Elinzanetant (Lynkuet) Dosing for Menopausal Hot Flashes
The recommended dosage of LYNKUET is 120 mg (two 60 mg capsules) taken orally once daily at bedtime at about the same time each day. [1] Treatment is continued with dosing adjustments based on interacting drugs and hepatic laboratory status. [1]
Administration Instructions
LYNKUET is taken with or without food. [1] Each dose is swallowed whole with water. [1] If a bedtime dose is missed, the next dose is taken as scheduled the following day. [1] Two doses are not taken on the same day to make up for a missed dose. [1]
Drug-Interaction Dosage Modifications
Concomitant use with strong CYP3A4 inhibitors and grapefruit (juice) is avoided. [1] Concomitant use with moderate CYP3A4 inhibitors requires a dose reduction to 60 mg orally once daily at bedtime. [1] After discontinuation of a moderate CYP3A4 inhibitor, LYNKUET is returned to the usual 120 mg once-daily dosage after 3 to 5 half-lives of the inhibitor. [1] Concomitant use with strong and moderate CYP3A4 inducers is avoided. [1]
Monitoring Before Initiation
Baseline hepatic laboratory tests are required before starting LYNKUET, including ALT, AST, alkaline phosphatase, and total and direct bilirubin. [1] LYNKUET is not started if ALT or AST is greater than or equal to 2 times the upper limit of normal (ULN). [1] LYNKUET is not started if total bilirubin is greater than or equal to 2 times the ULN. [1]
Ongoing Monitoring During Therapy
Follow-up hepatic transaminase testing is performed 3 months after initiation of therapy. [1] Patients are monitored for signs or symptoms of liver injury, including new onset fatigue, decreased appetite, nausea, vomiting, pruritus, jaundice, pale feces, dark urine, or abdominal pain. [1] LYNKUET is discontinued and hepatic laboratory testing is obtained promptly if signs or symptoms suggesting liver injury occur. [1]
Discontinuation Thresholds for Hepatic Laboratory Abnormalities
LYNKUET is discontinued if transaminase elevations exceed 5 times the ULN. [1] LYNKUET is discontinued if transaminase elevations exceed 3 times the ULN with total bilirubin exceeding 2 times the ULN. [1] Alternative causes of hepatic laboratory test elevations are excluded. [1]
Age-Specific and Organ Impairment Considerations
No dose adjustment is required for patients with mild to severe renal impairment defined as eGFR 15 to less than 90 mL/min. [1] End-stage renal disease (eGFR <15 mL/min) with or without hemodialysis is not recommended. [1] No dose adjustment is required for mild (Child-Pugh A) hepatic impairment. [1] LYNKUET is not recommended for moderate or severe hepatic impairment (Child-Pugh B or C). [1]
Clinical Safety Monitoring Beyond Hepatic Function
LYNKUET has central nervous system effects including somnolence, fatigue, vertigo, dizziness, and presyncope. [1] Nervous system effects occurred in 11.9% of patients receiving LYNKUET compared with 3.5% receiving placebo in the OASIS trials. [1] Patients experiencing nervous system effects are advised to refrain from driving or engaging in hazardous activities until the effects resolve. [1]
Patient Counseling Considerations for a 77-Year-Old
Pregnancy-related precautions are not applicable to most patients at age 77, but LYNKUET labeling includes a contraindication in pregnancy. [1] Medication review for CYP3A4 inhibitors, CYP3A4 inducers, and grapefruit (juice) is performed to prevent clinically important exposure changes. [1]