Saturday, 24 October 2020 20:45–21:35: POSTER DISCUSSION SESSION: New Therapeutics in Phase I and II studies| Volume 138, SUPPLEMENT 2, S12, October 2020

Initial results from a phase 1 trial of OKI-179, an oral Class 1-selective depsipeptide HDAC inhibitor, in patients with advanced solid tumors

      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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