Potential approaches to targeting LSCs based on epigenetic modulators
| Epigenetic target . | Description . | Therapy, if applicable . | Active and recruiting trials . |
|---|---|---|---|
| DOT1L | H3K79 methyltransferase; pathogenic in MLL-rearranged AML63 | Pinometostat | N/A for AML |
| LSD1 | Lysine-specific demethylase64,65 | IMG-7289 | NCT02842827 |
| GSK2879552 | NCT02177812 | ||
| Tranylcypromine | NCT02273102 | ||
| NCT02261779 | |||
| INCB059872 | NCT02712905 | ||
| BET | Bromodomain and extra terminal protien66 | CPI-0610 | NCT02158858 |
| FT-1101 | NCT02543879 | ||
| OTX015 | N/A for AML | ||
| TEN-010 | NCT02308761 | ||
| MK-8628 | NCT02698189 | ||
| BAY1238097 | N/A for AML | ||
| GSK525762 | NCT01943851 | ||
| INCB054329 | NCT02431260 | ||
| INCB057643 | NCT02711137 | ||
| EZH2 | Enhancer of zeste 2 polycomb repressive complex 2 subunit67 | Tazemetostat | N/A for AML |
| CPI-1205 | N/A for AML | ||
| GSK2816126 | N/A for AML | ||
| MAK683 | N/A for AML |
| Epigenetic target . | Description . | Therapy, if applicable . | Active and recruiting trials . |
|---|---|---|---|
| DOT1L | H3K79 methyltransferase; pathogenic in MLL-rearranged AML63 | Pinometostat | N/A for AML |
| LSD1 | Lysine-specific demethylase64,65 | IMG-7289 | NCT02842827 |
| GSK2879552 | NCT02177812 | ||
| Tranylcypromine | NCT02273102 | ||
| NCT02261779 | |||
| INCB059872 | NCT02712905 | ||
| BET | Bromodomain and extra terminal protien66 | CPI-0610 | NCT02158858 |
| FT-1101 | NCT02543879 | ||
| OTX015 | N/A for AML | ||
| TEN-010 | NCT02308761 | ||
| MK-8628 | NCT02698189 | ||
| BAY1238097 | N/A for AML | ||
| GSK525762 | NCT01943851 | ||
| INCB054329 | NCT02431260 | ||
| INCB057643 | NCT02711137 | ||
| EZH2 | Enhancer of zeste 2 polycomb repressive complex 2 subunit67 | Tazemetostat | N/A for AML |
| CPI-1205 | N/A for AML | ||
| GSK2816126 | N/A for AML | ||
| MAK683 | N/A for AML |
N/A, not applicable.