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MEDICAL INFORMATION
Elinzanetant Key Facts
What dosages is Elinzanetant available in?
Elinzanetant is available as 60 mg soft gelatin capsules. The recommended dose is 120 mg (two 60 mg capsules) taken orally once daily at bedtime.
What is Elinzanetant used for?
Elinzanetant is indicated for the treatment of moderate to severe vasomotor symptoms (VMS) due to menopause, commonly known as hot flashes. It is a non-hormonal option suitable for women who cannot or choose not to use hormone therapy.
How does Elinzanetant work?
Elinzanetant is a dual neurokinin 1 (NK1) and neurokinin 3 (NK3) receptor antagonist. It works by inhibiting Substance P and Neurokinin B through antagonism of NK1 and NK3 receptor signalling on kisspeptin/neurokinin B/dynorphin (KNDy) neurons in the hypothalamus.
During menopause, falling estrogen levels cause these neurons to become overactive, disrupting the body’s temperature regulation and leading to hot flashes. By blocking both NK1 and NK3 receptors, Elinzanetant helps restore normal thermoregulation, reducing the frequency and severity of hot flashes and associated sleep disturbances.
How do I take Elinzanetant?
Take Elinzanetant 120 mg (two 60 mg capsules) orally once daily at bedtime, at approximately the same time each day.
Take with or without food. Swallow the capsules whole with water — do not cut, crush, or chew them.
If you miss a dose at bedtime, skip it and take the next dose as scheduled the following night. Do not take two doses on the same day to make up for a missed dose.
Avoid grapefruit and grapefruit juice during treatment as it can increase the amount of Elinzanetant in your blood.
Is it safe for me to take Elinzanetant?
Elinzanetant is a safe and effective treatment when used for its FDA-approved indication. However, like all medicines, it can cause side effects. You should discuss potential risks with your healthcare provider before starting treatment.
Before starting Elinzanetant, your healthcare provider should:
• Confirm you are not pregnant
• Check your liver function with a blood test
• Repeat the liver blood test 3 months after starting treatment
Tell your healthcare provider if you have:
• Liver problems — Elinzanetant is not recommended if you have moderate or severe liver impairment
• End-stage kidney disease — Elinzanetant is not recommended in this setting
• A history of seizures — use with caution
• Any plans to become pregnant — Elinzanetant is contraindicated in pregnancy
Elinzanetant Common Side Effects
Common side effects of Elinzanetant (≥2% and more frequent than placebo):
• Headache
• Fatigue
• Dizziness
• Somnolence (sleepiness)
• Abdominal pain
• Rash
• Diarrhoea
• Muscle spasms
• Nausea
• Gastroesophageal reflux disease (heartburn)
Some patients have reported mild to moderate photosensitivity (increased sensitivity to sunlight). Nervous system effects such as drowsiness, fatigue, and dizziness occurred in approximately 12% of patients in clinical trials. Patients should be cautious about driving or operating machinery until they know how Elinzanetant affects them.
Elinzanetant Serious Side Effects
Serious side effects are uncommon with Elinzanetant but contact your healthcare provider immediately if you experience any of the following:
Liver problems (hepatic transaminase elevations): Seek medical attention if you notice new onset fatigue, decreased appetite, nausea, vomiting, itching, yellowing of skin or eyes (jaundice), pale stools, dark urine, or abdominal pain. Liver blood tests should be performed before starting treatment and at 3 months.
CNS depressant effects and daytime impairment: Somnolence, dizziness, and other nervous system effects occurred in approximately 12% of patients. Do not drive or engage in hazardous activities until these effects have resolved.
Risk of pregnancy loss: Animal studies indicate Elinzanetant may cause pregnancy loss or stillbirth. It is contraindicated in pregnancy.
Seizures: Use with caution if you have a history of seizures, as one case of seizure was reported in a patient with a prior seizure history during clinical trials.
Effects of other drugs, drug classes and over-the-counter products on Elinzanetant
Elinzanetant is primarily metabolised by the CYP3A4 enzyme. The following drug interactions are important:
Drugs that increase Elinzanetant exposure (avoid or reduce dose):
• Strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, clarithromycin, ritonavir): avoid concomitant use
• Grapefruit and grapefruit juice: avoid during treatment
• Moderate CYP3A4 inhibitors (e.g. fluconazole, diltiazem, verapamil, erythromycin): reduce Elinzanetant dose to 60 mg once daily
Drugs that reduce Elinzanetant effectiveness (avoid):
• Strong CYP3A4 inducers (e.g. rifampicin, carbamazepine, phenytoin, St John’s Wort): avoid concomitant use
• Moderate CYP3A4 inducers: avoid concomitant use
Drugs affected by Elinzanetant:
• Elinzanetant is a weak CYP3A4 inhibitor and may increase exposure of CYP3A4 substrates. Avoid concomitant use with CYP3A4 substrates where small increases in concentration may lead to serious adverse effects.
Always tell your physician and pharmacist about all medicines, supplements (including herbal products), and vitamins you are taking.
Who makes Elinzanetant?
Various FDA-approved generic manufacturers
Is Elinzanetant safe in pregnancy?
Elinzanetant is contraindicated in pregnancy. Based on animal reproduction studies, Elinzanetant may cause pregnancy loss or stillbirth when administered during pregnancy. Fetal malformations were not observed in these studies.
Women of reproductive potential should:
• Have a negative pregnancy test before starting Elinzanetant
• Use effective contraception during treatment and for 2 weeks after stopping
• Discontinue Elinzanetant immediately if pregnancy is confirmed
Breastfeeding: There are no human data on the presence of Elinzanetant in breast milk. Animal studies show Elinzanetant is present in animal milk and metabolites were detected in the plasma of nursing pups. The potential risk to a breastfed infant is unknown. Discuss with your healthcare provider before breastfeeding while on Elinzanetant.
What is the brand name for Elinzanetant?
NowPatient has taken all reasonable steps to ensure that all material is factually accurate, complete, and current. However, the knowledge and experience of a qualified healthcare professional should always be sought after instead of using the information on this page. Before taking any drug, you should always speak to your doctor or another qualified healthcare provider.
The information provided here about medications is subject to change and is not meant to include all uses, precautions, warnings, directions, drug interactions, allergic reactions, or negative effects. The absence of warnings or other information for a particular medication does not imply that the medication or medication combination is appropriate for all patients or for all possible purposes.
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