Fezolinetant (1 brand name, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- VEOZAH
Boxed Warning
Hepatotoxicity has occurred with the use of VEOZAH in the postmarketing setting (5.1). • Perform hepatic laboratory tests prior to initiation of treatment to evaluate for hepatic function and injury. Do not start VEOZAH if either aminotransferase is ≥ 2 x the upper limit of normal (ULN) or if the total bilirubin is ≥ 2 x ULN for the evaluating laboratory. • Perform follow-up hepatic laboratory testing monthly for the first 3 months, at 6 months, and 9 months of treatment (2.1, 5.1). • Advise patients to discontinue VEOZAH immediately and seek medical attention including hepatic laboratory tests if they experience signs or symptoms that may suggest liver injury (new onset fatigue, decreased appetite, nausea, vomiting, pruritus, jaundice, pale feces, dark urine, or abdominal pain) (2.1, 5.1). • Discontinue VEOZAH if transaminase elevations are > 5 x ULN, or if transaminase elevations are > 3 x ULN and the total bilirubin level is > 2 x ULN. • If transaminase elevations > 3 x ULN occur, perform more frequent follow-up hepatic laboratory tests until resolution (5.1).
Indications and Usage
VEOZAH® is indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.
Contraindications
VEOZAH is contraindicated in women with any of the following conditions: •Known cirrhosis [see Warnings and Precautions ( 5.1), Use in Specific Populations (8.7), and Clinical Pharmacology (12.3)]. •Severe renal impairment or end-stage renal disease [see Use in Specific Populations (8.6) and Clinical Pharmacology ( 12.3)]. •Concomitant use with CYP1A2 inhibitors [see Drug Interactions (7.1) and Clinical Pharmacology ( 12.3)].
Adverse Reactions
The following serious adverse reactions are discussed elsewhere in the labeling: •Hepatic Transaminase Elevation and Hepatotoxicity [see Warnings and Precautions (5.1)].
Mechanism of Action
VEOZAH 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.
Overdosage
Treatment of overdose consists of discontinuation of VEOZAH therapy with institution of appropriate symptomatic care.