Table 1.
Main FXR agonist available and under investigation.
| FXR Agonist Product Name |
Current Trials Status | Notes on Mechanism of Action | Reference/Protocol Registration |
|---|---|---|---|
| Obeticholic acid (Ocaliva®) | FDA/EMA approval for PBC in 2016 | 100 times higher affinity than CDCA | Kowdley KV et al. Hepatology. 2018 [40] |
| Efficacy to NASH (phase3) | Neuschwander-Tetri BA et al. Lancet. 2015 [39] | ||
| Bile Acid Malabsorption (phase2) | Walters JR. Aliment Pharmacol Ther. 2015 [48] | ||
| LMB763 | NAFLD (phase2) | NCT02913105 | |
| LJN452 | NAFLD (phase2) | NCT02855164 | |
| GS9674 | NAFLD (phase2) | NCT02854605 | |
| PSC (phase2) | NCT02943460 | ||
| WAY-362450 | phase1 | NCT00499629. 2007 | |
| PX20606 | phase1 | NCT01998659, NCT01998672 | |
| GW4064 | in mice | ||
| INT-767 | in mice | dual FXR and TGR5 agonist |
Table legend: PBC: primitive biliary cholangiopathies; NASH: non alcoholic steato-hepatitis; NAFLD: non alcoholic fatty liver disease; PSC: primary sclerosing cholangitis; CDCA: chenodeoxycholic acid; TGR5: G protein-coupled bile acid receptor.