Drug intelligence / Profile preview

OKI-5

Development stage
Preclinical
Lead developer
OnKure Therapeutics
Modality
Small Molecules
01

Overview

OKI-5 is a potent and selective Class I histone deacetylase (HDAC) inhibitor. It is a synthetic derivative of largazole, a natural macrocyclic depsipeptide known for its high potency against Class I HDACs. OKI-5 is being researched for the treatment of pulmonary hypertension (PH), a condition characterized by pathological vascular remodeling. In preclinical models using precision-cut lung slices (PCLS), OKI-5 has demonstrated the ability to reduce the expression of genes associated with inflammation (CCL2), proliferation (Mki67), and fibrosis (tenascin-C). It is frequently evaluated in combination with bromodomain inhibitors (such as JQ1) to synergistically target epigenetic drivers of PH pathogenesis.

02

Targets

HDAC1 (Histone Deacetylase 1)

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