Table 2.
Epigenetic Inhibitors That Are Approved or in Clinical Development
| Name | Target | Approved/in clinical development∗ | References/identifier number† |
|---|---|---|---|
| Azacitidine and decitabine | DNMT inhibitors | Myelodysplastic syndrome | 105 |
| Vorinostat (Merck) and romidepsin (Celgene) | Pan-HDAC inhibitor | Cutaneous T-cell lymphoma | 106, 107 |
| Ruxolitinib | JAK1/2 inhibitors | Intermediate or high-risk myelofibrosis | 108 |
| Entinostat | Class I HDAC inhibitor | Phase III in breast cancer; phase I and II in Hodgkin lymphoma and kidney cancer∗ | NCT00866333, NCT01038778, NCT01349959 |
| Panobinostat (Novartis) | Pan-HDAC inhibitor | Phase III in Hodgkin lymphoma and multiple myeloma; phase II/III in cutaneous T-cell lymphoma∗ | NCT01034163, NCT01023308, NCT00425555107 |
| CI-994 (CI-994) | Pan-HDAC inhibitor | Phase II completed in advanced myeloma∗; phase III currently in non–small-cell lung cancer∗ | NCT00005624107 |
| Phenelzine sulfate | HDM inhibitor | Phase II in prostate cancer∗ | NCT01253642 |
| Epigallocatechin gallate | DNMT inhibitor | Phase II in multiple myeloma∗ | NCT01589887 |
| EPZ-6438 | EZH2 | Phase I/II clinical trials for solid tumors and hematological malignancies∗ | NCT01897571 |
| EPZ-5676 | DOT1L inhibitor | Phase I in relapsed/refractory adult and pediatric MLL-rearranged leukemias∗ | NCT02141828, NCT01684150 |
| GSK2879552 | LSD1 inhibitor | Phase I for acute myeloid leukemia∗ | NCT02177812 |
| CPI-0610 and OTX015 | BET inhibitors | Phase I in refractory acute leukemias and HM∗ | NCT02158858, NCT01713582 |
DNMT, DNA methyltransferase; HDAC, histone deacetylase; HDM, histone demethylase; HM, hematologic malignancies; JAK, Janus kinase; MLL, mixed-lineage leukemia.
∗
Denotes the inhibitors that are in clinical development.
†
Identifier numbers are for studies found on the Clinical Trials website (https.clinicaltrials.gov).