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VEOZAH is not a hormone.
It’s a first-in-class selective NK3R antagonist that works differently to directly block NKB, a known trigger of VMS, from binding on the KNDy neuron1,3,4
It’s a first-in-class selective NK3R antagonist that works differently to directly block NKB, a known trigger of VMS, from binding on the KNDy neuron1,3,4
KNDy=kisspeptin/neurokinin B/dynorphin, NK3R=neurokinin 3 receptor, NKB=neurokinin B.
Reduce
KNDy NEURONAL ACTIVITY
Balance
THERMO- REGULATORY ACTIVITY
Block
THE BINDING OF NKB
Watch the MOA of VEOZAH
How VEOZAH disrupts hot flashes1
ESTROGEN ALPHA RECEPTOR
NKB
NK3 RECEPTOR
Thermoregulatory homeostasis
KNDy neurons in the hypothalamus are inhibited by estrogen and stimulated by the neuropeptide NKB. This balance contributes to body temperature regulation.5
Impact of NKB
Estrogen decline during the menopause transition disrupts this balance with NKB. Unopposed, NKB signaling causes heightened KNDy neuronal activity.5
The thermoregulatory center triggers heat dissipation mechanisms, including vasodilation and sweating—VMS.5
VEOZAH inhibits
binding of NKB to NK3 R
VEOZAH is a nonhormonal selective NK3R antagonist that blocks NKB binding on the KNDy neuron to modulate neuronal activity in the thermoregulatory center. This action helps to reduce the number and intensity of hot flashes and night sweats.1
VEOZAH directly targets NK3R with a high affinity, more than 450-fold higher than NK1 or NK2 receptors.1
KNDy=kisspeptin/neurokinin B/dynorphin, NK1=neurokinin 1, NK2=neurokinin 2, NK3R=neurokinin 3 receptor, NKB=neurokinin B.
IMPORTANT SAFETY INFORMATION
INDICATIONS AND USAGE
EXPAND
COLLAPSE
COLLAPSE
IMPORTANT SAFETY INFORMATION
INDICATIONS AND USAGE
CONTRAINDICATIONS
VEOZAH is contraindicated in women with any of the following:
- Known cirrhosis
- Severe renal impairment or end-stage renal disease
- Concomitant use with CYP1A2 inhibitors
VEOZAH® (fezolinetant) is a neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.
CONTRAINDICATIONS
VEOZAH is contraindicated in women with any of the following:
- Known cirrhosis
- Severe renal impairment or end-stage renal disease
- Concomitant use with CYP1A2 inhibitors
INDICATIONS AND USAGE
VEOZAH® (fezolinetant) is a neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.
WARNINGS AND PRECAUTIONS
Hepatic Transaminase Elevation
Elevations in serum transaminase [alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST)] levels > 3x the upper limit of normal (ULN) occurred in 2.3% of women receiving VEOZAH and 0.9% of women receiving placebo in three clinical trials. No serum elevations in total bilirubin (> 2x ULN) occurred. Women with ALT or AST elevations were generally asymptomatic. Transaminase levels returned to pretreatment levels (or close to these) without sequelae with dose continuation, and upon dose interruption, or discontinuation. Women with cirrhosis were not studied.
Perform baseline bloodwork to evaluate for hepatic function and injury prior to VEOZAH initiation. Do not start VEOZAH if concentration of ALT or AST is ≥ 2x ULN or if the total bilirubin is elevated (e.g., ≥ 2x ULN) for the evaluating laboratory. If baseline hepatic transaminase evaluation is < 2x ULN and the total bilirubin is normal, VEOZAH can be started. Perform follow-up evaluations of hepatic transaminase concentration at 3 months, 6 months, and 9 months after initiation of therapy and when symptoms (such as nausea, vomiting, or yellowing of the skin or eyes) suggest liver injury.
ADVERSE REACTIONS
The most common adverse reactions with VEOZAH ≥ 2% and > placebo (VEOZAH % vs. placebo %) are: abdominal pain (4.3% vs. 2.1%), diarrhea (3.9% vs. 2.6%), insomnia (3.9% vs. 1.8%), back pain (3.0% vs. 2.1%), hot flush (2.5% vs. 1.6%), and hepatic transaminase elevation (2.3% vs. 0.8%).
Please click here for full Prescribing Information for VEOZAH® (fezolinetant).
REFERENCES: 1. VEOZAH [package insert]. Northbrook, IL: Astellas Pharma US, Inc. 2. Thurston RC. Vasomotor symptoms. In: Crandall CJ, Bachman GA, Faubion SS, et al., eds. Menopause Practice: A Clinician’s Guide. 6th ed. Pepper Pike, OH: The North American Menopause Society, 2019:43-55. 3. The North American Menopause Society. The 2023 nonhormone therapy position statement of the North American Menopause Society. Menopause 2023;30(6):573-90. 4. Jayasena CN, Comninos AN, Stefanopoulou E, et al. Neurokinin B administration induces hot flushes in women. Sci Rep (Epub) 02-16-2015. 5. Depypere H, Lademacher C, Siddiqui E, Fraser GL. Fezolinetant in the treatment of vasomotor symptoms associated with menopause. Expert Opin Investig Drugs 2021;30(7):681-94.