GFT1007

GFT1007 is the **main active metabolite of elafibranor**, generated through metabolism by the cytosolic enzyme prostaglandin reductase 1 (PTGR1)[1][8]. It is an **agonist of peroxisome proliferator-activated receptors (PPAR)**—specifically PPAR alpha, PPAR delta, and to a lesser extent, PPAR gamma[2][3][7][9]. GFT1007 exhibits higher activity for PPAR alpha compared to PPAR delta and PPAR gamma (with a 3- to 8-fold selectivity for PPAR alpha)[2][3][9]. It is thought to play a key role in modulating bile acid synthesis, detoxification, and output, thus contributing to decreased bile toxicity, reduced inflammation, and protection from cholestatic liver injury[3][9]. GFT1007 does not significantly inhibit most major drug-metabolizing enzymes or transporters in clinically relevant concentrations, though it does inhibit UGT1A6, with unknown clinical relevance[1][3][5].