Table 1.
Pharmacological agents targeting macrophages in alcoholic liver disease, non-alcoholic steatohepatitis, viral hepatitis, or hepatocellular carcinoma.
| Target | Agent | Mechanism of action | Phase | Clinical trial number |
|---|---|---|---|---|
| ALCOHOLIC LIVER DISEASE | ||||
| Gut bacteria | Combined vancomycin and gentamycin and meropenem | Inhibiting macrophage activation by gut bacteria eradication | Ongoing | NCT03157388 |
| NON-ALCOHOLIC STEATOHEPATITIS | ||||
| Galectin 3 | GR-MD-02 | Galectin 3 antagonist on macrophages |
Phase 2 | NCT02462967 |
| CCR2/CCR5 | Cenicriviroc | CCR2/CCR5 antagonist (inhibits monocyte/macrophage infiltration) |
Phase 2 | NCT02217475 |
| PPARα/δ | Elafibranor | Dual PPARα/δ agonist, PPARδ agonist promotes anti-inflammatory differentiation | Phase 3 | NCT02704403 |
| VIRAL HEPATITIS | ||||
| GM-CSF | Entecavir plus GM-CSF | GM-CSF promotes macrophage differentiation | Ongoing | NCT03164889 |
| GM-CSF | Y peginterferon alpha-2b plus GM-CSF | GM-CSF promotes macrophage differentiation | Phase 2 | NCT02332473 |
| HEPATOCELLULAR CARCINOMA | ||||
| CSF1R | Chiauranib | Multi-target inhibitor that suppresses angiogenesis-related kinases, mitosis-related kinase Aurora B, and CSF1R. Blockade of CSF1R decreases the macrophage differentiation. | Phase 1 | NCT03245190 |
| CCR2/5 | Nivolumab plus CCR2/5 inhibitor | CCR2/CCR5 antagonist (inhibits monocyte/macrophage infiltration) |
Phase 2 | NCT04123379 |
CCR2, CC chemokine receptor 2, CSF1R, colony-stimulating factor 1 receptor, GM-CSF, granulocyte-macrophage colony-stimulating factor.