Table 1.
Selected candidate drugs for treatment of hepatic injury and fibrosis.
| Molecular Target | Compound | Effect |
|---|---|---|
| Apoptosis signal-regulating kinase 1 (ASK1) | Selonsertib (GS-4997) | oral bioavailable inhibitor of ASK1, thereby preventing the production of inflammatory and fibrotic acting cytokines |
| Hepatic metabolism | Obeticholic acid | synthetically modified bile acid and potent agonist of the farnesoid X nuclear receptor (FXR) |
| Elafibranor | Orally administered drug acting on the 3 sub-types of PPAR (PPARα, PPARγ, PPARδ) | |
| Tropifexor | Investigational drug which acts as an agonist of the farnesoid X nuclear receptor (FXR) | |
| Cilofexor (GS-9674) | agonist of the farnesoid X nuclear receptor (FXR) which improves cholestasis and liver injury | |
| AKN-083 | farnesoid X receptor (FXR) agonist | |
| INT-767 | a dual agonist targeting the farnesoid X receptor (FXR) and the G protein-coupled bile acid receptor 1 (GPBAR1) | |
| Aramchol | An orally active fatty acid bile acid conjugate that inhibits stearoyl coenzyme A desaturase 1 (SCD1) | |
| Saroglitazar | Agonist of PPARα (and PPARγ) | |
| Lanifibranor | Orally administered drug acting on the 3 sub-types of PPAR (PPARα, PPARγ, PPARδ) | |
| Firsocostat (GS-0976) | Liver-targeted acetyl-CoA carboxylase (ACC) inhibitor | |
| PF-05221304 | Liver-targeted acetyl-CoA carboxylase (ACC) inhibitor | |
| Chemokine receptors | Cenicriviroc | blocks the chemokine receptors CC chemokine receptor 2 (CCR2) and CCR5 |
| Caspases | Emricasan | Prevents cells death by inhibition of caspases |
| VX-166 | The drug has anti-apoptotic activity and prevents release of interleukins | |
| Nivocasan (GS-9450) | hepatoprotective activity preventing fibrosis and apoptosis | |
| Fibroblast growth factor 21 (FGF21) | Pegbelfermin (BMS-986036) | PEGylated FGF21 analogue that improves metabolic parameters |
| Fibroblast growth factor 19 (FGF19) | Aldafermin (NGM282) | Synthetic FGF19 analogue preventing hepatic fat accumulation and liver damage |
| Glucagon-like peptide-1 receptor | Liraglutide | GLP-1 receptor agonist triggering insulin synthesis |
| Semaglutide | GLP-1 receptor agonist triggering insulin synthesis |