Table 2.
List of some epigenetic drugs in clinical trials.
| Targets | Drugs/inhibitors | Phase | Types of cancer/tumor |
|---|---|---|---|
| DNA methyltransferase (DNMT) | Guadecitabine (SGI-110) | Phase I | Cholangiocarcinoma, malignant melanoma, non-small cell lung cancer, pancreatic cancer, mesothelioma |
| Phase II | Acute myeloid leukemia, chronic myelomonocytic leukemia, bladder cancer; myeloproliferative disorders, ovarian cancer | ||
| Hydralazine (apresoline) | Phase I | Solid tumors | |
| Phase II | Cutaneous T-cell lymphoma, hepatocellular carcinoma | ||
| MG98 (HYB 101584) | Phase II | Metastatic renal carcinoma | |
| Histone deacetylase (HDAC) | VPA (valproic acid) | Phase II | Glioma, metastatic colorectal cancer |
| Mocetinostat (MGCD-0103) | Phase I | Metastatic leiomyosarcoma, pancreatic cancer, melanoma | |
| Phase II | Solid tumors; | ||
| Resminostat (4SC-201) | Phase I | Biliary cancer; solid tumors, pancreatic cancer | |
| Phase II | Hepatocellular carcinoma, non-small cell lung cancer, Hodgkin lymphoma, biliary cancer | ||
| Non-coding RNA | MRG-106 | Phase I | Cutaneous T-cell lymphoma, diffuse large B-cell lymphoma, adult T-cell leukemia/lymphoma, chronic lymphocytic leukemia |
| MesomiR-1 | Phase I | Malignant pleural mesothelioma, non-small cell lung cancer | |
| CALAA-01 | Phase I | Solid tumors | |
| ATU027 | Phase I | Solid tumors | |
| Phase II | Pancreatic cancer | ||
| Bromodomain and extra-terminal (BET) | Molibresib (I-BET762) | Phase I/II | NUT carcinoma, solid tumors |
| Lysine-specific demethylase (LSD) | Iadademstat (ORY-1001) | Phase I/II | Acute myeloid leukemia |
| GSK2879552 | Phase I | Small cell lung cancer, acute myeloid leukemia | |
| Disruptor of telomeric silencing 1-like (DOT1L) | Pinometostat (EPZ5676) | Phase I/II | Acute myeloid leukemia |