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Mechanism and clinical trial phase of drugs against EZH2
| Mechanism of action | Name | Specific for EZH2 | Status | Ref |
|---|---|---|---|---|
| SAH hydrolase inhibitors | DZnep | No | Pre-clinical | [92] |
| SAM-competitive inhibitors | Tazemetostat | Yes | Phase II | [93] |
|
GSK126 (GSK2816126) |
Yes | Phase I | [94] | |
| SHR2554 | Yes | Phase I | [76] | |
| Interfering the interaction between EZH2 and EED |
EED226 (MAK683) |
Yes | Phase I | [77] |
| Promoting EZH2 degradation | Sorafenib | No | FDA approval | [79] |
