Fezotan

Fezolinetant is a neurokinin 3 (NK3) receptor antagonist that blocks neurokinin B (NKB) binding on the kisspeptin/neurokinin B/dynorphin (KNDy) neuron to modulate neuronal activity in the thermoregulatory center. Fezolinetant has high affinity for the NK3 receptor (Ki value of 19.9 to 22.1 nmol/L), which is more than 450-fold higher than binding affinity to NK1 or NK2 receptors.

Treatment with fezolinetant did not show any clear trends in sex hormones measured (follicle-stimulating hormone, testosterone, estrogen, and dehydroepiandrosterone sulfate) in menopausal women. Transient decrease of luteinizing hormone (LH) levels was observed at peak concentrations of fezolinetant.

Fezolinetant is a substrate of CYP1A2. Concomitant use of Fezolinetant with drugs that are weak, moderate, or strong CYP1A2 inhibitors, increase the plasma Cmax and AUC of Fezolinetant. Fezolinetant is contraindicated in individuals using CYP1A2 inhibitors.

Common side efects of Fezolinetant include:

• stomach (abdominal) pain
• diarrhea
• difculty sleeping
• back pain
• hot fashes or hot fushes

Stop Fezolinetant if you have the following signs or symptoms of liver problems:

• nausea
• vomiting
• itching
• yellowing of the eyes or skin (jaundice)
• pale feces
• dark urine
• pain in the right upper stomach (abdomen)

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. 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.

Hepatic Transaminase Elevation and Hepatotoxicity: Elevations in serum transaminase concentrations greater than 3 times the upper limit of normal (ULN) occurred in the clinical trials. Perform hepatic laboratory tests prior to initiation of Fezolinetant to evaluate for hepatic function and injury. Patient should not start Fezolinetant if the concentration of alanine aminotransferase (ALT) or aspartate aminotransferase (AST) is equal to or exceeds 2 times the ULN or if the total bilirubin is elevated (for example, equal to or exceeds 2 times the ULN) for the evaluating laboratory. Patient should perform follow-up hepatic laboratory tests monthly for the frst 3 months, at 6 months, and 9 months after initiation of therapy.

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

Store below 30°C. Keep away from light and out of the reach of children.