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ELINZANETANT
LYNKUET blocks NK1 and NK3 receptors, reducing Substance P and Neurokinin B signaling to modulate neuronal activity in thermoregulation.
Elinzanetant is a marketed drug designed to address moderate to severe vasomotor symptoms due to menopause by blocking NK1 and NK3 receptors, thereby modulating neuronal activity in thermoregulation. Its key strength lies in its dual receptor blockade mechanism, which effectively reduces Substance P and Neurokinin B signaling, potentially offering superior symptom control compared to single-target therapies. The primary risk is the key composition patent expiry in 2028, which could lead to increased competition from generic alternatives.
At a glance
| Generic name | ELINZANETANT |
|---|---|
| Target | NK1, NK3 |
| Modality | Small molecule |
| Phase | FDA-approved |
Mechanism of action
LYNKUET works by blocking the NK1 and NK3 receptors, which are involved in the signaling of Substance P and Neurokinin B. By inhibiting these receptors, it reduces the activity of KNDy neurons, which play a role in regulating body temperature and can help reduce hot flashes.
Approved indications
- Moderate to severe vasomotor symptoms due to menopause
Common side effects
- Headache
- Fatigue
- Dizziness
- Somnolence
- Abdominal pain
- Rash
- Diarrhea
- Muscle spasms
Drug interactions
- Strong CYP3A4 Inhibitors and grapefruit (juice)
- Moderate CYP3A4 Inhibitors
- Strong and Moderate CYP3A4 Inducers
- CYP3A4 Substrates
Key clinical trials
- An Observational Study to Learn More About How Elinzanetant is Used and How Well it Works for Women With Menopause Symptoms in United States
- A Study to Learn More About How Well Elinzanetant Works and How Safe it is for the Treatment of Vasomotor Symptoms (Hot Flashes) That Are Caused by Hormonal Changes Over 26 Weeks in Women Who Have Been Through the Menopause (PHASE3)
- A Study to Learn More About How Well Elinzanetant Works and How Safe it is for the Treatment of Vasomotor Symptoms (Hot Flashes) That Are Caused by Hormonal Changes Over 26 Weeks in Women Who Have Been Through the Menopause (OASIS-2) (PHASE3)
- Finding Links Between Hot flASHes and CardioVascular Disease (PHASE2)
- A Study to Learn More About How Well Elinzanetant Works and How Safe it is Compared to Placebo for the Treatment of Hot Flashes Caused by Anti-cancer Therapy in Women With, or at High Risk for Developing Hormone-receptor Positive Breast Cancer (PHASE3)
- A Study to Investigate Relative Bioavailability, Safety and Tolerability of Single- and Multiple-doses of Elinzanetant in Healthy Female Participants (PHASE1)
- A Study to Learn More About How Well Elinzanetant Works and How Safe it is for the Treatment of Vasomotor Symptoms (Hot Flashes) That Are Caused by Hormonal Changes Over 52 Weeks in Women Who Have Been Through the Menopause (PHASE3)
- A Study to Learn About How Elinzanetant Works and How Safe it is in Women Having Sleep Disturbances Associated With Menopause (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |