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Table 1 FDA-approved epigenetic therapeutics in malignancies

From: Advances in epigenetic therapeutics with focus on solid tumors

Epigenetic therapeutics

Target

Date of approval

Approved indication

Reference

DNMTi

Azacitidine (Vidaza)

DNMT-1 inhibition

5/2004

MDS

[172,173,174]

Decitabine (Dacogen)

DNMT-1 inhibition

5/2006

MDS

[175]

HDACi

Vorinostat (Zolinza)

Class I and II HDACs

10/2006

Progressive, persistent, or recurrent CTCL disease on or following two systemic therapies

[176, 177]

Romidepsin (Istodax)

Class I HDACs primarily

11/2009

CTCL after at least one prior systemic therapy

[178, 179]

5/2011

PTCL after at least one prior therapy

Belinostat (Beleodaq)

Class I, II and IV HDACs

7/2014

Relapsed or refractory PTCL

[180]

Panobinostat (Farydak)

Class I, II and IV HDACs

2/2015

MM (in combination with bortezomib and dexamethasone) after at least two prior regimens, including bortezomib and an immunomodulatory agent

[181]

IDH mutation inhibitor

Enasidenib (Idhifa)

IDH2 mutant enzyme

8/2017

Relapsed or refractory AML with an IDH2 mutation

[109]

Ivosidenib (Tibsovo)

IDH1 mutant enzyme

7/2018

Relapsed or refractory AML with an IDH1 mutation

[110, 111]

EZH2 inhibitor

Tazemetostat (Tazverik)

EZH2 inhibition

6/2020

Relapsed or refractory (R/R) FL with EZH2 mutation and who have received at least 2 prior systemic therapies, and for adult patients with R/R FL who have no satisfactory alternative treatment options

[113]

1/2020

Metastatic or locally advanced epithelioid sarcoma not eligible for complete resection

[112]

  1. CTCL cutaneous T-Cell lymphoma, DNMT-1 DNA demethyltransferase-1, DNMTi DNA methyltransferase inhibitor, FDA US Food and Drug Administration, FL follicular lymphoma, HDACi histone deacetylase inhibitor, IDH isocitrate dehydrogenase, MDS myelodysplastic syndrome, MM multiple myeloma, PTCL peripheral T-cell lymphoma, CTCL cutaneous T-cell lymphoma