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Synopsis

Synopsis

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Chemistry

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Also known as: 1629229-37-3, Esn364, Esn-364, Fezolinetant [usan], 83vne45kxx, A2693
Molecular Formula
C16H15FN6OS
Molecular Weight
358.4  g/mol
InChI Key
PPSNFPASKFYPMN-SECBINFHSA-N
FDA UNII
83VNE45KXX

Fezolinetant
Fezolinetant is under investigation in clinical trial NCT04234204 (A Study to Find Out if Fezolinetant Helps Reduce Moderate to Severe Hot Flashes in Women in Asia Going Through Menopause).
1 2D Structure

Fezolinetant

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(4-fluorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone
2.1.2 InChI
InChI=1S/C16H15FN6OS/c1-9-13-19-20-14(15-18-10(2)21-25-15)23(13)8-7-22(9)16(24)11-3-5-12(17)6-4-11/h3-6,9H,7-8H2,1-2H3/t9-/m1/s1
2.1.3 InChI Key
PPSNFPASKFYPMN-SECBINFHSA-N
2.1.4 Canonical SMILES
CC1C2=NN=C(N2CCN1C(=O)C3=CC=C(C=C3)F)C4=NC(=NS4)C
2.1.5 Isomeric SMILES
C[C@@H]1C2=NN=C(N2CCN1C(=O)C3=CC=C(C=C3)F)C4=NC(=NS4)C
2.2 Other Identifiers
2.2.1 UNII
83VNE45KXX
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Esn364

2.3.2 Depositor-Supplied Synonyms

1. 1629229-37-3

2. Esn364

3. Esn-364

4. Fezolinetant [usan]

5. 83vne45kxx

6. A2693

7. Chembl3608680

8. As3472693-00

9. (4-fluorophenyl)-[(8r)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5h-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone

10. Es-256364

11. A-2693

12. As-3472693-00

13. (r)-(4-fluorophenyl)(8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8h)-yl)methanone

14. Methanone, ((8r)-5,6-dihydro-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-1,2,4-triazolo(4,3-a)pyrazin-7(8h)-yl)(4-fluorophenyl)-

15. Fezolinetant [inn]

16. Unii-83vne45kxx

17. Fezolinetant [who-dd]

18. Schembl16114810

19. Gtpl10422

20. Esn-364esn-364

21. Dtxsid601103615

22. Ex-a6226

23. Bdbm50112244

24. Who 10205

25. Compound 3 [pmid:26191358]

26. Cs-7952

27. Ac-36697

28. Hy-19632

29. D87169

30. Q27269455

31. ((8r)-5,6-dihydro-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-1,2,4-triazolo(4,3-a)pyrazin-7(8h)-yl)(4-fluorophenyl)methanone

32. (4-fluorophenyl)((8r)-5,6-dihydro-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-(1,2,4)triazolo(4,3-a)pyrazin-7(8h)-yl)methanone

33. (4-fluorophenyl)((8r)-8-methyl-3-(3-methyl-1,2,4- Thiadiazol-5-yl)-5,6-dihydro-1,2,4-triazolo(4,3-a)pyrazin- 7(8h)-yl)methanone

2.4 Create Date
2016-02-23
3 Chemical and Physical Properties
Molecular Weight 358.4 g/mol
Molecular Formula C16H15FN6OS
XLogP31.6
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count7
Rotatable Bond Count2
Exact Mass358.10120846 g/mol
Monoisotopic Mass358.10120846 g/mol
Topological Polar Surface Area105 Ų
Heavy Atom Count25
Formal Charge0
Complexity505
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1

API SUPPLIERS

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Moehs Iberica

Spain

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Neuland Laboratories

India

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Virtual BoothNeuland Laboratories- A dedicated 100% API provider.

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Metrochem API Private Limited

India

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Virtual BoothMetrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.

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Dr. Reddy's Laboratories

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Virtual BoothDRL offers a portfolio of products & services, including APIs, CMO services, generics, biosimilars & differentiated formulations.

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Shandong Loncom Pharmaceutical

China

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Virtual BoothShandong Loncom is an R&D-focused manufacturer of Anti-cancer APIs.

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Sichuan Elixir Pharmaceuticals

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Virtual BoothSichuan Elixir Pharmaceutical, a manufacturer of small molecule APIs & a CMO/CDMO service provider for anti-tumor characteristic APIs..

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Hebi Xinhe Pharmaceutical

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Mankind Pharma

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Beijing Sjar Technology Developmen...

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Drugs in Development

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Details:

Veozah (fezolinetant) is a neurokinin 3 (NK3) receptor antagonist being investigated for the treatment of vasomotor symptoms in patients with breast cancer.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: Veozah

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable August 27, 2024

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01

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : Veozah (fezolinetant) is a neurokinin 3 (NK3) receptor antagonist being investigated for the treatment of vasomotor symptoms in patients with breast cancer.

Brand Name : Veozah

Molecule Type : Small molecule

Upfront Cash : Not Applicable

August 27, 2024

blank

Details:

Veozah (fezolinetant) is a neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: Veozah

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 03, 2024

blank

02

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : Veozah (fezolinetant) is a neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.

