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 | |
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 | |
Romidepsin (Istodax) | Class I HDACs primarily | 11/2009 | CTCL after at least one prior systemic therapy | |
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 | |
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] |