Table 1 Epi-drugs currently in clinical trial

DNMT

Azacytidine (Vidaza®)

Monotherapy

MDS, AML

FDA approved

[86]

Polytherapy (cytarabine)

AML

III

[158]

Decitabine (Dacogen®)

Monotherapy

MDS, AML

FDA approved

[87]

Polytherapy (Talacotuzumab)

AML

III

[159]

Disulfiram

Polytherapy (Chelated Zinc)

Melanoma

II

NCT02101008

EGCG

Polytherapy (Green tea)

PC

II

NCT00666562

hydralazine

Polytherapy (magnesium valproate)

Refractory solid tumour

II

[160]

SGI-110

Monotherapy

HCC

II

NCT01752933

Polytherapy (Pemetrexed, Cisplatin, Gefitinib)

NSCLC

II

[161]

6-thioguanine

Polytherapy (Dexamethasone, Cyclophosphamide, Vincristine etc.)

Lymphoma

IV

[162]

4′-thio-2′-deoxycytidine (TdCyd)

Monotherapy

Solid tumour

I (recruiting)

[163]

MG98

Monotherapy

Solid tumour

I

[164]

HDAC

Abexinostat (PCI-24781)

Monotherapy

Lymphoma

I & II

[165]

Polytherapy (Doxorubicin)

Sarcoma, lymphoma

I & II

[166]

CUDC-101

Monotherapy

Solid tumour

I

[167]

Belinostat (Beleodaq /PXD101)

Monotherapy

PTCL; HCC, Burkitt lymphoma, DLBCL, thymic carcinoma, MDS

FDA approved;

[98]

II

[168]

Polytherapy (Paclitaxel, Carboplatin)

Ovarian cancer, fallopian tube cancer, bladder cancer

I & II

NCT00421889

Entinostat (SNDX-275)

Polytherapy (Entinostat, Exemestane, Placebo)

Breast cancer

II

[169]

Givinostat (ITF2357)

Monotherapy

Polycythemia vera

I & II

NCT01901432

HDAC

Mocetinostat (MGCD0103)

Polytherapy (Gemcitabine)

Metastatic leiomyosarcoma

II

NCT02303262

Panobinostat (LBH-589)

Monotherapy

MM; thyroid carcinoma, RCC, breast cancer, AML

FDA approved;

[99]

II

[170]

Polytherapy (Placebo)

Hodgkin’s lymphoma, MM

III

[171]

Pracinostat (SB939)

Monotherapy

MLD

II

[172]

Polytherapy (Ruxolitinib)

MLD

II

NCT02267278

Romidepsin (Depsipeptide/FK228)

Monotherapy

CTCL, PTCL

FDA approved

[101]

Polytherapy (Alisertib, Pralatrexate, Gemcitabine)

Relapsed PTCL

III

NCT01482962

Valproic acid (VPA)

Polytherapy (Azacytidine, All-trans retinoic acid)

MDS, AML

II

[173]

Vorinostat (SAHA)

Monotherapy

CTCL

FDA approved

[97]

Polytherapy (KW-0761)

AML

III

[174]

BET

I-BET762 (GSK525762/molibresib)

Monotherapy

Neoplasms

II (recruiting)

NCT01943851

Polytherapy (Abiraterone, Enzalutamide, Prednisone)

Solid tumour

I (recruiting)

NCT03150056

OTX-015 (MK-8628)

Monotherapy

AML, DLBCL, ALL, MM

I

[175]

TEN-010 (RO6870810)

Monotherapy

Advanced solid tumors

I (recruiting)

NCT01987362

Polytherapy (atezolizumab, daratumumab, venetoclax, rituximab)

Advanced MM

I (recruiting)

NCT03292172

CPI-0610

Polytherapy (Ruxolitinib)

Myelofibrosis, AML, MDS

I & II (recruiting)

NCT02158858

FT-1101

Polytherapy (Azacitidine)

AML, non-Hodgkin lymphoma

I

NCT02543879

BET

ZEN003694

Polytherapy (Talazoparib)

TNBC

II (recruiting)

NCT03901469

BMS-986158

Monotherapy

Lymphoma, brain tumour

I (recruiting)

NCT03936465

Polytherapy (Nivolumab)

Advanced tumour

I & II (recruiting)

NCT02419417

ABBV-075

Polytherapy (Vnenetolaclx)

Solid tumour and hematologic malignancies

I

NCT02391480

GS-5829

Polytherapy (Exemestane, Fulvestrant)

Solid tumour, lymphoma

I

NCT02392611

PLX51107

Polytherapy (Azacitidine, BRD4 inhibitor)

AML, MDS

I (recruiting)

NCT04022785

ncRNA

MesomiR-1 (miR-16)

Monotherapy

NSCLC, malignant pleural mesothelioma

I

[176]

Miravirsen (miR-122)

Monotherapy

Hepatitis C

II

[177]

MRX34 (miR-34)

Monotherapy

Primary liver cancer, SCLC, lymphoma, MM, RCC

I (terminated)

NCT01829971

MRG110 (anti-miR-92)

Polytherapy (Placebo)

Wound healing

I

NCT03603431

MRG201 (miR-29)

Polytherapy (Placebo)

Fibrous scar tissue formation

I

NCT02603224

MRG106 (miR-155)

Polytherapy (Cobomarsen, SAHA)

CTCL, Mycosis fungoides

II (recruiting)

NCT03713320

Patisiran

Monotherapy

Rare polyneuropathy

FDA approved

[136]

Polytherapy (Vutrisiran)

Amyloidosis

III (recruiting)

NCT03759379

RG-012 (anti-miR-21)

Monotherapy

Alport syndrome

I

NCT03373786

TargomiRs (miR-15/17)

Monothearpy

Malignant pleural mesothelioma, NSCLC

I

[176]