Table 6.
Drugs and associated epigenetic targets in the context of MNA NB.
| Name | Drug Target in NB | Effect on MYCN in MNA NB | Clinical Status | Citation |
|---|---|---|---|---|
| ARV-825 | BRD4 inhibitor | Downregulation | Pre-clinical | [190] |
| BIX-01294 | EHMT2 (HMT) inhibitor | Downregulation | Pre-clinical | [178] |
| BL1521 | Pan-HDAC inhibitor | Downregulation | Pre-clinical | [166,191] |
| BMS-986158 | BRD4 inhibitor | Not specifically characterized | Pre-clinical and clinical Phase I:
|
[169] |
| Cambinol | SIRT1 (HDAC) inhibitor | Not specifically characterized | Pre-clinical | [72] |
| Decitabine (5-Azacytidine) | DNMT 1 inhibitor | Not specifically characterized | Pre-clinical and clinical Phase I:
|
[184,192] |
| Entinostat (MS-275) | HDAC I inhibitor | Downregulation | Pre-clinical | [167] |
| GSK343, Tazemetostat (EPZ6438), JQEZ5, GSK126 | EZH2 inhibitors | Downregulation (GSK343), others not specifically characterized | Pre-clinical and clinical Phase II (EPZ6439):
|
[35,55,173,175,193] |
| I-BET726 (GSK726) | BRD4 inhibitor | Downregulation | Pre-clinical | [194] |
| JQ1/OTX-015 | BRD4 inhibitor | Downregulation | Pre-clinical | [159] |
| JQAD1 | EP300 (HAT) inhibitor | Downregulation | Pre-clinical | [69] |
| Molibresib (GSK525762, I-BET762) | BRD2/3/4 | Downregulation | Pre-clinical and clinical Phase I:
|
[195] |
| Panobinostat | Pan-HDAC inhibitor | Downregulation | Pre-clinical and clinical Phase II:
|
[159] |
| PCI-48012 | HDAC 8 inhibitor | Downregulation | Pre-clinical | [170] |
| Romidepsin (FK228) | HDAC I inhibitor | Not specifically characterized | Pre-clinical | [171] |
| SGC0946 | DOT1L (HMT) inhibitor | Unknown | Pre-clinical | [76] |
| SGI-1027, Nanaomycin A | DNMT1/3 inhibitors | Not specifically characterized | Pre-clinical | [185] |
| Trichostatin A | HDAC I/II inhibitor | Downregulation | Pre-clinical | [164] |
| Valproic acid (VPA) | HDAC I inhibitor | Downregulation | Pre-clinical and clinical Phase I:
|
[196] |
| Vorinostat (SAHA) | HDAC I inhibitor | Downregulation | Pre-clinical and clinical Phase I:
Phase II:
|
[165] |