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Synopsis

Synopsis

ACTIVE PHARMA INGREDIENTS

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KDMF

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NDC API

NDC API

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VMF

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API

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Chemistry

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Also known as: 923978-27-2, Gft505, Gft-505, 824932-88-9, Elafibranor [inn], Elafibranor [usan]
Molecular Formula
C22H24O4S
Molecular Weight
384.5  g/mol
InChI Key
AFLFKFHDSCQHOL-IZZDOVSWSA-N
FDA UNII
2J3H5C81A5

Elafibranor
Elafibranor (code name GFT505) is a multimodal and pluripotent medication for treatment of atherogenic dyslipidemia for an overweight patient with or without diabetes. It is an oral treatment that acts on the 3 sub-types of PPAR (PPARa, PPARg, PPARd) with a preferential action on PPARa. As of February 2016, elafibranor has completed 8 clinical trials and a phase III is in progress.
1 2D Structure

Elafibranor

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-[2,6-dimethyl-4-[(E)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy]-2-methylpropanoic acid
2.1.2 InChI
InChI=1S/C22H24O4S/c1-14-12-16(13-15(2)20(14)26-22(3,4)21(24)25)6-11-19(23)17-7-9-18(27-5)10-8-17/h6-13H,1-5H3,(H,24,25)/b11-6+
2.1.3 InChI Key
AFLFKFHDSCQHOL-IZZDOVSWSA-N
2.1.4 Canonical SMILES
CC1=CC(=CC(=C1OC(C)(C)C(=O)O)C)C=CC(=O)C2=CC=C(C=C2)SC
2.1.5 Isomeric SMILES
CC1=CC(=CC(=C1OC(C)(C)C(=O)O)C)/C=C/C(=O)C2=CC=C(C=C2)SC
2.2 Other Identifiers
2.2.1 UNII
2J3H5C81A5
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxo-1-propenyl)phenoxyl)-2-methylpropanoic Acid

2. Gft505

2.3.2 Depositor-Supplied Synonyms

1. 923978-27-2

2. Gft505

3. Gft-505

4. 824932-88-9

5. Elafibranor [inn]

6. Elafibranor [usan]

7. Gft 505

8. Elafibranor(gft505)

9. 2-[2,6-dimethyl-4-[(e)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy]-2-methylpropanoic Acid

10. 2j3h5c81a5

11. Elafibranor (usan)

12. (e)-2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-en-1-yl)phenoxy)-2-methylpropanoic Acid

13. 2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-en-1-yl)phenoxy)-2-methylpropanoic Acid

14. 2-{2,6-dimethyl-4-[(1e)-3-[4-(methylsulfanyl)phenyl]-3-oxoprop-1-en-1-yl]phenoxy}-2-methylpropanoic Acid

15. Propanoic Acid, 2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxo-1-propen-1-yl)phenoxy)-2-methyl-

16. Unii-2j3h5c81a5

17. Gft-505;elafibranor

18. Surecn815512

19. Elafibranor [who-dd]

20. Schembl815512

21. Chembl3707395

22. Schembl16552997

23. Gtpl11135

24. Ex-a757

25. Dtxsid601045330

26. Bcp19067

27. Zhb93288

28. Bdbm50502541

29. Mfcd27987940

30. S3720

31. Zinc114643710

32. Ccg-268462

33. Cs-5522

34. Db05187

35. (e)-2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-enyl)phenoxy)-2-methylpropanoic Acid

36. Ac-31455

37. Ac-35189

38. As-57112

39. Be163306

40. Hy-16737

41. D11208

42. A856857

43. J-690356

44. Q15409440

45. 2-(2,6-dimethyl-4-(3-(4-(methylsulfanyl)phenyl)-3-oxoprop- 1-en-1-yl)phenoxy)-2-methylpropanoic Acid

46. 2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-en-1-yl)phenoxy)-2-methylpropanoicacid

47. 2-[2,6-dimethyl-4-[(1e)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methylpropanoic Acid

48. Propanoic Acid, 2-(2,6-dimethyl-4-((1e)-3-(4-(methylthio)phenyl)-3-oxo-1-propen-1-yl)phenoxy)-

49. Propanoic Acid, 2-[2,6-dimethyl-4-[(1e)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methyl-

2.4 Create Date
2006-10-25
3 Chemical and Physical Properties
Molecular Weight 384.5 g/mol
Molecular Formula C22H24O4S
XLogP35.1
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count5
Rotatable Bond Count7
Exact Mass384.13953042 g/mol
Monoisotopic Mass384.13953042 g/mol
Topological Polar Surface Area88.9 Ų
Heavy Atom Count27
Formal Charge0
Complexity537
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count1
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Investigated for use/treatment in atherosclerosis and diabetes mellitus type 2.


