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Table 1 Characteristics of HDACis in MM (selected)

From: Exploring the role of histone deacetylase and histone deacetylase inhibitors in the context of multiple myeloma: mechanisms, therapeutic implications, and future perspectives

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)

 

III

Class I, IIa

Cervical and ovarian

Sodium butyrate

 

II

Class I, IIa

Colonic cancer

Penyl butyrate

 

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Approved for MM in 2015 (withdrawn in 2022)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)

 

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)

 

I/II

Class I, II, IV

RRMM and solid tumors

ITF2357 (Gavinostat)

 

II

Class I, II

Refractory leukemia and RRMM

PXD101 (Belinostat)

Yes (USA) Approved for PTCL

 

Class I, II, IV

PTCL and RRMM

NVP-LAQ824 (Dacinostat)

 

I

Class I, II

NSCC and colonic cancer

Suberoylanilide bis-hydroxamic acid (SBHA)

  

Class I

Melanoma and sarcoma

RAS2410 (Resminostat)

 

I/II

Class I, II

Hodgkin lymphoma and HCC

ACY-1215 (Rocilinostat)

 

I

HDAC6

RRMM

CR-2408

  

Class I, II, IV

MM

Practinostat

 

II

Class I, II, IV

Prostate cancer

CHR-3996 (Nanatinostat)

 

I

Class I

Refractory metastatic solid tumors

Benzamide

MGCD-0103 (Mocetinostat)

 

II

Class I, IV

Hodgkin lymphoma

SNDX-275 (MS-275, Entinostat)

 

II/III

Class I

Leukemia, colorectal, gastric, pancreatic, lung, ovarian, MM

CI-994 (Tacedinaline)

 

III

Class I

Pancreatic cancer, NSCC, MM, leukemia

4SC-202 (Domatinostat)

 

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

  

Class I

Melanoma and leukemia

Mercaptoketone

KD5170

  

Class I, II

MM

Sirtuins inhibitors

Nicotinamide

 

III

Class III

Laryngeal cancer

Sirtinol

 

Preclinical

SIRT1, II

 

Cambinol

 

Preclinical

SIRT1, II

 

EX-527

 

Preclinical/I/II

SIRT1, II

Huntington disease, glaucoma

Others

Tubacin

  

HDAC6

MM

ACY-241 (Citarinostat)

 

Ib

HDAC6

MM

  1. MM: multiple myeloma, RRMM: relapsed/refractory multiple myeloma, CTCL: cutaneous T-cell lymphoma, PTCL: peripheral T-cell lymphoma, NSCC: non-small cell lung carcinoma, HCC: hepatocellular carcinoma, ATLL: adult T-cell leukemia-lymphoma