Background: Epigenetic escape is a major mechanism for cancer progression during treatment with
targeted therapies. While HDAC inhibitors are approved as single agents in hematological
cancers, activity in solid tumors has been limited. This is possibly due to the promiscuous
inhibitory properties of unselective inhibitors, toxicity profiles that limit combination
strategies, and, in some cases, inferior pharmacokinetic profiles. OKI-179 is a novel,
oral pro-drug analog of largazole, a compound in the romidepsin-depsipeptide class
of natural products. OKI-179 potently inhibits HDAC 1,2,3 (IC50 = 1.2, 2.4, 2.0 nM, respectively), with no significant inhibition of Class IIa HDACs.
Here we present the initial data for OKI-179 in a phase I dose-escalation trial (NCT03931681).
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