Elafibranor

Elafibranor
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
Molar mass 384.489 g/mol

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 :

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

  1. ↑ Cariou, B.; Zair, Y.; Staels, B.; Bruckert, E. (2011). "Effects of the New Dual PPAR / Agonist GFT505 on Lipid and Glucose Homeostasis in Abdominally Obese Patients with Combined Dyslipidemia or Impaired Glucose Metabolism". Diabetes Care 34 (9): 2008–2014. doi:10.2337/dc11-0093. PMC 3161281. PMID 21816979.
  2. ↑ "Advanced Compound Status" (Press release). Genfit.
  3. ↑ "GFT505 Broadens Its Therapeutic Potential" (PDF) (Press release). Retrieved 31 Mar 2013.
  4. ↑ US Patent No. 7655641 "96 dpi image of original patent USPTO 7655641" (PDF). Retrieved 31 Mar 2013.
  5. ↑ "GFT-505" (PDF). Drugs of the Future 37 (8): 555–559. 2012.
  6. ↑ Cariou, Bertrand; Staels, Bart (2014-10-01). "GFT505 for the treatment of nonalcoholic steatohepatitis and type 2 diabetes". Expert Opinion on Investigational Drugs 23 (10): 1441–1448. doi:10.1517/13543784.2014.954034. ISSN 1744-7658. PMID 25164277.
  7. ↑ Staels, Bart; Rubenstrunk, Anne; Noel, Benoit; Rigou, Géraldine; Delataille, Philippe; Millatt, Lesley J.; Baron, Morgane; Lucas, Anthony; Tailleux, Anne (2013-12-01). "Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis". Hepatology 58 (6): 1941–1952. doi:10.1002/hep.26461. ISSN 1527-3350.
  8. ↑ Cariou, Bertrand; Hanf, Rémy; Lambert-Porcheron, Stéphanie; Zaïr, Yassine; Sauvinet, Valérie; Noël, Benoit; Flet, Laurent; Vidal, Hubert; Staels, Bart (2013-05-28). "Dual Peroxisome Proliferator–Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in Abdominally Obese Subjects". Diabetes Care: DC_122012. doi:10.2337/dc12-2012. ISSN 0149-5992. PMC 3781493. PMID 23715754.
  9. ↑ "Elafibranor, an Agonist of the Peroxisome Proliferator-activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening - Gastroenterology". www.gastrojournal.org. Retrieved 2016-03-08.
  10. ↑ clinical trials involving GFT505
  11. ↑ Quintero, Pablo; Arrese, Marco (2013-12-01). "Nuclear control of inflammation and fibrosis in nonalcoholic steatohepatitis: therapeutic potential of dual peroxisome proliferator-activated receptor alpha/delta agonism". Hepatology (Baltimore, Md.) 58 (6): 1881–1884. doi:10.1002/hep.26582. ISSN 1527-3350. PMID 23787705.
  12. ↑ Hanf, Rémy; Millatt, Lesley J.; Cariou, Bertrand; Noel, Benoit; Rigou, Géraldine; Delataille, Philippe; Daix, Valérie; Hum, Dean W.; Staels, Bart (2014-11-01). "The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects". Diabetes & Vascular Disease Research 11 (6): 440–447. doi:10.1177/1479164114548027. ISSN 1752-8984. PMID 25212694.

External links


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