Table 3.
Representative inhibitors of EZH2 or LSD1 in lung cancer.
| Compound | Structure | Mechanism and potency | Clinical Trial Number | Ref |
|---|---|---|---|---|
| DZNep |  |
SAH hydrolase inhibitor (Ki = 50 pM) |
N/A | [155, 160] |
| GSK2816126 (GSK126) |  |
SAM-competitive EZH2 inhibitor (IC50 = 9.9 nM) |
NCT02082977 | [165, 172] |
| EPZ6438 (Tazemetostat) |  |
SAM-competitive EZH2 inhibitor (Ki = 2.5 nM) (IC50 = 11 nM) |
NCT01897571 NCT02601950 NCT02601937 |
[167, 172] |
| CPI1205 |  |
SAM-competitive EZH2 inhibitor |
NCT02395601 | [168, 172] |
| GSK-2879552 |  |
FAD-dependent irreversible LSD1 inhibitor (Kiapp = 1.7 μM) |
NCT02034123 | [98, 176] |
| RG6016 (ORY-1001) |  |
FAD-dependent irreversible LSD1 inhibitor (IC50 < 20 nM) |
NCT02913443 | [177] |
N/A: Not available.