Elinzanetant

Elinzanetant is a prescription medication indicated for the treatment of moderate-to-severe vasomotor symptoms (VMS) due to menopause.

• Elinzanetant is available under the following different brand names: Lynkuet.

Common side effects of Elinzanetant include:

• headache 
• abdominal pain
• fatigue 
• rash
• dizziness
• diarrhea
• somnolence
• muscle spasms 

Serious side effects of Elinzanetant include:

• central nervous system (CNS) depressant effect and daytime impairment
• hepatic transaminase elevations
• risk of pregnancy loss
• risk of seizures in people with a history of seizures

Rare side effects of Elinzanetant include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Capsule

• 60 mg

Menopausal Vasomotor Symptoms

Adult dosage

• 120 mg orally daily at bedtime (at approximately the same time each day)

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

Drug interaction overview

• Elinzanetant is a sensitive CYP3A4 substrate and a weak CYP3A4 inhibitor
• Strong CYP3A4 inhibitors
  • Avoid coadministration
  • Strong inhibitors increase elinzanetant exposure, which may increase the risk of adverse effects
• Moderate CYP3A4 inhibitors
  • Modify dose
  • Decrease elinzanetant dose if coadministered with moderate CYP3A4 inhibitors
• Strong or moderate CYP3A4 inducers
  • Avoid coadministration
  • Strong and moderate CYP3A4 inducers decrease elinzanetant exposure, which may reduce its efficacy
• Sensitive CYP3A4 substrates
  • Avoid coadministration unless otherwise recommended in the prescribing information for CYP3A4 substrates, where minimal concentration changes may lead to serious adverse reactions

Contraindications

• Pregnancy; exposure to elinzanetant may cause pregnancy loss or stillbirth when administered during pregnancy

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Elinzanetant?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Elinzanetant?”

Cautions

• CNS depressant effect and daytime impairment
• Nervous system effects (eg, somnolence, fatigue, vertigo, dizziness, presyncope) reported
• Advise patients of the potential for somnolence and other nervous system effects
• Advise patients who experience these effects to refrain from driving or engaging in hazardous occupations or activities until the effects have resolved
• Hepatic transaminase elevations
  • Elevations in serum transaminase (ALT and/or AST) concentrations of 3x ULN or more reported
  • Perform baseline bloodwork (including ALT, AST, alkaline phosphatase, and total bilirubin [TB] and direct bilirubin) before initiating to evaluate for hepatic function and injury
  • Do not start therapy if serum transaminase concentration is 2x ULN and more, or if TB is 2x ULN and more
  • Perform follow-up evaluations of hepatic transaminase concentration 3 months after initiating
  • Advise patients to discontinue elinzanetant immediately and seek medical attention, including hepatic laboratory tests, if they experience signs or symptoms that may suggest liver injury (eg, new onset fatigue, decreased appetite, nausea, vomiting, pruritus, jaundice, pale feces, dark urine, or abdominal pain)
  • Discontinue if transaminase elevations are more than 5x ULN or if transaminase elevations are more than 3x ULN and TB is more than 2x ULN
  • Exclude alternative causes of hepatic laboratory test elevation
• Risk of pregnancy loss
  • Contraindicated for use in pregnancy
  • Findings from animal studies suggest that Elinzanetant can cause pregnancy loss or stillbirth
  • Exclude pregnancy in females of reproductive potential before initiating
  • Advise females of reproductive potential to use effective contraception during treatment and for 2 weeks after the last dose
• Seizure risk
  • Seizure was reported in 1 patient with a history of seizures in clinical trials
  • Additionally, convulsions were observed in studies conducted in male and female rats
  • Caution in patients with a history of seizures or with conditions that potentially lower seizure threshold

Pregnancy and Lactation

• Contraindicated during pregnancy
  • If pregnancy occurs during use, discontinue treatment
  • Based on findings from animal reproduction studies, it may cause pregnancy loss or stillbirth, but not fetal malformations when administered during pregnancy
  • There are no data on use during pregnancy in women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
• Contraception
  • Use effective contraception during treatment and for 2 weeks after stopping treatment
• Lactation
  • There are no data on the presence of elinzanetant or its metabolites in human milk, its effects on breastfed children, or milk production
  • Elinzanetant is present in animal milk; when a drug is present in animal milk, it is likely to be present in human milk