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For the treatment of moderate to severe Vasomotor Symptoms (VMS)—commonly referred to as hot flashes and night sweats—due to menopause1,2

Woman spraying VEOZAH™ (fezolinetant) logo fire extinguisher in office

REDEFINEhowYOU
TARGET VMS

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

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

Hypothalamus shown in brain Hypothalamus shown in brain

Watch the MOA of VEOZAH

TRANSCRIPT

Mechanism of action

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MOA video transcript

6 mins 30 secs 

Moderate to severe Vasomotor Symptoms, also known as VMS or hot flashes and night sweats, are the most bothersome symptoms of menopause. Growing evidence has led to a different treatment pathway that directly targets a source of VMS in the hypothalamus.

Meet VEOZAH™ (fezolinetant). VEOZAH is not a hormone. It is a first-in-class NK3R antagonist that works differently to directly block a mechanism that triggers VMS.

KNDy neurons in the hypothalamus are inhibited by estrogen and stimulated by the neuropeptide NKB. This balance contributes to body temperature regulation. During the menopause transition, estrogen decline disrupts this balance with NKB. Unopposed, NKB signaling causes heightened KNDy activity and altered activity on the thermoregulatory center, resulting in VMS.

VEOZAH directly targets this source of VMS. By selectively binding to NK3R, VEOZAH blocks NKB, modulating neuronal activity in the thermoregulatory center to reduce heat signaling that triggers hot flashes and night sweats.

It’s time to put the mechanism of VEOZAH to work for your appropriate VMS patients.

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.

IMPORTANT SAFETY INFORMATION

WARNING: RISKS OF HEPATOTOXICITY

Hepatotoxicity has occurred with the use of VEOZAH in the postmarketing setting.

  • Perform hepatic laboratory tests prior to initiation of treatment to evaluate for hepatic function and injury. Do not start VEOZAH if either aminotransferase is ≥ 2x the upper limit of normal (ULN) or if the total bilirubin is ≥ 2x 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.
  • 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).
  • Discontinue VEOZAH if transaminase elevations are > 5x ULN, or if transaminase elevations are > 3x ULN and the total bilirubin level is > 2x ULN.
  • If transaminase elevations > 3x ULN occur, perform more frequent follow-up hepatic laboratory tests until resolution.

CONTRAINDICATIONS

VEOZAH is contraindicated in women with any of the following:

  1. Known cirrhosis
  2. Severe renal impairment or end-stage renal disease
  3. Concomitant use with CYP1A2 inhibitors

WARNINGS AND PRECAUTIONS

Hepatotoxicity

In 3 clinical trials, elevations in serum transaminase [alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST)] levels > 3x ULN occurred in 2.3% of women receiving VEOZAH and 0.9% of women receiving placebo. No elevations in serum 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.

In the postmarketing setting, cases of drug-induced liver injury with elevations of ALT, AST, alkaline phosphatase (ALP), and total bilirubin occurred within 40 days of starting VEOZAH. Patients reported a general sense of feeling unwell and symptoms of fatigue, nausea, pruritus, jaundice, pale feces, and dark urine. The patients’ signs and symptoms gradually resolved after discontinuation of VEOZAH.

Perform baseline hepatic laboratory tests to evaluate for hepatic function and injury [including serum ALT, serum AST, serum ALP, and serum bilirubin (total and direct)] prior to VEOZAH initiation. Do not start VEOZAH if ALT or AST is ≥ 2x ULN or if the total bilirubin is ≥ 2x ULN for the evaluating laboratory.

Perform follow-up hepatic laboratory tests monthly for the first 3 months, at 6 months, and 9 months after initiation of therapy.

See BOXED WARNING for full hepatic laboratory testing protocol and discontinuation criteria. Exclude alternative causes of hepatic laboratory test elevations.

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 see accompanying full Prescribing Information, including BOXED WARNING, for VEOZAH (fezolinetant).

