Chemical class | Drug name | Approved by the FDA | In Phase I/II/III clinical trials | Reported targets (HDAC) | Type of cancer targeted against |
---|---|---|---|---|---|
Short-chain fatty acid | Valproic acid (VPA) | Â | III | Class I, IIa | Cervical and ovarian |
Sodium butyrate | Â | II | Class I, IIa | Colonic cancer | |
Penyl butyrate | Â | II | Class I, IIa | Urea cycle disorders | |
Hydroxamic acid | LBH589 (Panobinostat) | Approved for MM in 2015 (withdrawn in 2022) | III | Class I, II, IV | MM and CTCL |
Trichostain-A (TSA) | Â | Preclinical | Class I, II, IV | Cervical and hepatoma | |
SAHA (Vorinostat) | Yes (USA) Approved for CTCL | I/II | Class I, II, IV | CTCL | |
JNJ-26481585 (Qusinostat) | Â | I/II | Class I, II, IV | RRMM and solid tumors | |
ITF2357 (Gavinostat) | Â | II | Class I, II | Refractory leukemia and RRMM | |
PXD101 (Belinostat) | Yes (USA) Approved for PTCL | Â | Class I, II, IV | PTCL and RRMM | |
NVP-LAQ824 (Dacinostat) | Â | I | Class I, II | NSCC and colonic cancer | |
Suberoylanilide bis-hydroxamic acid (SBHA) | Â | Â | Class I | Melanoma and sarcoma | |
RAS2410 (Resminostat) | Â | I/II | Class I, II | Hodgkin lymphoma and HCC | |
ACY-1215 (Rocilinostat) | Â | I | HDAC6 | RRMM | |
CR-2408 | Â | Â | Class I, II, IV | MM | |
Practinostat | Â | II | Class I, II, IV | Prostate cancer | |
CHR-3996 (Nanatinostat) | Â | I | Class I | Refractory metastatic solid tumors | |
Benzamide | MGCD-0103 (Mocetinostat) | Â | II | Class I, IV | Hodgkin lymphoma |
SNDX-275 (MS-275, Entinostat) | Â | II/III | Class I | Leukemia, colorectal, gastric, pancreatic, lung, ovarian, MM | |
CI-994 (Tacedinaline) | Â | III | Class I | Pancreatic cancer, NSCC, MM, leukemia | |
4SC-202 (Domatinostat) | Â | I | Class I | Advanced hematological malignancies | |
Chidamide (Tucidinostat) | Yes (China) | II | Class I, IIb | Solid tumors, PTCL, MM and ATLL | |
Cyclic peptide | Depsipeptide (FR901228, FK228, Romidepsin) | Yes (USA) Approved for CTCL | II | Class I | CTCL and RRMM |
Apicidin | Â | Â | Class I | Melanoma and leukemia | |
Mercaptoketone | KD5170 | Â | Â | Class I, II | MM |
Sirtuins inhibitors | Nicotinamide | Â | III | Class III | Laryngeal cancer |
Sirtinol | Â | Preclinical | SIRT1, II | Â | |
Cambinol | Â | Preclinical | SIRT1, II | Â | |
EX-527 | Â | Preclinical/I/II | SIRT1, II | Huntington disease, glaucoma | |
Others | Tubacin | Â | Â | HDAC6 | MM |
ACY-241 (Citarinostat) | Â | Ib | HDAC6 | MM |