Elafibranor

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Elafibranor
Elafibranor.svg
Systematic (IUPAC) name
2-[2,6 dimethyl-4-[3-[4-(methylthio)phenyl]-3-oxo-1(E)-propenyl]phenoxyl]-2-methylpropanoic acid[1]
Clinical data
Pregnancy
category
  • N/A
Legal status
  • Investigational
Identifiers
CAS Number 923978-27-2
ATC code none
PubChem CID: 9864881
ChemSpider 8040573
Synonyms GFT505, SureCN815512
Chemical data
Formula C22H24O4S
Molecular mass 384.489 g/mol
  • O=C(O)C(Oc1c(cc(cc1C)\C=C\C(=O)c2ccc(SC)cc2)C)(C)C
  • 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+
  • Key:AFLFKFHDSCQHOL-IZZDOVSWSA-N

Elafibranor (GFT505) a experimental medication that is being studied and developed by Genfit for the treatment of cardiometabolic diseases including diabetes, insulin resistance, dyslipidemia, and non-alcoholic fatty liver disease (NAFLD).[2][3]

Elafibranor is a dual PPARα/δ agonist.[4][5]

Elafibranor is mainly focused on the treatment of NASH disease.[6]

Clinical studies

Administered to over 800 patients and healthy volunteers to date, Elafibranor has demonstrated :

  • beneficial properties for NASH :[7]
  • Improvement of insulin sensitivity and glucose homeostasis [8]

Phase 2b (GOLDEN) results were published online in GastroEnterology in February 2016 [9] and will be fully available in the paper version in May 2016.

As of February 2016 GFT505 has completed 8 clinical trials and a phase III is in progress.[10]

Pre-clinical studies

Efficacy on histological NASH parameters (steatosis, inflammation, fibrosis) in animal disease models – anti-fibrotic activities [11]

The absence of safety concern has been confirmed in a full toxicological package up to 2-year carcinogenicity studies and cardiac studies (in mice).[12]

See also

References

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External links


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  2. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ US Patent No. 7655641 Lua error in package.lua at line 80: module 'strict' not found.
  5. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  6. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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  8. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  9. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  10. ↑ clinical trials involving GFT505
  11. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  12. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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