Table 3.
Small molecules with EZH2-inhibiting activity.
| EZH2 inhibitor | Disease | Fibrosis-related output | Status | Ref./Identifier |
|---|---|---|---|---|
| DzNep | Tumor | Inhibits HSC cell cycle arrest | Drug discovery | 34 |
| GSK126 | Lymphomas, multiple myeloma | Inhibits hepatocyte autophagy and HSC activation | I clinical trial | 154 |
| GSK503 | Tumors | Inhibits TGF-β pathway | Drug discovery | 155 |
| EPZ-6438 | Lymphomas, advanced solid tumors | Induces HSC G2/M arrest and apoptosis | II clinical trial | 156 |
| MC4343 | Tumors | _ | I clinical trial | NCTO3854474 |
| MC4355 | Tumors | _ | II clinical trial | NCTO3213665 |
| CPI-1205 | B-cell lymphoma | _ | II clinical trial | NCT02395601 |
| CPI-360 | Tumors | _ | I clinical trial | NCTO2860286 |
| CPI-169 | Tumors | _ | Pre-clinical | WO2013120104A2 |
| EPZ005687 | Lymphoma, Solid tumors | _ | Pre-clinical | US20130317026A1 |