LYNKUET is indicated for the treatment of moderate to severe vasomotor symptoms (VMS) due to menopause.¹

LYNKUET is a neurokinin 1 (NK1) and neurokinin 3 (NK3) receptor antagonist.¹

Inhibition of Substance P and Neurokinin B through antagonism of NK1 and NK3 receptor signaling on kisspeptin/neurokinin B/dynorphin (KNDy) neurons can modulate neuronal activity in thermoregulation associated with hot flashes.¹

Elinzanetant has higher affinity for human NK1 receptors (pKi values of 8.7 to 10.2) and NK3 receptors (pKi values of 8.0 to 8.8) than for human NK2 receptors (pKi values of approximately 6.0).¹

Learn more about the MOA.

The co-primary endpoints in the OASIS 1 and OASIS 2 clinical trials were the mean change in the frequency and severity of moderate to severe VMS from baseline to Weeks 4 and 12, including day and night hot flashes, measured using the Hot Flash Daily Diary. Please see Study Designs for full study information including primary and secondary endpoints.¹

Recommended Evaluation and Testing Before Initiation of LYNKUET¹

• Exclude pregnancy in females of reproductive potential
• Perform baseline hepatic laboratory tests to evaluate for hepatic function and injury [including serum alanine aminotransferase (ALT), serum aspartate aminotransferase (AST), serum alkaline phosphatase (ALP), and serum bilirubin (total and direct)] before initiating treatment with LYNKUET. Do not start LYNKUET if ALT or AST is ≥2 times upper limit of normal (ULN) or if the total bilirubin is ≥2 times ULN

The recommended dosage of LYNKUET is 120 mg (two 60 mg capsules) orally once daily at bedtime at about the same time each day. If a dose is missed at bedtime, take the next dose as scheduled on the following day. Two doses should not be taken on the same day to make up for a missed dose.¹

LYNKUET can be taken with or without food. Capsules should be taken with water and swallowed whole. Do not cut, crush, or chew capsules.¹
 

Dosage Modifications for Drug Interactions
Strong CYP3A4 Inhibitors and grapefruit (juice): Avoid concomitant use with LYNKUET.¹

Moderate CYP3A4 Inhibitors: Reduce LYNKUET dosage to 60 mg once daily at bedtime. After discontinuation of the moderate CYP3A4 inhibitor (after 3 to 5 half-lives of the inhibitor), LYNKUET should be used at the usual dosage of 120 mg once daily.¹

Strong and Moderate CYP3A4 Inducers: Avoid concomitant use with LYNKUET.¹

See Prescribing Information and Dosing & Administration for detailed instructions.

Perform baseline hepatic laboratory tests to evaluate for hepatic function and injury [including serum alanine aminotransferase (ALT), serum aspartate aminotransferase (AST), serum alkaline phosphatase (ALP), and serum bilirubin (total and direct)] before initiating treatment with LYNKUET. Do not start LYNKUET if ALT or AST is ≥2 times upper limit of normal (ULN) or if the total bilirubin is ≥2 times ULN. Perform follow-up evaluations of hepatic transaminase concentration 3 months after initiation of therapy.¹

The following warnings are associated with LYNKUET¹:


Central Nervous System (CNS) Depressant Effect and Daytime Impairment

In the three OASIS trials, nervous system effects (including somnolence, fatigue, vertigo, dizziness, and presyncope) occurred in 11.9% of patients on LYNKUET compared to 3.5% on placebo. Advise patients about 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 [alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST)] concentrations equal to or greater than three times the ULN occurred in 0.6% of patients receiving LYNKUET and 0.4% of patients receiving placebo up to 12 weeks in three clinical trials. Perform baseline bloodwork (including ALT, AST, alkaline phosphatase, and total and direct bilirubin) prior to initiation of LYNKUET to evaluate for hepatic function and injury. Do not start therapy if serum transaminase concentration is equal to or exceeds two times the ULN or if the total bilirubin is equal to or exceeds two times the ULN. Perform follow-up evaluations of hepatic transaminase concentration 3 months after initiation of therapy.


Advise patients to discontinue LYNKUET immediately and seek medical attention including hepatic laboratory tests if they experience signs or symptoms that may suggest liver injury (new onset fatigue, decreased appetite, nausea, vomiting, pruritus, jaundice, pale feces, dark urine, or abdominal pain). 

Discontinue LYNKUET if transaminase elevations exceed five times the ULN or if transaminase elevations exceed three times the ULN and total bilirubin exceeds two times the ULN. 

Exclude alternative causes of hepatic laboratory test elevations.

