Table 1.
Summary of Main HDACi Drugs and Agents in Clinical Trials.
| Class | Compound | HDAC target | Phase | Company | Condition tested in Clinical Trials |
|---|---|---|---|---|---|
| Hydroxamic acid | Zolinza, vorinostat (SAHA) | Classes I and II | FDA | Merck | Approved for CTCL, phase I/ II for gastric cancer, NSCLC, thyroid cancer and advanced cancers |
| Panobinostat (LBH589) | Classes I and II | III | Novartis | Phase III trial for CTCL and phase II for CML, MM, NHL, HL, BC, chordoma, prostate and others advanced solid tumors | |
| Belinostat (PXD101) | Classes I and II | II | TopoTarget | Relapsed ovarian cancer, TCL, thymoma, thymic carcinoma, MM, NSCLC, brain tumors | |
| Givinostat or Gavinostat (ITF2357) | Classes I and II | II | Italfarmaco | Relapsed leukemias and MM | |
| Trichostatin (TSA) | Classes I and II | N/A | N/A | N/A | |
| Abexinostat (PCI-24781) | Classes I and II | II | Pharmacyclics | BCL, sarcoma | |
| LAQ-824 | Classes I and II | I | Novartis | Solid and hematologic malignancies | |
| Pracinostat (SB939) | Classes I, II and SIRT 1 | II | MEI Pharma | Prostate cancer, solid tumors, hematologic malignancies | |
| JNJ-26481585 | HDAC1, HDAC6 | I | Johnson & Johnson | Leukemia, CTCL and solid tumors | |
| CUDC-101 | Classes I and II | I | Curis | Head and neck, gastric, BC, liver cancer, MM, NSCLC | |
| CHR-3996 | Class I | I | Chroma Therapeutics | Solid tumors | |
| CHR-2845 | Class I | I | Chroma Therapeutics | Hematological diseases or lymphoid malignancies | |
| Quisinostat (JNJ 26481585) | Class I | II | MedKoo bioscience | CTCL, MM | |
| CG200745 | Pan-HDAC | I | CrystalGenomics, Inc, | Solid tumors | |
| Rocilinostat (ACY-1215) | HDAC6 | I and II | MedKoo bioscience | MM | |
| Benzamides | Entinostat (MS-275 SNDX275) | HDAC1,HDAC2,HDAC3 | II | Schering | HL, lung cancer, ALL, BC, melanoma and advanced solid tumors |
| Mocetinostat (MGCD0103) | HDAC1 and HDAC2 | II | Methylgene | AML | |
| Tacedinaline (CI-994) | HDAC1 and HDAC2 | II and III | Parke-Davis Pharmaceutical | MM, pancreatic cancer, phase III for Lung Cancer | |
| AR-42 | Pan-HDAC | I | Arno Therapeutics | MM, CLL or lymphoma | |
| 4SC-202 | HDAC1, HDAC2, HDAC3 | I | MedKoo bioscience | Hematological malignancies | |
| Resminostat (4SC-201) | Classes I and II | I and II | MedKoo bioscience | Hepatocellular carcinoma, colorectal cancer and HL | |
| Cyclic Peptides | Romidepsin/Istodax (FK228 and FR901228) | HDAC1 and HDAC2 | FDA | Celgene | Aproved for CTCL |
| Aliphatic Acids | Valproic Acid | Classes I and IIa | II and III | Abbot | Phase III trials for cervical cancer, ovarian cancer and phase II for sarcomas, BC, malignant melanoma, AML, brain tumors and advanced cancers |
| Phenylbutyrate (PB) | Classes I and IIa | I and II | Targon Corporation | Colorectal cancer, malignant gliomas, solid tumors, leukemias, lymphomas | |
| Butyrate | Classes I and IIa | I, II and III | Lymphoproliferative disorders, prostate cancer or other solid tumors, phase III for ovarian cancer |
ALL: acute lymphoblastic leukemia; AML: Acute Myeloid leukemia; BC: Breast Cancer; BCL: B-Cell Lymphoma; CLL: Chronic Lymphocytic Leukemia; CML: Chronic Myeloid Leukemia; CTCL: Cutaneous T Cell Lymphoma; HL: Hodgkin Lymphoma; MM: Multiple Myeloma; N/A: not available; NHL: Non-Hodgkin Lymphoma; NSCLC: Non-Small- Cell Lung Carcinoma; TCLT: T Cell Lymphoma.