Elinzanetant (1 brand name, 1 dosage form, 1 route)
Available dosage forms: CAPSULE.
Routes of administration: ORAL.
Brand Names
- LYNKUET
Indications and Usage
LYNKUET is indicated for the treatment of moderate to severe vasomotor symptoms (VMS) due to menopause.
Contraindications
LYNKUET is contraindicated in pregnancy. Exposure to LYNKUET may cause pregnancy loss or stillbirth when administered during pregnancy [see Use in Specific Populations (8.1, 8.3)].
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: Central Nervous System (CNS) Depressant Effect and Daytime Impairment [see Warnings and Precautions (5.1)] Hepatic Transaminase Elevations [see Warnings and Precautions (5.2)]
Mechanism of Action
LYNKUET is a neurokinin 1 (NK1) and neurokinin 3 (NK3) receptor antagonist. 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. 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).
Overdosage
There is no specific antidote for LYNKUET. In the case of overdose, the individual should be closely monitored, and supportive treatment should be considered based on signs and symptoms.