fezolinetant at a glance
Medicine class
Selective neurokinin-3 receptor antagonist
Main use
Moderate to severe menopausal hot flushes and night sweats
Administration
Swallow the tablet whole with liquid; it may be taken with or without food
Important monitoring
Liver blood tests are required before and during treatment
What is fezolinetant used for?
The selected UK product is licensed for:
Treatment of moderate to severe vasomotor symptoms associated with menopause, including hot flushes and night sweats.
How does fezolinetant work?
Falling oestrogen levels around menopause can disturb neurokinin B signalling in the hypothalamus, affecting temperature regulation. Fezolinetant blocks neurokinin-3 receptors on KNDy neurons, helping stabilise this system without acting as an oestrogen.
fezolinetant preparations and strengths
Tablet
Route: Oral
Strengths: 45 mg
How to take fezolinetant
Follow the prescriber’s directions and use the tablet consistently.
Swallow whole with liquid.
Do not break, crush or chew the tablet.
It may be taken with or without food.
fezolinetant side effects
Common or expected effects
- Diarrhoea
- Difficulty sleeping
- Abdominal pain
- Raised ALT or AST liver enzymes on blood tests
Get urgent medical advice
- Drug-induced liver injury, which may cause jaundice, dark urine, pale stools, itching, marked tiredness, nausea, vomiting, reduced appetite or abdominal pain
fezolinetant in pregnancy
Fezolinetant is contraindicated in known or suspected pregnancy. If pregnancy occurs, it should be stopped and the prescriber contacted promptly. People who could become pregnant should use effective non-hormonal contraception because some ethinyl-oestradiol contraceptives interact with fezolinetant.
fezolinetant while breastfeeding
Fezolinetant is not indicated while breastfeeding, and transfer into human milk is unknown. A prescriber should weigh the benefits of breastfeeding against the need for treatment because risk to the child cannot be excluded.
fezolinetant interactions
A pharmacist or prescriber should check all medicines before treatment, including contraception and non-prescription products.
Moderate or strong CYP1A2 inhibitors
These can substantially increase fezolinetant exposure and must not be used concurrently.
Fluvoxamine
Strong CYP1A2 inhibition markedly increases fezolinetant exposure, so concurrent use is contraindicated.
Mexiletine or enoxacin
These inhibit CYP1A2 and must not be taken with fezolinetant.
Ethinyl-oestradiol-containing contraceptives
Common questions about fezolinetant
Answers are fully visible for fast scanning and source review.
What is fezolinetant used for?
It treats moderate to severe hot flushes and night sweats associated with menopause.
Is fezolinetant a hormone?
No. It is a non-hormonal neurokinin-3 receptor antagonist and does not replace oestrogen.
Can fezolinetant be taken with food?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.