Fezolinetant
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2023
- First approval year
- 2023
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Fezolinetant
- Molecular weight
- 358.4
- Structure (SMILES)
- Cc1nsc(-c2nnc3n2CCN(C(=O)c2ccc(F)cc2)[C@@H]3C)n1
- veoza
- Veoza
- veozah
- Veozah
- a 2693
- A-2693
- a2693
- A2693
- as 3472693 00
- AS-3472693-00
- as3472693 00
- AS3472693-00
- es 256364
- ES-256364
- esn 364
- ESN-364
- esn364
- Esn364
- ESN364
- fezolinetant
- Fezolinetant
- Fezolinetant [INN]
- Fezolinetant [MI]
- Fezolinetant [USAN]
- Fezolinetant [WHO-DD]
- fezolinetant inn
- fezolinetant mi
- fezolinetant usan
- fezolinetant who dd
And 2 more, listed on the interactive page.
- ATC classification codes
- G02CX06
Sources for recorded values
- CAS registry numbers
- 1629229-37-3
- ChEMBL ID
- CHEMBL3608680
- InChIKey
- PPSNFPASKFYPMN-SECBINFHSA-N
- PubChem compound IDs
- 117604931
- RxNorm IDs (RxCUI)
- 2637134
- FDA ingredient codes (UNII)
- 83VNE45KXX
- Applicant
- ASTELLAS
- Approval date
- 12 May 2023
- Application number
- NDA216578
- Status
- Authorised
- Status date
- 7 Dec 2023
- Authorisation date
- 7 Dec 2023
- Approved indications
- Veoza is indicated for the treatment of moderate to severe vasomotor symptoms (VMS) associated with menopause.
- Product number
- EMEA/H/C/005851
- Authorisation holder
- Astellas Pharma Europe B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Hot Flashes
- Menopause
European medicines record
- Patents
- 4
- Designations
- 0
- Earliest recorded loss of exclusivity
- 28 Mar 2034
- First in class
- Yes
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- United States (FDA)
- Approved
- European Union (EMA)
- Authorised
- Pharmacology name
- fezolinetant
- Type
- Synthetic organic
- Drug name stem
- -tant
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Antagonist
- Action type
- Antagonist
- Target
- NK3 receptor
- Gene symbol
- TACR3
- Protein identifier
- P29371
- Median affinity
- 7.6
- Affinity units
- pKi
- Primary target
- Yes
- Mechanism
- Neurokinin 3 receptor antagonist
- Action type
- Antagonist
- Target
- Neuromedin-K receptor
- Protein identifier
- P29371
Open Targets mechanisms
- Mechanism
- Neurokinin 3 receptor antagonist
- Action type
- Antagonist
- Target
- Neuromedin-K receptor
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Kidney Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003086
- Subject identifier
- D007674
- Condition
- Hot Flashes
- Highest recorded phase
- 4
- Condition identifier
- HP:0031217
- Subject identifier
- D019584
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003086
- Highest recorded phase
- 1
- Condition identifier
- GO_0042697
- Condition identifier
- GO_0042697
- Highest recorded phase
- 4
- Condition identifier
- HP_0031217
- Condition identifier
- HP_0031217
- Highest recorded phase
- 4
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
- Warning
- Black Box Warning
- Effect
- hepatotoxicity
- Warning
- Black Box Warning
- Effect
- immune system toxicity
- Warning
- Black Box Warning
- Effect
- teratogenicity
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- hepatotoxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- immune system toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- teratogenicity
- Country
- United States
- Event
- alanine aminotransferase abnormal
- Reports
- 3
- Reporting signal score
- 7.5477
- Event
- alanine aminotransferase increased
- Reports
- 113
- Reporting signal score
- 289.781
- Event
- anal rash
- Reports
- 1
- Reporting signal score
- 6.31154
- Event
- aspartate aminotransferase abnormal
- Reports
- 3
- Reporting signal score
- 8.76914
- Event
- aspartate aminotransferase increased
- Reports
- 76
- Reporting signal score
- 172.039
- Event
- asthenia
- Reports
- 2
- Reporting signal score
- 6.55492
- Event
- blood alkaline phosphatase increased
- Reports
- 19
- Reporting signal score
- 31.8585
- Event
- blood bilirubin increased
- Reports
- 12
- Reporting signal score
- 15.2033
- Event
- brain fog
- Reports
- 4
- Reporting signal score
- 18.3912
- Event
- chromaturia
- Reports
- 6
- Reporting signal score
- 7.25449
- Event
- drug effective for unapproved indication
- Reports
- 5
- Reporting signal score
- 11.3552
- Event
- dyspnoea
- Reports
- 1
- Reporting signal score
- 15.6258
- Event
- faeces pale
- Reports
- 3
- Reporting signal score
- 7.87333
- Event
- gamma-glutamyltransferase increased
- Reports
- 29
- Reporting signal score
- 61.0007
- Event
- glomerular filtration rate decreased
- Reports
- 5
- Reporting signal score
- 7.12937
- Event
- hepatic enzyme abnormal
- Reports
- 4
- Reporting signal score
- 7.98108
- Event
- hepatic enzyme increased
- Reports
- 92
- Reporting signal score
- 242.308
- Event
- hot flush
- Reports
- 17
- Reporting signal score
- 23.4666
- Event
- insomnia
- Reports
- 20
- Reporting signal score
- 8.04927
- Event
- liver function test increased
- Reports
- 41
- Reporting signal score
- 113.336
- Event
- loss of therapeutic response
- Reports
- 2
- Reporting signal score
- 6.20604
- Event
- nightmare
- Reports
- 8
- Reporting signal score
- 9.10332
- Event
- pain
- Reports
- 2
- Reporting signal score
- 9.51294
- Event
- product prescribing issue
- Reports
- 4
- Reporting signal score
- 9.53736
- Event
- symptom recurrence
- Reports
- 3
- Reporting signal score
- 9.27741
And 2 more, listed on the interactive page.