Risk of Pregnancy Loss

LYNKUET is contraindicated for use in pregnancy. Findings from animal studies suggest that LYNKUET can cause pregnancy loss or stillbirth. Exclude pregnancy in females of reproductive potential prior to initiating LYNKUET. Advise females of reproductive potential to use effective contraception during treatment with LYNKUET and for 2 weeks after stopping LYNKUET.



Risk of Seizures in Patients with History of Seizures

Seizure was reported in one patient with a history of seizures in the clinical trials of LYNKUET. In addition, convulsions were observed in studies conducted in male and female rats. Use LYNKUET with caution in patients with a history of seizures or with conditions that potentially lower the seizure threshold.

The Common Adverse Reactions Reported in ≥ 2% in LYNKUET and Greater than Placebo in a 52-week study were: headache (9.6% vs 7.0%), fatigue (7.3% vs 2.9%), dizziness (6.1% vs 1.9%), somnolence (5.1% vs 1.3%), abdominal pain (4.5% vs 2.5%), rash (4.2% vs 1.6%), diarrhea (3.8% vs 1.0%), and muscle spasms (3.2% vs 0.6%).¹

Please see the Prescribing Information.

LYNKUET is contraindicated in pregnancy. Exposure to LYNKUET may cause pregnancy loss or stillbirth when administered during pregnancy.¹

Elinzanetant is primarily metabolized via CYP3A4 enzyme.¹

Drug Interactions: Concomitant Use of Other Drugs Affect the Use of LYNKUET
Strong and Moderate CYP3A4 Inhibitors¹

Prevention or Management

• Strong CYP3A4 Inhibitors and grapefruit (juice): Avoid concomitant use
• Moderate CYP3A4 Inhibitors: Reduce the LYNKUET dosage

Clinical Effect(s)

• Strong and moderate CYP3A4 inhibitors increase elinzanetant exposure, which may increase the risk of LYNKUET-associated adverse reactions

Strong and Moderate CYP3A4 Inducers¹

Prevention or Management

• Strong and moderate CYP3A4 inducers: Avoid concomitant use

Clinical Effect(s)

• Strong and moderate CYP3A4 inducers decrease elinzanentant exposure, which may reduce the effectiveness of LYNKUET

Effects of LYNKUET on Other Drugs
CYP3A4 Substrates
Avoid concomitant use unless otherwise recommended in the Prescribing Information for CYP3A4 substrates where minimal concentration changes may lead to serious adverse reactions. 

Elinzanetant is a weak inhibitor of CYP3A4. Concomitant use of LYNKUET increases exposure of CYP3A4 substrates, which may increase the risk of adverse reactions related to these substrates.

The LYNKUET resources page has tools to help you, your office, and your eligible patients get started with LYNKUET such as an access guide and sample letters to walk your office through completing coverage requests on behalf of your patients.

LYNKUET may not be covered by all commercial plans right away, but Bayer is dedicated to ensuring all appropriate women can access it. Through our partnership with BlinkRx, a digital pharmacy service, patients can get LYNKUET at the lowest available cost. See the Savings & Support page for more details.

As a Leader in Women’s Healthcare, Bayer has partnered with BlinkRx, a digital pharmacy service, to provide the LYNKUET Access Savings & Support program (LASS) to help your eligible patients get started on LYNKUET at the lowest available cost.
See the Savings & Support page for more details.

Commercially insured patients may be eligible for the Copay Savings Program for LYNKUET, which may reduce their copay to as little as $25 per month.*

Commercial patients who use BlinkRx will be automatically enrolled in the Copay Savings Program.

Patients using retail pharmacies must apply for the Copay Savings Program by visiting LynkuetSavings.com and provide the copay card to their pharmacy when picking up their prescription.

*Patients are eligible if they are commercially insured. Benefit limitations apply. Patients who are enrolled in any type of government insurance or reimbursement programs are not eligible. Full terms and conditions apply. Call 844-LYNKUET or visit  

LynkuetSavings.com

 for more information.

BlinkRx works with all appropriate patients to determine coverage, automatically identify savings, and apply the lowest possible costs. 

• With BlinkRx, eligible commercial patients may pay as little as $25 per month for LYNKUET.*
• If the patient’s government health insurance plan does not cover LYNKUET or there are challenges affording their prescription cost, BlinkRx can provide affordability options to patients to access LYNKUET at the lowest available cost.

*Terms and Conditions apply. Not available in Puerto Rico. Patient Affordability Program only available through BlinkRx. Click

here

for full Terms and Conditions.

Learn more at Savings & Support page.