Fezolinetant

Fezolinetant was approved for marketing in the United States on May 12, 2023, for the treatment of moderate to severe vasomotor symptoms (VMS) caused by menopause.

On December 7th of the same year, the drug also obtained marketing authorization in Europe under the trade name Veoza.

Fezolinetant reduces the frequency and severity of severe VMS in menopause by blocking the binding of neurokinin B (NKB) to kispeptin/neurokinin/dynorphin (KNDy) neurons.

1.Main components

Fezolinetant

2.Adapt to the population

Fezolinetant is indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.

3.Medication for special populations

3.1Pregnancy

There are no data on Fezolinetant use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

3.2Lactation

There are no data on the presence of fezolinetant in human milk, the effects on the breastfed child, or the effects on milk production. It is not known if fezolinetant is present in human milk.

3.3Pediatric Use

The efficacy and safety of Fezolinetant in individuals less than 18 years of age have not been established.

3.4Geriatric Use

There have not been sufficient numbers of geriatric women involved in clinical trials utilizing Fezolinetant to determine  whether those over 65 years of age differ from younger women in their response to Fezolinetant.

3.5Renal Impairment

Fezolinetant is contraindicated in individuals with severe (eGFR 15 to less than 30 mL/min/1.73 m2 ) renal impairment or  end-stage renal disease (eGFR less than 15 mL/min/1.73 m2 ). No dose adjustment of  Fezolinetant is recommended for individuals with mild (eGFR 60 to less than 90 mL/min/1.73 m2 ) or moderate (eGFR 30 to  less than 60 mL/min/1.73 m2 ) renal impairment.

3.6Hepatic Impairment

Child-Pugh Class A or B hepatic impairment increased the exposure of Fezolinetant.  Fezolinetant has not been studied in individuals with Child-Pugh Class C hepatic impairment. 

Fezolinetant is contraindicated in individuals with cirrhosis.

4.Drug overdose

Treatment of overdose consists of discontinuation of Fezolinetant therapy with institution of appropriate symptomatic care.

5.Drug storage

Store at 20°C to 25°C (68°F to 77°F) with excursions permitted from 15°C to 30°C (59°F to 86°F).

6.Pharmacokinetics

The median (range) time to reach fezolinetant Cmax is 1.5 (1 to 4) hours in healthy women.

from FDA，2024.08