Table 2 Overview of current clinical trials evaluating DNMT-inhibitors and HDAC-inhibitors in breast cancer

DNMT inhibitor

Azacitidine

Advanced BC

Entinostat^a

Objective response rate

60

II

R

01349959

Advanced/metastatic BC

Nab-paclitaxel

45

I/II

R

00748553

Decitabine

Advanced/metastatic TNBC

Panobinostat^b (±tamoxifen)

The maximum tolerated dose of decitabine and panobinostat

60

I/II

R

01194908

FdCyd

Solid tumors, including BC

Tetrahydrouridine

To determine the safety of FdCyd

20

I

R

01479348

FdCyd

Solid tumors, including BC

Tetrahydrouridine

To determine PFS and/or response rate of FdCyd plus tetrahydrouridine

185

I

R

00978250

EGCG

Newly diagnosed BC

-

To determine whether EGCG can affect proliferation rate and induce apoptosis

20

II

R

00949923

Newly diagnosed BC

-

To evaluate the effects of EGCG on various biomarkers

32

II

A

00676793

Stage I-III BC

-

To determine the safety and maximum tolerated dose of EGCG

40

I

A

00516243

HDAC inhibitor

Vorinostat

BC

Lapatinib

Clinical benefit rate

47

I/II

R

01118975

Recurrent/metastatic BC

-

To evaluate the safety of vorinostat

49

I/II

A

00416130

Advanced BC

Capecitabine

The maximum tolerated dose, safety, and efficacy of vorinostat plus capecitabine

47

II

U

00719875

Local recurrent/metastatic BC

Paclitaxel/bevacizumab

The maximum tolerated dose, and objective response rate of vorinostat in combination with paclitaxel/bevacizumab

58

I/II

U

00368875

Metastatic BC

Ixabepilone

Dose limiting toxicity

56

I

A

01084057

Hormone-refractory BC

Aromatase inhibitor

Clinical benefit rate

14

II

R

01720602

Locally advanced BC

Paclitaxel/trastuzumab

To determine the recommended phase II dose

54

I/II

U

00574587

Hormone-refractory BC

Aromatase inhibitor

Clinical benefit rate

20

II

R

01153672

Newly diagnosed BC

Nab-paclitaxel/carboplatin

Pathologic complete response rate

74

II

A

00616967

HIV + with solid tumor, including BC

Paclitaxel/carboplatin

Maximum tolerated dose

66

I

R

01249443

Brain metastases, including from BC

Paclitaxel/carboplatin plus radiotherapy

Maximum tolerated dose

24

I

A

00838929

Entinostat

Locally recurrent/metastatic ER + BC, or NSCLC

±Exemestane

Pharmacokinetics of entinostat in fasted and fed subjects

28

I

R

01594398

Newly diagnosed TNBC

Anastrozole

Safety, tolerability and recommended phase II dose (phase I cohort); change in proliferation, ER/PR expression (phase II cohort)

41

I/II

R

01234532

HER2-positive metastatic BC

Lapatinib

Recommended phase II dose (phase I cohort); objective response rate (phase II cohort)

70

I/II

R

01434303

Advanced BC

Azacitidine^a

Objective response rate

60

II

R

01349959

Panobinostat

Metastatic TNBC

Letrozole

Maximum tolerated dose, adverse events (phase I cohort); response rate (phase II cohort)

48

I/II

R

01105312

Advanced/metastatic TNBC

Decitabine^b (±tamoxifen)

The maximum tolerated dose of decitabine and panobinostat

60

I/II

R

01194908

HER2-negative locally recurrent/metastatic BC

-

Objective response rate

118

II

A

00777049

VPA

Newly diagnosed locally advanced/metastatic BC

FEC

Pathologic response rate

55

II

R

01010854

Newly diagnosed BC

-

To determine whether VPA levels correlate with leukocyte and tumor histone acetylation

33

NA

R

01007695

Depsipeptide

Solid or hematologic malignancy, including BC

-

Safety, tolerability, maximum tolerated dose and pharmacokinetics

132

I

R

01638533