Related medicinesFezolinetantElinzanetant
Where it comes from
- Made in
- The KNDy neurons of the arcuate nucleus, which make kisspeptin, neurokinin B and dynorphin together
- Sent out by
- Within the KNDy network, each pulse of GnRH; unrestrained after menopause when oestrogen is gone
- Acts on
- KNDy neurons themselves (synchrony)
- The thermoregulatory centre of the preoptic area
What it does
- Synchronises the KNDy neurons into the pulses that drive GnRH
- With oestrogen gone, overactive KNDy neurons fire the heat-loss centre: the hot flush
- Loss of neurokinin B or its receptor causes hypogonadotropic hypogonadism
In medicine
- Fezolinetant (2023), an NK3R blocker, treats the hot flushes of menopause without hormones; elinzanetant, which blocks NK1 and NK3, followed in 2025 1
- An infusion of neurokinin B provokes flushing in volunteers
- Liver blood tests are checked before and during fezolinetant treatment, after reports of serious liver injury 4
Beyond the body’s own use
- In the SKYLIGHT 1 phase 3 trial, 527 women were randomised and fezolinetant cut both the frequency and the severity of hot flushes against placebo at four and twelve weeks 1
- Elinzanetant did the same in the OASIS 1 and 2 trials, about 400 women each, and also improved sleep disturbance 2
- The FDA added a warning in December 2024 about rare but serious liver injury with fezolinetant, with monthly liver blood tests advised for the first three months 4
- Blocking NK3R in polycystic ovary syndrome lowered LH by half and total testosterone by a quarter in a phase 2 trial of 65 women; no approved use has followed 3
Sources
- Lederman et al., Fezolinetant for moderate-to-severe vasomotor symptoms (SKYLIGHT 1), Lancet 2023
- Pinkerton et al., Elinzanetant for vasomotor symptoms, OASIS 1 and 2, JAMA 2024
- George et al., Neurokinin B receptor antagonism in women with polycystic ovary syndrome, Journal of Clinical Endocrinology and Metabolism 2016
- FDA drug safety communication, Serious liver injury with Veozah (fezolinetant)
This card describes what a medicine is for and what the evidence says; it recommends nothing. Talk to your clinician about anything you read here.