(4) Romidepsin (also known as Istodax®): Romidepsin is a selective inhibitor of
HDAC (histone deacetylase) that was discovered from cultures of
Chromobacterium violaceum. Romidepsin was too approved for valuable
treatment of CTCL (cutaneous T cell lymphoma).
Table 2 The first generation of epi-drugs
Drug name Chemical structure
Target
a
Use
b
Azacytidine
O
N
H 2 N
N
N
O
OH
HO
OH
DNMT1
Approved for the
treatment of
MDS [26] and
relapsed AML
[27]
Decitabine
O
N
H 2 N
N
N
O
OH
OH
DNMT1
Approved for
MDS and for
treatment of
elderly AML
patients [28]
Vorinostat
O
H
N
O
N
H
OH
Class I &
II HDACs
Approved for
CTCL [29].
Phase II trial in
recurrent
glioblastoma and
unresectable
gastric cancer
[30]
Romidepsin
O
N
H
NH
S
S
N
H
NH
O
O
O
O
O
H
H
H
Class I
HDACs
Approved for
CTCL [31] and
relapsed PTCL
[32]
Phase I/II trial in
recurrent
high-grade
glioma [33]
Belinostat
HN
O
OH
S
N
H
O O
pan-HDAC Approved for
relapsed/
refractory PTCL
[34]
a DNMT1 (DNA methyltransferase 1), HDACs (histone deacetylases)
b
MDS (myelodysplastic syndrome), AML (acute myeloid leukemia), CTCL (cutaneous T cell
lymphoma), PTCL (peripheral T cell lymphoma)
252
S. Loharch et al.