Table 2.
| Compound | Target | Mechanism of action |
|---|---|---|
| Endothelin antagonist | ET-1 | Inhibits HSC activation and fibrogenesis |
| A receptor antagonist (LU135252) | ||
| Angiotensin system inhibitors | RAS | Blocks profibrogenic effects of angiotensin II |
| Captopril, enalapril, perindopril; losartan, irbesartan, telmisartan | ||
| PPAR-γ | Unknown | |
| Glitazones (pioglitazone, rosiglitazone, troglitazone) | ||
| Anti-TGF-β | TGF-β1 | Inhibits HSC fibrogenesis, apoptosis |
| Anti-integrin αϖβ6 antagonist (EMD405270), TGF-β antisense oligonucleotides, soluble TGF-β decoy receptors | ||
| Gliotoxin | HSC | Induces apoptosis |
| MMP-inducers | Extracellular matrix | Increase MMP fibrolytic activity |
| Halofuginone | ||
| TIMP inhibitor | TIMP-1 | Enhanced MMP activity |
| Neutralizing anti-TIMP-1 antibody | ||
| Sulfasalazine | NF-κβ | Induce HSC apoptosis |
| SiRNA | HSP47 | Induces matrix degradation |
| Immunosuppressants | ||
| Mycophenolate mofetil, rapamycin | Inhibits HSC activation | |
| Angiogenesis inhibitors | ||
| VEGF receptor 1 and 2 antagonists (PTK, sorafenib, vatalanib), anti-integrin αvβ3 (EMD409915) |
Abbreviations: PPAR-γ, peroxisome proliferator-activated receptor-gamma; TGF-β, transforming growth factor beta; HSC, hepatic stellate cell/myofibroblast; MMP, matrix metalloproteinase; TIMP, tissue inhibitor of matrix metalloproteinase; HSP47, heat shock protein 47; VEGF, vascular endothelial growth factor; PTK, protein tyrosine kinase; NF, nuclear factor; ET-1, endothelin-1; RAS, renin-angiotensin system.