 to 3 per day
    1. Less effective than hormonal therapy
    2. Similar to SNRIs, SSRIs and Gabapentin in hot flash reduction
  • Background
  1. Cost: $550 per month when released in 2023
  • Dosing
  1. Fezolinetant (Veozah) 45 mg orally daily
    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. Obtain baseline hepatic panel prior to starting, then in 3, 6 and 9 months
  • Drug Interactions
  1. CYP1A2 Inhibitors (e.g. Allopurinol, Omeprazole)
    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. Modi (2019) Neuroendocrinology 109(3):242-8 +PMID: 30504731 [PubMed]