- NCT04003142
- NCT04003155
- NCT04003389
- NCT04234204
- NCT04451226
- NCT05034042
- NCT05419908
- NCT06206408
- NCT06206421
- NCT06440967
- NCT04476849
- NCT04482270
- Dose
- 45 mg
- Route
- Oral
- How often
- Once daily
- Administer at about the same time each day
- Do not cut, crush, or chew tablets
- Swallow whole
- Take with liquids
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 0
- Polar surface area
- 76.8
- Calculated partition coefficient (ALogP)
- 2.46
- Calculated partition coefficient (XLogP)
- 1.6
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 2
- Heavy atoms
- 25
- Molecular formula
- C16H15FN6OS
- Monoisotopic mass
- 358.10120846
- Natural product
- No
- 0469-2460
- 0469-2660
- 0469-2760
- Recorded assays
- 101
- Active assays
- 23
Active assay types
- Confirmatory
These details could not be displayed.
Related records
Trials (31)
- A Dose-ranging Study of the Efficacy of ESN364 in Postmenopausal Women Suffering Vasomotor Symptoms (Hot Flashes)
- A Study Following Women in Menopause Treated With a Non-hormonal Therapy for Hot Flashes and Night Sweats
- A Study in Canada to Follow Outcomes of Women in Menopause Treated With Fezolinetant for Hot Flashes, When Given in Clinical Practice
- A Study in Germany to Learn About the Value of Fezolinetant in Treating Hot Flashes and Night Sweats in Women During Menopause
- A Study of Fezolinetant to Treat Hot Flashes in Women Going Through Menopause
- A Study to Assess Bioequivalence of Fezolinetant Formulations in Healthy Female Participants
- A Study to Assess Long-term Safety of Fezolinetant Given to Japanese Women Going Through Menopause
- A Study to Assess the Effect of Food With Fezolinetant in Healthy Female Participants
- A Study to Assess the Safety and Tolerability of Fezolinetant in Women Seeking Treatment for Relief of Vasomotor Symptoms (VMS) Associated With Menopause
- A Study to Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ESN364 in Healthy Japanese Male and Pre- and Post-menopausal Female Subjects
- A Study to Confirm if Fezolinetant Helps Reduce Hot Flashes in Chinese Women Going Through Menopause
- A Study to Confirm if Fezolinetant Helps Reduce Hot Flashes in Japanese Women Going Through Menopause
- A Study to Confirm if Fezolinetant Helps Reduce Hot Flashes in Women With Breast Cancer Who Are Having Hormone Therapy
- A Study to Confirm if Fezolinetant Helps to Reduce Hot Flashes in Indian Women Going Through Menopause
- A Study to Evaluate the Pharmacokinetics and Safety of Fezolinetant in Healthy Chinese Female Subjects
- A Study to Find Out How Safe Long-term Treatment With Fezolinetant is in Women With Hot Flashes Going Through Menopause
- A Study to Find Out if Fezolinetant Helps Reduce Moderate to Severe Hot Flashes in Women Going Through Menopause
- A Study to Find Out if Fezolinetant Helps Reduce Moderate to Severe Hot Flashes in Women Going Through Menopause - 2
- A Study to Find Out if Fezolinetant Helps Reduce Moderate to Severe Hot Flashes in Women in Asia Going Through Menopause
- A Study to Find the Best Dose of Fezolinetant to Treat Hot Flashes in Women Going Through Menopause
In development for (2)
- Kidney disorder Phase 1
- Liver disorder Phase 1
Targets (1)
- TACR3 Neurokinin 3 receptor antagonist