Elafibranor

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable agonist of peroxisome proliferator-activated receptor (PPAR)-alpha (PPARa) and -delta (PPARd), with bile acids reducing activity. Upon oral administration, elafibranor, and its main active metabolite GFT1007, target, bind to and activate PPARa and PPARd in the liver. This induces the expression of fibroblast growth factor 21 (FGF21) and downregulates CYP7A1, the key enzyme responsible for the synthesis of bile acids from cholesterol. By reducing CYP7A1 expression, bile acid synthesis is reduced. This leads to reduced bile toxicity, and reduced inflammation and scarring associated with primary biliary cholangitis (PBC).

**Synonyms:** - ELAFIBRANOR - GFT 505 - GFT-505 - GFT505 - IQIRVO