Elafibranor is a peroxisome proliferator-activated receptor agonist used to treat primary biliary cholangitis in adults with intolerance of inadequate response to ursodeoxycholic acid. Elafibranor is a dual peroxisome proliferator-activated receptor (PPAR) α and β/δ agonist that works to inhibit bile acid synthesis.
- Mechanism
- Curator reviewed · 8 references
Proliferator-activated receptor (PPAR) is a nuclear receptor that regulates numerical cellular processes, including lipid metabolism and inflammation. Different subtypes of PPARs have different roles and functions, and two of these subtypes - PPAR-alpha (α) and PPAR-delta (δ) (also known as PPARβ) - have been identified as therapeutic targets for diabetes and lipid disorders. PPARα controls lipid flux in the liver and regulates plasma levels of triglycerides and high-density lipoprotein (HDL) cholesterol. PPARδ activation leads to fatty acid transport and oxidation, increased HDL levels, and improved glucose homeostasis. PPARα and PPARδ also mediate anti-inflammatory actions.
While the exact mechanism of action has not been fully elucidated, elafibranor and its active metabolite (GFT1007) are dual α and β/δ agonists. The signalling pathway for PPARδ was reported to include Fibroblast Growth Factor 21 (FGF21)-dependent downregulation of CYP7A1, the key enzyme for the synthesis of bile acids from cholesterol.
- Primary indication
- Elafibranor is indicated for the treatment of primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults who have had an inadequate response to UDCA, or as monotherapy in patients unable to tolerate...Curator reviewed · 2 structured indications
- Formula / weight
- C22H24O4S · 384.49 g/mol (avg)
- First approval
- Canada, 2025 · United States, 2024 · European Union, 2025
- Also known as
- PROPANOIC ACID, 2-(2,6-DIMETHYL-4-((1E)-3-(4-(METHYLTHIO)PHENYL)-3-OXO-1-PROPEN-1-YL)PHENOXY)- · PROPANOIC ACID, 2-(2,6-DIMETHYL-4-(3-(4-(METHYLTHIO)PHENYL)-3-OXO-1-PROPEN-1-YL)PHENOXY)-2-METHYL-
- Code names
- GFT-505 · IPN60190
- Brand names
Resolves to
AFLFKFHDSCQHOL-IZZDOVSWSA-NSMILESCSC1=CC=C(C=C1)C(=O)\C=C\C1=CC(C)=C(OC(C)(C)C(O)=O)C(C)=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Elafibranor, and which of those have an active Phase 3 trial?
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