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Elafibranor

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Elafibranor
Clinical data
Other namesGFT505, SureCN815512
ATC code
Identifiers
  • 2-[2,6 Dimethyl-4-[3-[4-(methylthio)phenyl]-3-oxo-1(E)-propenyl]phenoxyl]-2-methylpropanoic acid[1]
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H24O4S
Molar mass384.49 g·mol−1
3D model (JSmol)
  • 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 (INN,[2] code name GFT505) is an 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).[3][4][5]

Elafibranor is a dual PPARα/δ agonist.[6][7]

Medical uses[edit]

elafibranor is indicated for the treatment of Primary Biliary Cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults who have an inadequate response to UDCA, or as monotherapy in patients unable to tolerate UDCA.[8][9]

Elafibranor and its main active metabolite GFT1007 are peroxisome proliferator-activated receptor (PPAR) agonists, both of which activate PPAR-alpha, PPAR-gamma, and PPAR-delta in vitro.[10]

Adverse effects[edit]

The most common adverse reactions include weight gain, diarrhea, abdominal pain, nausea, vomiting, arthralgia, constipation, muscle injury, fracture, gastroesophageal reflux disease, dry mouth, weight loss, and rash.[10]

History[edit]

In 2019, the FDA granted elafibranor Breakthrough Therapy Designation, based on Phase II data, for treatment of Primary Biliary Cholangitis (PBC) in adults with inadequate response to ursodeoxycholic acid (UDCA).[11] The designation was granted to Genfit.

In June 2024, the US FDA has granted accelerated approval to elafibranor. The approval was based on positive Phase III ELATIVE trial data.[12] The designation was granted to Ipsen.[13]

See also[edit]

References[edit]

  1. ^ Cariou B, Zaïr Y, Staels B, Bruckert E (September 2011). "Effects of the new dual PPAR α/δ agonist GFT505 on lipid and glucose homeostasis in abdominally obese patients with combined dyslipidemia or impaired glucose metabolism". Diabetes Care. 34 (9): 2008–14. doi:10.2337/dc11-0093. PMC 3161281. PMID 21816979.
  2. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 74" (PDF). World Health Organization. p. 10. Archived (PDF) from the original on 10 November 2016. Retrieved 9 November 2016.
  3. ^ "Advanced Compound Status" (Press release). Genfit. Archived from the original on 2013-04-11.
  4. ^ "GFT505 Broadens Its Therapeutic Potential" (PDF) (Press release). Archived (PDF) from the original on 10 July 2021. Retrieved 31 Mar 2013.
  5. ^ Cariou B, Staels B (October 2014). "GFT505 for the treatment of nonalcoholic steatohepatitis and type 2 diabetes". Expert Opinion on Investigational Drugs. 23 (10): 1441–8. doi:10.1517/13543784.2014.954034. PMID 25164277. S2CID 3190253.
  6. ^ US Patent No. 7655641 "96 dpi image of original patent USPTO 7655641" (PDF). Retrieved 31 Mar 2013.[dead link]
  7. ^ Vázquez-Carrera, M. (2012). "GFT-505" (PDF). Drugs of the Future. 37 (8): 555–559. doi:10.1358/dof.2012.037.08.1835977. S2CID 258323049.[permanent dead link]
  8. ^ "Ipsen's Iqirvo® receives U.S. FDA accelerated approval as a first-in-class PPAR treatment for primary biliary cholangitis". IPSEN (Press release). 10 June 2024. Retrieved 11 June 2024.
  9. ^ "Historic Milestone Achieved with U.S. FDA Accelerated Approval of Ipsen's Iqirvo for Primary Biliary Cholangitis". wallstreet-online.de (in German). 2024-06-10. Retrieved 2024-06-11.
  10. ^ a b "Prescribing information for IQIRVO" (PDF). U.S. Food and Drug Administration (FDA) (Press release). 10 June 2024. Retrieved 2024-06-11. Public Domain This article incorporates text from this source, which is in the public domain.
  11. ^ "GENFIT announces FDA Grant of Breakthrough Therapy Designation to Elafibranor for the Treatment of PBC".
  12. ^ Ipsen (2024-05-09). A Double-blind, Randomized, Placebo-Controlled Study and Open-label Long Term Extension to Evaluate the Efficacy and Safety of Elafibranor 80 mg in Patients With Primary Biliary Cholangitis With Inadequate Response or Intolerance to Ursodeoxycholic Acid (Report). clinicaltrials.gov.
  13. ^ "Historic Milestone Achieved with U.S. FDA Accelerated Approval of Ipsen's Iqirvo for Primary Biliary Cholangitis". wallstreet-online.de (in German). 2024-06-10. Retrieved 2024-06-11.

External links[edit]

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