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Table 3 New HDAC inhibitors in clinical trials

From: New clinical developments in histone deacetylase inhibitors for epigenetic therapy of cancer

HDACI Other agents Dose & schedule disease Phase Pts No Outcome Reference
CI-994 capecitabine 4–6 mg/m2 solid tumors I 54 MTD:6 mg/m2 [49, 50]
CI-994 gemcitabine 2–8 mg/m2 po qd solid tumors I 20 MTD:6 mg/m2+
Gem1000 mg/m2
[47]
CI-994 paclitaxel carboplatin 4–6 mg/m2 solid tumors I 30 MTD: 4 mg/m2 [48]
CI-994   8 mg/m2 po qd solid tumors I/II 53 MTD:8 mg/m2 [46]
FK228 gemcitabine 7–12 mg/m2 Pancreatic, Solid tumors I 33 MTD: 12 mg/m2+
Gem 800 mg/m2
[53]
FK228   1–9 mg/m2 thyroid, Solid tumors I 26 MTD: 9 mg/m2 [54]
FK228   18 mg/m2i.v. d1 & d5, q3w MDS, AML II 12 CR: 8%
SD: 50%
[55]
FK228   17.8 mg/m2 d1 & d7, q 3w lung cancer II 19 No response [56]
FK228   14 mg/m2 i.v.d1, 8, 15 q4w T-cell lymphoma II 42 no myocardial
damage
[58]
FK228   13 mg/m2 i.v.d 1, 8, 15, q4w Kidney CA II 29 Insufficient activity
(7% RR)
[57]
ITF2357   150 mg or 100 mgQ12 h 4 d MM II 16 PR: 6% SD: 31% [61]
ITF2357   100 mg PO Hodgkins II 15 SD: 54% [60]
LBH589 Docetaxel
prednisone
15–20 mg po qod CRPC I 16 Oral study closed.
IV form ongoing
[64]
LBH589   20 mg day 1, 3 5 CTCL II 40 RR: 12% [65]
LBH589   4.8–11.5 mg/m2 IV Hematological neoplasms I 15 Study halted due to
QTc prolongation
[63]
MGCD0103 gemcitabine Phase I: 50–110 mg
Phase II: 90 mg
solid tumors I/II 29 MTD: 90 mg [70]
MGCD0103   12.5–56 mg/m2/d solid tumors I 38 MTD: 45 mg/m2 [68]
MGCD0103   20–80 mg/m2 leukemia I 29 MTD: 60 mg/m2 [69]
MGCD0103   85 mg, 110 mg NHL II 50 RR: 23% [71]
MGCD0103   85 mg, 110 mg HL II 33 RR: 38% [72]
MS-275   4–10 mg/m2 leukemia I 38 MTD:8 mg/m2 [75]
MS-275   4–6 mg/m2 Solidtumors, lymphoma I 27 MTD:6 mg/m2 [76]
MS-275   3–7 mg/m2 melanoma II 28 SD: 21–29% [77]
PCI-24781   2.0–2.4 mg/kg solid tumors I 15 MTD: pending [49]
PBA   9–45 g/d solid tumors I 28 MTD:27 g/day [82]
PBA   150–515 mg/kg/d solid tumors I 24 MTD:410 mg/kg [81]
PBA   60 mg -360 mg/kg/d solid tumors I 21 MTD:300 mg/kg [80]
PBA 5-FU 410 mg/kg/d colorectal cancer I 9 MTD: Not reported [83]
PBA azacitidine 200 mg/kg/d AML MDS II 10 RR:50% [84]
PXD101   1000 mg/m2/d ×5 Ovarian ca II 30 SD: 60% [88]
PXD101   600, 900, 1000 mg/m2/day Hematological neoplasms I 16 MTD: 1000 mg/m2/day [87]
PXD101   150–1200 mg/m2/day solid tumors I 46 MTD: 1000 mg/m2/day [86]
VPA   30–120 mg kg(-1) day(-1) IV × 5 solid tumors I 26 MTD: 60 mg/kg/day [93]
VPA ATRA serum level 50–100 mcg/ml AML II 58 RR: 5% (not active) [90]
VPA ATRA 5–10 mg/kg AML I 26 Insufficient activity [91]
VPA   20 – 40 mg/kg/d × 5 Cervical ca I 12 MTD: Not reported [92]
  1. HDAC: histone deacetylase inhibitor; CR: complete responses; PR: partial response; SD: stable disease. MTD: maximal tolerated dose; RR: response rate