elinzanetant

Action and Spectrum

Actions: 

Elinzanetant is a neurokinin-1,3 receptor antagonist that works by blocking the activity of neurokinin B (NKB) and substance P, two neurotransmitters involved in regulating body temperature and reproductive hormone pathways. 

During menopause, declining estrogen levels lead to increased NKB signaling in a region of the hypothalamus known as the median preoptic nucleus, which plays a key role in thermoregulation. This overactivation disrupts the body’s temperature control, resulting in vasomotor symptoms (VMS) such as hot flashes and night sweats. 

Drug Interaction

Adverse Reaction

Frequency Defined   

Headache 

Fatigue or asthenia  

Somnolence (sleepiness/drowsiness)  

Dizziness  

Diarrhea 

Rash 

Muscle spasms/cramping 

Black Box Warning

Black Box Warning    

May cause central nervous system effects and daytime impairment (e.g., drowsiness, dizziness) patients advised not to drive or operate machinery if affected. 

Increased liver enzyme values were observed and require monitoring of liver function.  

Contraindication / Caution

Contraindication/Caution:   

Contraindication 

Pregnancy and breastfeeding 

Pregnancy / Lactation

Pregnancy Warnings:   

Pregnancy category: N/A   

Lactation: Excretion in human breastmilk is unknown   

Pregnancy categories:   

Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or in the later trimester.   

Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women.   

Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.   

Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women.    

Category N: There is no data available for the drug under this category.    

Pharmacology

Pharmacology:   

Elinzanetant is a neurokinin-1,3 receptor antagonist that works by blocking the activity of neurokinin B (NKB) and substance P, two neurotransmitters involved in regulating body temperature and reproductive hormone pathways. 

During menopause, declining estrogen levels lead to increased NKB signaling in a region of the hypothalamus known as the median preoptic nucleus, which plays a key role in thermoregulation. This overactivation disrupts the body’s temperature control, resulting in vasomotor symptoms (VMS) such as hot flashes and night sweats. 

Adminstartion

Administration:   

The mode of administration is oral in form of tablets. 

Patient Information Leaflet

Patient information leaflet   

Generic Name: elinzanetant 

Why do we use elinzanetant?  

Elinzanetant is primarily being developed for the management of menopausal vasomotor symptoms (VMS) such as hot flashes and night sweats in women experiencing menopause or perimenopause.