 BACK TO VIDEO

How VEOZAH disrupts hot flashes1

Estrogen
ESTROGEN
Estrogen alpha receptor
ESTROGEN ALPHA RECEPTOR
Neurokinin B
NKB
Neurokinin 3 receptor
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

Thermoregulatory homeostasis showing the KNDy neuron inhibited by estrogen and stimulated by NKB

MECHANISM OF ACTION

TRANSCRIPT

MECHANISM OF ACTION

MECHANISM OF ACTION

MECHANISM OF ACTION

Impact of NKB

Estrogen decline during the menopause transition disrupts this balance. Unopposed, NKB signaling causes heightened KNDy neuronal activity.5

The thermoregulatory center triggers heat dissipation mechanisms, including vasodilation and sweating—VMS.5

MECHANISM OF ACTION

MECHANISM OF ACTION

MECHANISM OF ACTION

MECHANISM OF ACTION

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

MECHANISM OF ACTION

MECHANISM OF ACTION

MECHANISM OF ACTION

MECHANISM OF ACTION

KNDy=kisspeptin/neurokinin B/dynorphin, NK1=neurokinin 1, NK2=neurokinin 2, NK3R=neurokinin 3 receptor, NKB=neurokinin B.

RESOURCE

Share the first-in-class MOA of VEOZAH1,3

Quickly reference VEOZAH in your practice.

Share the first-in-class MOA of VEOZAH1,3

Quickly reference VEOZAH in your practice.

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Mechanism of action flashcard

IMPORTANT SAFETY INFORMATION

INDICATIONS AND USAGE

EXPAND COLLAPSE

IMPORTANT SAFETY INFORMATION

INDICATIONS AND USAGE

WARNING: RISKS OF HEPATOTOXICITY

Hepatotoxicity has occurred with the use of VEOZAH in the postmarketing setting.

  • Perform hepatic laboratory tests prior to initiation of treatment to evaluate for hepatic function and injury. Do not start VEOZAH if either aminotransferase is ≥ 2x the upper limit of normal (ULN) or if the total bilirubin is ≥ 2x 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.
  • 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).
  • Discontinue VEOZAH if transaminase elevations are > 5x ULN, or if transaminase elevations are > 3x ULN and the total bilirubin level is > 2x ULN.
  • If transaminase elevations > 3x ULN occur, perform more frequent follow-up hepatic laboratory tests until resolution.

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:

  1. Known cirrhosis
  2. Severe renal impairment or end-stage renal disease
  3. Concomitant use with CYP1A2 inhibitors

WARNING: RISKS OF HEPATOTOXICITY

Hepatotoxicity has occurred with the use of VEOZAH in the postmarketing setting.

  • Perform hepatic laboratory tests prior to initiation of treatment to evaluate for hepatic function and injury. Do not start VEOZAH if either aminotransferase is ≥ 2x the upper limit of normal (ULN) or if the total bilirubin is ≥ 2x 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.
  • 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).
  • Discontinue VEOZAH if transaminase elevations are > 5x ULN, or if transaminase elevations are > 3x ULN and the total bilirubin level is > 2x ULN.
  • If transaminase elevations > 3x ULN occur, perform more frequent follow-up hepatic laboratory tests until resolution.
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.

CONTRAINDICATIONS

VEOZAH is contraindicated in women with any of the following:

  1. Known cirrhosis
  2. Severe renal impairment or end-stage renal disease
  3. Concomitant use with CYP1A2 inhibitors

WARNINGS AND PRECAUTIONS

Hepatotoxicity

In 3 clinical trials, elevations in serum transaminase [alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST)] levels > 3x ULN occurred in 2.3% of women receiving VEOZAH and 0.9% of women receiving placebo. No elevations in serum 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.

In the postmarketing setting, cases of drug-induced liver injury with elevations of ALT, AST, alkaline phosphatase (ALP), and total bilirubin occurred within 40 days of starting VEOZAH. Patients reported a general sense of feeling unwell and symptoms of fatigue, nausea, pruritus, jaundice, pale feces, and dark urine. The patients’ signs and symptoms gradually resolved after discontinuation of VEOZAH.

Perform baseline hepatic laboratory tests to evaluate for hepatic function and injury [including serum ALT, serum AST, serum ALP, and serum bilirubin (total and direct)] prior to VEOZAH initiation. Do not start VEOZAH if ALT or AST is ≥ 2x ULN or if the total bilirubin is ≥ 2x ULN for the evaluating laboratory.

Perform follow-up hepatic laboratory tests monthly for the first 3 months, at 6 months, and 9 months after initiation of therapy.

See BOXED WARNING for full hepatic laboratory testing protocol and discontinuation criteria. Exclude alternative causes of hepatic laboratory test elevations.

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, including BOXED WARNING, 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.