Histone deacetylase inhibitors (HDACi) have been demonstrated as an emerging class of
anticancer drugs involved in regulation of gene expression and chromatin remodeling thus indicating
valid targets for different types of cancer therapeutics. The pan-deacetylase inhibitor panobinostat
(Farydac®, LBH589) is developed by Novartis Pharmaceuticals and a newly US FDA approved
drug for the multiple myeloma. It is under clinical investigation for a range of hematological
and solid tumors worldwide in both oral and intravenous formulations. Panobinostat inhibits tumor
cell growth by interacting with acetylation of histones and nonhistone proteins as well as various
apoptotic, autophagy-mediated targets and various tumorigenesis pathways involved in the
development of cancer. The current article summarizes the status of panobinostat in gastrointestinal
cancers. Preclinical and clinical data suggest that panobinostat has potential inhibitory activity in
hepatocellular, pancreatic, colorectal, gastric and gastrointestinal stromal tumors. Clinical evaluations
of panobinostat are currently underway. Herein, we have also reviewed the rationale behind
the combination therapy under the trials and possible future prospective for the treatment of GI tumors.
Keywords: HDAC, HDACi, panobinostat, combination therapy, GI tumors, preclinical and clinical studies.
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