Elinzanetant

Aka: Elinzanetant, Lynkuet

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II. Indications

  1. Refractory Vasomotor Symptoms of Menopause (Hot Flashes)
    1. Second-line option when hormonal therapy is contraindicated

III. Contraindications

  1. Seizure Disorder
  2. Cirrhosis or liver transaminases >2x upper limit normal

IV. Mechanism

  1. Elinzanetant blocks both Neurokinin 3 and neurokinin 1 receptors
    1. Contrast with Fezolinetant which primarily blocks Neurokinin 3 receptor
  2. Neurokinin 3 Receptor Antagonist
    1. Small molecule NK3 Receptor Antagonist
    2. Blocks neurokinin B (NKB) at the infundibular nucleus of the Hypothalamus
  3. Neurokinin-1 Receptor Antagonist
    1. Cross the blood brain barrier to inhibit CNS substance-P activity
    2. Typically used to prevent Chemotherapy Induced Nausea and Vomiting
    3. Blocks the neurokinin-1 receptor (a tachykinin)
      1. Antiemetic (synergistic with 5-HT3 Antagonists)
      2. Anxiolysis and Antidepressant properties
  4. Neurokinin B (NKB) regulates temperarture
    1. Blockade can decrease Vasomotor Symptoms of Menopause (Hot Flashes)

V. Medications

  1. Elinzanetant Capsules 60 mg
  2. 120 mg (two 60 mg capsules) orally once daily at bedtime with or without food.

VI. Dosing

  1. Elinzanetant 120 mg (two 60 mg capsules) orally once daily at bedtime with or without food
  2. Swallow capsules whole. Do not cut, crush, or chew capsules

VII. Adverse Effects

  1. Common
    1. Headache
    2. Dizziness
    3. Drowsiness
  2. Serious
    1. Hepatic Transaminase Elevations
      1. Unlike Fezolinetant, Elinzanetant does not carry the same liver injury warning
      2. Do not start Elinzanetant if transaminases are >2x upper limit normal
      3. However, obtain baseline hepatic panel prior to starting, then at 3 months
        1. Stop medication if transaminases increase >2x upper limit normal
    2. Seizures
      1. May trigger Seizures in those with Epilepsy

VIII. Safety

  1. Containdicated in Pregnancy
    1. May cause pregnancy loss or Stillbirth

IX. Efficacy

  1. Elinzanetant reduces Hot Flashes by 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

X. Drug Interactions

  1. Avoid with strong CYP3A4 inhibitors (e.g. Clarithromycin, Grapefruit)
    1. Decrease Elinzanetant dose to 60 mg when moderate CYP3A4 inhibitors are used

XI. Resources

  1. Elinzanetant (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f42884ff-7dff-419c-8a0c-affe2ed73818

XII. References

  1. (2025, Jan) Presc Insights, No. 420111

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