Brand Name : Veozah

Molecule Type : Small molecule

Upfront Cash : Not Applicable

March 03, 2024

blank

Details:

Veozah (fezolinetant) works by blocking NKB binding on the kisspeptin/neurokinin B/dynorphin neuron to modulate neuronal activity in the hypothalamus to reduce the frequency and severity of moderate to severe VMS due to menopause.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: Veozah

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 10, 2023

blank

03

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : Veozah (fezolinetant) works by blocking NKB binding on the kisspeptin/neurokinin B/dynorphin neuron to modulate neuronal activity in the hypothalamus to reduce the frequency and severity of moderate to severe VMS due to menopause.

Brand Name : Veozah

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 10, 2023

blank

Details:

Veoza (fezolinetant), an investigational oral, nonhormonal medicine in clinical development for the treatment of moderate to severe vasomotor symptoms (VMS) associated with menopause.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: Veozah

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 13, 2023

blank

04

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : Veoza (fezolinetant), an investigational oral, nonhormonal medicine in clinical development for the treatment of moderate to severe vasomotor symptoms (VMS) associated with menopause.

Brand Name : Veozah

Molecule Type : Small molecule

Upfront Cash : Not Applicable

October 13, 2023

blank

Details:

Veozah (fezolinetant) works by blocking NKB binding on the kisspeptin/neurokinin B/dynorphin neuron to modulate neuronal activity in the hypothalamus to reduce the frequency and severity of moderate to severe VMS due to menopause.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: Veozah

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 28, 2023

blank

05

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : Veozah (fezolinetant) works by blocking NKB binding on the kisspeptin/neurokinin B/dynorphin neuron to modulate neuronal activity in the hypothalamus to reduce the frequency and severity of moderate to severe VMS due to menopause.

Brand Name : Veozah

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 28, 2023

blank

Details:

Veozah (fezolinetant) works by blocking NKB binding on the kisspeptin/neurokinin B/dynorphin neuron to modulate neuronal activity in the hypothalamus to reduce the frequency and severity of moderate to severe VMS due to menopause.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: Veozah

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 13, 2023

blank

06

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : Veozah (fezolinetant) works by blocking NKB binding on the kisspeptin/neurokinin B/dynorphin neuron to modulate neuronal activity in the hypothalamus to reduce the frequency and severity of moderate to severe VMS due to menopause.

Brand Name : Veozah

Molecule Type : Small molecule

Upfront Cash : Not Applicable

May 13, 2023

blank

Details:

ESN364 (fezolinetant) works by blocking NKB binding on the kisspeptin/neurokinin B/dynorphin neuron to modulate neuronal activity in the hypothalamus to reduce the frequency and severity of moderate to severe VMS due to menopause.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: ESN364

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable February 20, 2023

blank

07

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : ESN364 (fezolinetant) works by blocking NKB binding on the kisspeptin/neurokinin B/dynorphin neuron to modulate neuronal activity in the hypothalamus to reduce the frequency and severity of moderate to severe VMS due to menopause.

Brand Name : ESN364

Molecule Type : Small molecule

Upfront Cash : Not Applicable

February 20, 2023

blank

Details:

Fezolinetant is an investigational selective NK3 receptor antagonist and is not approved for use anywhere in the world. Safety analyses demonstrated that both endometrial hyperplasia and endometrial malignancy were within pre-specified limits for fezolinetant-treated patients.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: ESN364

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 12, 2022

blank

08

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : Fezolinetant is an investigational selective NK3 receptor antagonist and is not approved for use anywhere in the world. Safety analyses demonstrated that both endometrial hyperplasia and endometrial malignancy were within pre-specified limits for fezolin...

Brand Name : ESN364

Molecule Type : Small molecule

Upfront Cash : Not Applicable

October 12, 2022

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Details:

Results from the SKYLIGHT 1™ and SKYLIGHT 2™ pivotal trials characterize the efficacy and safety of ESN364 (fezolinetant) for the treatment of moderate to severe VMS associated with menopause.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: ESN364

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 30, 2022

blank

09

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : Results from the SKYLIGHT 1™ and SKYLIGHT 2™ pivotal trials characterize the efficacy and safety of ESN364 (fezolinetant) for the treatment of moderate to severe VMS associated with menopause.

Brand Name : ESN364

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 30, 2022

blank

Details:

ESN364 (fezolinetant) is an investigational oral, nonhormonal therapy in clinical development for the treatment of moderate to severe VMS associated with menopause.


Lead Product(s): Fezolinetant

Therapeutic Area: Obstetrics/Gynecology (Women’s Health) Brand Name: ESN364

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 05, 2022

blank

10

Antibody Engineering
Not Confirmed
Antibody Engineering
Not Confirmed

Details : ESN364 (fezolinetant) is an investigational oral, nonhormonal therapy in clinical development for the treatment of moderate to severe VMS associated with menopause.

Brand Name : ESN364

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 05, 2022

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Patents & EXCLUSIVITIES

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US Patents

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01

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ASTELLAS

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FEZOLINETANT

US Patent Number : 9422299

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 216578

Patent Use Code : U-3622

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2034-03-28

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02

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ASTELLAS

Japan
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FEZOLINETANT

US Patent Number : 9987274

Drug Substance Claim :

Drug Product Claim :

Application Number : 216578

Patent Use Code : U-3622

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2034-03-28

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03

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ASTELLAS

Japan
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FEZOLINETANT

US Patent Number : 10836768

Drug Substance Claim :

Drug Product Claim :

Application Number : 216578

Patent Use Code : U-3621

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2034-03-28

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04

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ASTELLAS

Japan
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FEZOLINETANT

US Patent Number : 8871761

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 216578

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2031-04-04

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