Table 2.
HDAC inhibitors currently under clinical investigations.
| HDACis | Specificity | Cancer Types | Clinical Trial | Reference |
|---|---|---|---|---|
| Hydroxamic acid | ||||
| Vorinostat (SAHA) | Classes I, II and IV | CTCL | FDA Approved in 2006 | (Mann et al. 2007) |
| Belinostat (Beleodaq/PXD101) | Classes I, II and IV | PTCL | FDA approved in 2014 | (McDermott and Jimeno 2014) |
| Panobinostat (LBH-589) | Classes I, II and IV | MM | FDA approved in 2015 | (Richardson et al. 2015) |
| Resminostat (4SC-201) | Classes I and II | Advanced colorectal and hepatocellular carcinoma; HL | Phase II trial | (Brunetto et al. 2013; Zhao and Lawless 2015) |
| Givinostat (ITF2357) | Classes I and II | CLL; MM; HL | Phase II trial | (Galli et al. 2010; Locatelli et al. 2014) |
| Pracinostat (SB939) | Classes I, II and IV | AML | Phase II trial | (Zorzi et al. 2013) |
| Abexinostat (PCI-24781) | Classes I and II | Metastatic solid tumors; HL; non-HL; CLL | Phase I trial | (Choy et al. 2015; Morschhauser et al. 2015) |
| Quisinostat (JNJ-26481585) | Class I and II HDACs | Advanced solid tumor; lymphoma; CTCL | Phase I and II trial | (Venugopal et al. 2013) |
| MPT0E028 | HDAC1, 2, 6 | Advanced solid tumor | Phase I trial | (Zwergel et al. 2015) |
| CHR-3996 | Class I | Solid tumor | Phase I trial | (Banerji et al. 2012) |
| CUDC-101 | Classes I and II HDAC,EGFR, HER2 | Solid tumor | Phase I trial | (Shimizu et al. 2015) |
| CUDC-907 | Classes I and II HDAC, PI3K | MM; lymphoma; solid tumor | Phase I trial | (Qian et al. 2012) |
| Benzamides | ||||
| Entinostat (MS-275) | Class I | Solid and hematological malignancies | Phase I and II trial | (Knipstein and Gore 2011) |
| Mocetinostat (MGCD0103) | Class I and IV | Solid and hematological malignancies | Phase I and II trial | (Younes et al. 2011) |
| Tacedinaline (CI-994) | Class I | MM; lung and pancreatic cancer | Phase II and III trial | (Pauer et al. 2004) |
| Ricolinostat (ACY-1215) | HDAC6 | MM; lymphoma | Phase I and II trial | (Santo et al. 2012) |
| Chidamide (CS055/HBI-8000) | HDAC1, 2, 3, and 10 | Breast cancer; NSCLC | Phase II and III trial | (Dong et al. 2012; Shi et al. 2015) |
| Cyclic peptides | ||||
| Romidepsin (Depsipeptide/FK228) | Class I | CTCL; PTCL | FDA approved in 2009 and 2011 | (Frye et al. 2012) |
| Aliphatic fatty acids | ||||
| Valproic acid (VPA) | Class I and II | Solid and hematological malignancies | Phase I and II trial | (Bilen et al. 2015) |
| Phenylbutyrate | Classes I and II | Solid and hematological malignancies | Phase I and II trial | (Iannitti and Palmieri 2011) |
| AR-42 | Class I and IIb | AML | Phase I trial | (Guzman et al. 2014) |
| Pivanex (AN-9) | Classes I and II | NSCLC; myeloma; CLL | Phase II trial | (Reid et al. 2004) |
AML, acute myeloid leukemia; CLL, chronic lymphocytic leukemia; CTCL, cutaneous T cell lymphoma; HL, Hodgkin’s lymphoma; MM, multiple myeloma; NSCLC, non-small-cell lung cancer; PTCL, peripheral T cell lymphoma.