Treatment of primary biliary cholangitis


Treatment of non-alcoholic fatty liver disease (NAFLD) including non-alcoholic steatohepatitis (NASH)


5 Pharmacology and Biochemistry
5.1 Mechanism of Action

GFT505 is an oral treatment that acts on the 3 sub-types of PPAR (PPARa, PPARg, PPARd) with a preferential action on PPARa. It has a sophisticated mechanism of action. It is able to differentially recruit cofactors to the nuclear receptor, which subsequently lead to differential regulation of genes and biological effect. Therefore, the ability to identify and profile the activity of selective nuclear receptor modulator (SNuRMs) is a powerful approach to select innovative drug candidates with improved efficacy and diminished side effects. These pluripotent and multimodal molecules have significant positive effects on obesity, insulin-resistance and diabetes, atherosclerosis, inflammation, and the lipid triad (increasing of HDL cholesterol, lowering of triglycerides and LDL cholesterol).


API SUPPLIERS

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HRV Global Life Sciences

India

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Listed Suppliers

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Elafibranor

About the Company : HRV Global is a leading global manufacturer, seller & exporter of a wide range of APIs, advanced intermediates, pellets, food grade chemicals, food additives & food ingredients. It...

HRV Global is a leading global manufacturer, seller & exporter of a wide range of APIs, advanced intermediates, pellets, food grade chemicals, food additives & food ingredients. It offers services such as sourcing, manufacturing & supply, helping partners enter new markets worldwide. Its strong partnerships with major players in the pharma and food additive industries help HRV Global effectively promote projects and products. HRV Global represents over 30 large Indian drugmakers, primarily targeting Europe, the US & the Middle East markets. Headquartered in India, HRV Global has offices in the US, Switzerland, Dubai, Lithuania & Turkey.
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Drugs in Development

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Details:

Iqirvo (elafibranor) is an approved, novel, oral, PPAR alpha/delta agonist, as a treatment for patients with primary biliary cholangitis.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: Iqirvo

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 10, 2024

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01

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Iqirvo (elafibranor) is an approved, novel, oral, PPAR alpha/delta agonist, as a treatment for patients with primary biliary cholangitis.

Brand Name : Iqirvo

Molecule Type : Small molecule

Upfront Cash : Not Applicable

October 10, 2024

blank

Details:

Iqirvo (elafibranor) is an approved, novel, oral, PPAR alpha/delta agonist, as a treatment for patients with primary biliary cholangitis.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: Iqirvo

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 20, 2024

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02

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Iqirvo (elafibranor) is an approved, novel, oral, PPAR alpha/delta agonist, as a treatment for patients with primary biliary cholangitis.

Brand Name : Iqirvo

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 20, 2024

blank

Details:

Iqirvo (elafibranor) is a novel, oral, dual peroxisome activated receptor (PPAR) alpha/delta agonist, recommended for the treatment of patients with primary biliary cholangitis.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: Iqirvo

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable July 26, 2024

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03

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Iqirvo (elafibranor) is a novel, oral, dual peroxisome activated receptor (PPAR) alpha/delta agonist, recommended for the treatment of patients with primary biliary cholangitis.

Brand Name : Iqirvo

Molecule Type : Small molecule

Upfront Cash : Not Applicable

July 26, 2024

blank

Details:

Iqirvo (elafibranor) is a novel, oral, dual peroxisome activated receptor (PPAR) alpha/delta agonist, currently under investigation as a treatment for patients with primary biliary cholangitis.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: Iqirvo

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 10, 2024

blank

04

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Iqirvo (elafibranor) is a novel, oral, dual peroxisome activated receptor (PPAR) alpha/delta agonist, currently under investigation as a treatment for patients with primary biliary cholangitis.

Brand Name : Iqirvo

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 10, 2024

blank

Details:

GFT505 (elafibranor) is a novel, oral, once-daily, dual peroxisome activated receptor (PPAR) alpha/delta agonist, currently under investigation as a treatment for patients with primary biliary cholangitis.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: GFT505

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 07, 2023

blank

05

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : GFT505 (elafibranor) is a novel, oral, once-daily, dual peroxisome activated receptor (PPAR) alpha/delta agonist, currently under investigation as a treatment for patients with primary biliary cholangitis.

Brand Name : GFT505

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 07, 2023

blank

Details:

GFT505 (elafibranor) is a novel, oral, once-daily, dual peroxisome activated receptor (PPAR) alpha/delta (α,δ) agonist, currently under investigation as a treatment for patients with PBC, a rare liver disease.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: GFT505

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Genfit

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 30, 2023

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06

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Ipsen

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : GFT505 (elafibranor) is a novel, oral, once-daily, dual peroxisome activated receptor (PPAR) alpha/delta (α,δ) agonist, currently under investigation as a treatment for patients with PBC, a rare liver disease.

