Lynkuet

Lynkuet is a non-hormonal prescription treatment used to treat moderate to severe hot flashes (vasomotor symptoms) associated with menopause. Lynkuet (elinzanetant) is an oral capsule taken once a day.

Hot flashes are characterized by sudden feelings of intense heat, warmth in the face, neck, and chest, along with sweating. These vasomotor symptoms occur due to decreased estrogen levels during menopause.

Key Facts

• Lynkuet is the first dual NK1/NK3 receptor antagonist approved for menopausal hot flashes
• It offers a non-hormonal treatment alternative
• Take once daily at bedtime
• Requires liver monitoring and pregnancy prevention
• Most common side effects involve drowsiness and dizziness
• Avoid grapefruit or drinking grapefruit juice during treatment, and driving if experiencing side effects.

Unlike hormone replacement therapy, Lynkuet works through a unique mechanism. The active ingredient elinzanetant is a dual neurokinin 1 (NK1) and neurokinin 3 (NK3) receptor antagonist.

The drug targets specific KNDy neurons in the hypothalamus region of the brain. When estrogen levels drop during menopause, these neurons become overactive, disrupting the body's temperature control mechanisms. Lynkuet helps restore normal thermoregulation by blocking NK1 and NK3 receptors, reducing both the frequency and severity of hot flashes.

FDA approval was based on the OASIS Phase III clinical trial program. In both OASIS 1 (NCT05042362) and OASIS 2 (NCT05099159) studies, Lynkuet successfully met its primary endpoints:

• Relief from symptoms started within just seven days of beginning therapy.
• By the three-month mark, over 70% of participants had experienced a minimum 50% decrease in the frequency of hot flashes.
• These results improved further, with more than 80% seeing the same reduction by the six-month point.
• Improvements were observed both day and night.

Absolute Contraindications:

• Women who are pregnant

Use with Caution if You Have:

• Liver problems or elevated liver enzymes
• History of seizures or epilepsy
• Are of childbearing age (pregnancy testing and contraception required).

Pregnancy and Birth Control Requirements

Lynkuet can cause serious harm to an unborn baby, including pregnancy loss or stillbirth.

Women who can become pregnant must:

• Have a negative pregnancy test before starting treatment
• Use effective birth control during treatment
• Continue contraception for 2 weeks after stopping Lynkuet
• Stop taking Lynkuet immediately and contact their healthcare provider if pregnancy is suspected.

Most Common Side Effects

Side effects reported by 5% or more of patients include:

• Headache
• Fatigue
• Dizziness
• Drowsiness or sleepiness (somnolence)
• Abdominal pain
• Rash
• Diarrhea
• Muscle spasms.

Serious Side Effects and Warnings

Central Nervous System Effects

Lynkuet can cause difficulty staying awake (somnolence) and other neurological symptoms, including:

• Excessive daytime sleepiness or fatigue
• Vertigo (spinning sensation)
• Dizziness
• Presyncope (feeling faint).

If you experience these effects, avoid driving and hazardous activities until your symptoms resolve.

Liver Problems

Lynkuet may increase liver enzymes. Your healthcare provider will:

• Test your liver function before starting treatment
• Recheck liver tests 3 months after beginning therapy.

Stop taking Lynkuet and contact your doctor immediately if you experience:

• Unusual tiredness or fatigue
• Loss of appetite
• Nausea or vomiting
• Yellowing of skin or eyes (jaundice)
• Dark-colored urine
• Pale or clay-colored stools
• Abdominal pain
• Itching.

Seizure Risk

People with a history of seizures may be at increased risk. Seek immediate medical attention if you experience loss of consciousness or seizure activity.

Contact your healthcare provider if side effects are bothersome or persistent. To report side effects to the FDA, call 1-800-FDA-1088.

Standard Dose:

• Take 2 capsules by mouth once daily at bedtime.

Important Administration Instructions:

• Take at approximately the same time each evening
• Can be taken with or without food
• Swallow capsules whole with water
• Do not cut, crush, or chew the capsules
• If taking certain medications, your doctor may reduce your dose to 1 capsule daily.

Missed Dose:

• If you forget your bedtime dose, simply take your next scheduled dose the following evening. Do not double up or take more than 2 capsules in one day.

Grapefruit: Avoid eating grapefruit or drinking grapefruit juice during treatment, as this can affect how your body processes the medication.

Driving and Hazardous Activities: Lynkuet may cause drowsiness, dizziness, or fatigue. Avoid driving or operating machinery until you know how the medication affects you.

Certain medications can affect how Lynkuet works in your body or increase the risk of side effects. Always inform your healthcare provider about all medicines you take, including prescription medications, over-the-counter drugs, vitamins and supplements, and herbal products

Medications to AVOID While Taking Lynkuet

Strong CYP3A4 Inhibitors:

These medications significantly increase Lynkuet levels in your blood. Do not take Lynkuet with:

• Antifungals: ketoconazole (Nizoral), itraconazole (Sporanox), posaconazole (Noxafil), voriconazole (Vfend)
• Antibiotics: clarithromycin (Biaxin), telithromycin (Ketek)
• HIV medications: ritonavir (Norvir), cobicistat (Tybost), indinavir, nelfinavir, saquinavir
• Other medications: nefazodone (antidepressant), conivaptan (Vaprisol)

Strong and Moderate CYP3A4 Inducers:

These medications decrease Lynkuet levels, making it less effective. Avoid:

• Seizure medications: phenytoin (Dilantin), carbamazepine (Tegretol), phenobarbital
• Tuberculosis drugs: rifampin (Rifadin), rifabutin (Mycobutin)
• Herbal supplements: St. John's Wort
• Other medications: efavirenz (Sustiva), modafinil (Provigil), bosentan (Tracleer)

Medications Requiring Dose Adjustment

Moderate CYP3A4 Inhibitors:

If you take these medications, your doctor will reduce your Lynkuet dose to 1 capsule (60 mg) once daily:

• Antibiotics: erythromycin, ciprofloxacin (Cipro)
• Antifungals: fluconazole (Diflucan)
• Heart medications: diltiazem (Cardizem), verapamil (Calan)
• Antidepressants: fluvoxamine (Luvox)
• Other medications: aprepitant (Emend), cimetidine (Tagamet), cyclosporine, dronedarone (Multaq)

Food Interaction

Grapefruit and grapefruit juice act like strong CYP3A4 inhibitors and must be completely avoided during Lynkuet treatment.

• Store at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep in original packaging until ready to use.
• If the dose is reduced to 1 capsule, partially peel back the blister foil and leave the remaining capsule inside.
• Keep out of reach of children.

Active Ingredient: elinzanetant

Inactive Ingredients: all-rac-α-Tocopherol, caprylocaproyl macrogolglycerides, glycerol monocaprylocaprate, glycerol mono-oleate, polysorbate 80

Capsule Shell: edible ink, ferric oxide red, ferric oxide yellow, gelatin, sorbitol, special-glycerin, titanium dioxide.

Distributed by: Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ 07981 USA

For more information:

• Visit: www.lynkuet.com
• Call: 1-888-842-2937