Table 1.
Histone acetyltransferase inhibitors and histone deacetylase inhibitors.
| Chemical class | Compound | Clinical stage | Cancer specificity | Reference/NCT number |
|---|---|---|---|---|
| HATi | TH1834 | Preclinical | Breast cancer | 172 |
| C646 | Preclinical | Gastric cancer | 164 | |
| HDACi: Cyclic tetrapeptides | FK-228 (Romidepsin) | FDA approved (2009) | Cutaneous/peripheral T cell lymphoma | NCT00106431 |
| HDACi: Hydroxamic acid | SAHA (Vorinostat) | FDA approved (2006) | Cutaneous T cell lymphoma | NCT00918489 |
| PXD-101 (Belinostat) | FDA approved (2014) | Peripheral T cell lymphoma | NCT00413075 | |
| LBH-589 (Panobinostat) | FDA approved (2015) | Multiple myeloma | NCT00739414 | |
| Pyroxamide | Phase I and II | Solid and hematological tumors | NCT00042900 | |
| Resminostat | Phase II | Colorectal, hepatocellular carcinoma, lymphoma | NCT01037478 | |
| Givinostat | Phase II | Lymphoma, Hodgkin lymphoma, myeloma | NCT01761968 | |
| Pracinostat | Phase II | Acute myeloid leukemia | NCT03151304 | |
| CHAPs | Phase II | Hematological tumors | NCT03986970 | |
| TSA | Phase I | Solid tumors | NCT02959905 | |
| CBHA | Preclinical | Solid and hematological tumors | 173 | |
| Oxamflatin | Preclinical | Solid and hematological tumors | 174 | |
| Abexinostat | Phase I | Solid and hematological tumors | NCT03939182 | |
| Quisinostat | Phase I and II | Solid tumor, cutaneous T cell lymphoma | NCT01486277 | |
| MPT0E028 | Phase I | Solid tumor, B-cell lymphoma | NCT02350868 | |
| CHR 3996 | Phase I | Solid tumor | NCT00697879 | |
| CUDC 101 | Phase I | Solid tumor | NCT01171924 | |
| HDACi: Benzamides | Entinostat (MS-275) | Phase I and II | Solid and hematological malignancies | NCT04708470 |
| Chidamide | Phase II and II | Breast cancer; non-small-cell lung cancer | NCT04582955 | |
| Ricolinostat | Phase I and II | Multiple myeloma, lymphoma | NCT02091063 | |
| Tacedinaline | Phase II and III | Lung and pancreatic cancer; myeloma | NCT00005093 | |
| Mocetinostat | Phase I and II | Solid and hematological malignancies | NCT02282358 | |
| HDACi: Short-chain fatty acids | Valproic acid | Phase I and II | Solid and hematological malignancies | NCT01861990 |
| Sodium butyrate | Phase I | Colorectal | NCT05456763 | |
| AR-42 | Phase I | Acute myeloid leukemia | NCT01798901 | |
| Phenylbutyrate | Phase II | Solid and hematological tumors | NCT00005639 | |
| Pivanex | Phase II | Non-small cell lung cancer, myeloma, leukemia | NCT00073385 |
Abbreviations: HATi, histone acetyltransferase inhibitor; HDACi, histone deacetylase inhibitor.