Brand Name : GFT505

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 30, 2023

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Details:

The agreement gives Ipsen exclusive worldwide* license to develop, manufacture and commercialize GENFIT’s GFT505, an investigational treatment elafibranor, for people living with Primary Biliary Cholangitis (PBC).


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: GFT505

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Ipsen

Deal Size: $583.0 million Upfront Cash: $137.7 million

Deal Type: Licensing Agreement December 17, 2021

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07

Genfit

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Genfit

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : The agreement gives Ipsen exclusive worldwide* license to develop, manufacture and commercialize GENFIT’s GFT505, an investigational treatment elafibranor, for people living with Primary Biliary Cholangitis (PBC).

Brand Name : GFT505

Molecule Type : Small molecule

Upfront Cash : $137.7 million

December 17, 2021

blank

Details:

Company presents Elafibranor, dual agonism of peroxisome proliferator-activated alpha/delta receptors found to be efficacious in the treatment of PBC, a rare liver disease.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: GFT505

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 02, 2021

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08

Genfit

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Genfit

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Company presents Elafibranor, dual agonism of peroxisome proliferator-activated alpha/delta receptors found to be efficacious in the treatment of PBC, a rare liver disease.

Brand Name : GFT505

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 02, 2021

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Details:

ELATIVE™ is a randomized, double blind, placebo-controlled, global multicenter Phase 3 study evaluating the efficacy and safety of elafibranor, a dual PPAR alpha and delta agonist, in PBC.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: GFT505

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 24, 2020

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09

Genfit

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Genfit

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : ELATIVE™ is a randomized, double blind, placebo-controlled, global multicenter Phase 3 study evaluating the efficacy and safety of elafibranor, a dual PPAR alpha and delta agonist, in PBC.

Brand Name : GFT505

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 24, 2020

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Details:

Elafibranor did not demonstrate a statistically significant effect on the primary endpoint of NASH resolution without worsening of fibrosis.


Lead Product(s): Elafibranor

Therapeutic Area: Hepatology (Liver, Pancreatic, Gall Bladder) Brand Name: Undisclosed

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 11, 2020

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10

Genfit

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Genfit

France
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Elafibranor did not demonstrate a statistically significant effect on the primary endpoint of NASH resolution without worsening of fibrosis.

Brand Name : Undisclosed

Molecule Type : Small molecule

Upfront Cash : Not Applicable

May 11, 2020

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FDF Dossiers

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Ipsen

France
Medlab Asia & Asia Health
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Ipsen

France
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ELAFIBRANOR

Brand Name : IQIRVO

Dosage Form : TABLET;ORAL

Dosage Strength : 80MG

Packaging :

Approval Date : 2024-06-10

Application Number : 218860

Regulatory Info : RX

Registration Country : USA

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Patents & EXCLUSIVITIES

Check the patents & exclusivity for this product

US Patents

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IPSEN

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ELAFIBRANOR

US Patent Number : 11857523

Drug Substance Claim :

Drug Product Claim :

Application Number : 218860

Patent Use Code : U-3955

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-03-30

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Medlab Asia & Asia Health
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IPSEN

France
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Medlab Asia & Asia Health
Not Confirmed

ELAFIBRANOR

US Patent Number : 11850223

Drug Substance Claim :

Drug Product Claim :

Application Number : 218860

Patent Use Code : U-1854

Delist Requested :

Patent Use Description : TREATMENT OF PRIMARY B...

Patent Expiration Date : 2037-03-30

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03

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Medlab Asia & Asia Health
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IPSEN

France
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Medlab Asia & Asia Health
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ELAFIBRANOR

US Patent Number : 11331292

Drug Substance Claim :

Drug Product Claim :

Application Number : 218860

Patent Use Code : U-1854

Delist Requested :

Patent Use Description : TREATMENT OF PRIMARY B...

Patent Expiration Date : 2037-03-30

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04

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Medlab Asia & Asia Health
Not Confirmed

IPSEN

France
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Medlab Asia & Asia Health
Not Confirmed

ELAFIBRANOR

US Patent Number : 11185519

Drug Substance Claim :

Drug Product Claim :

Application Number : 218860

Patent Use Code : U-3955

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-03-30

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05

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Medlab Asia & Asia Health
Not Confirmed

IPSEN

France
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Medlab Asia & Asia Health
Not Confirmed

ELAFIBRANOR

US Patent Number : 7943661

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 218860

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2024-09-09

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06

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Medlab Asia & Asia Health
Not Confirmed

IPSEN

France
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Medlab Asia & Asia Health
Not Confirmed

ELAFIBRANOR

US Patent Number : 7632870

Drug Substance Claim :

Drug Product Claim : Y

Application Number : 218860

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2024-09-09

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