Formulary
Fezolinetant: Indications, Dosing, Side Effects and Interactions
Fezolinetant is a non-hormonal neurokinin-3 receptor antagonist that modulates neuronal activity in the hypothalamic thermoregulatory centre.
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Fezolinetant: Indications, Dosing, Side Effects and Interactions
Fezolinetant is a non-hormonal neurokinin-3 receptor antagonist that modulates neuronal activity in the hypothalamic thermoregulatory centre.
Drug action
Fezolinetant is a non-hormonal neurokinin-3 receptor antagonist that modulates neuronal activity in the hypothalamic thermoregulatory centre.
Indications and dose
**Moderate to severe vasomotor symptoms associated with menopause**
- **Adult** (By Mouth): 18-65 years 45 mg once daily.
Side effects
Common or very common Abdominal pain; diarrhoea; insomnia Frequency not known Drug-induced liver injury; endometrial adenocarcinoma
Interactions
**Other interactions (11):**
- Effect of other medicinal products on fezolinetant CYP1A2 inhibitors Fezolinetant is primarily metabolised by CYP1A2 and to a lesser extent by CYP2C9 and CYP2C19.
- Concomitant use of fezolinetant with medicinal products that are moderate or strong inhibitors of CYP1A2 (e.g., ethinyl oestradiol containing contraceptives, mexiletine, enoxacin, fluvoxamine)...
- Co-administration with fluvoxamine, a strong CYP1A2 inhibitor, resulted in an overall 1.8-fold increase in fezolinetant C max and 9.4-fold increase in AUC; no change in t max was observed.
- Given the large effect of a strong CYP1A2 inhibitor and supportive modelling, the increase in fezolinetant concentrations is expected to be of clinical concern also following concomitant use with...
- The increase in fezolinetant exposure was however not predicted to be clinically relevant following concomitant use with weak CYP1A2 inhibitors.
- CYP1A2 inducers In vivo data Smoking (moderate inducer of CYP1A2) decreased fezolinetant C max to a geometric LS mean ratio of 71.74%, while AUC decreased to a geometric LS mean ratio of 48.29%.
Pregnancy
Avoid (toxicity in animal studies). M
Breast feeding
Avoid (present in milk in animal studies). M
Hepatic impairment
Avoid in moderate to severe impairment (risk of increased exposure). M See also Important safety information .
Renal impairment
Avoid if eGFR less than 30 mL/minute/1.73 m 2 (limited information available). M See Prescribing in renal impairment .
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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