Drug intelligence / Profile preview

4-octyl itaconate

Development stage
Preclinical
Modality
Small Molecules
01

Overview

**4-Octyl itaconate** is a cell-permeable, synthetic derivative of the endogenous metabolite itaconate. It acts as a prodrug, delivering active itaconate into cells. Mechanistically, 4-octyl itaconate exerts anti-inflammatory effects primarily by activating the Nrf2 (nuclear factor erythroid 2-related factor 2) pathway through alkylation of KEAP1 (Kelch-like ECH-associated protein 1), leading to upregulation of antioxidant and cytoprotective genes[3][7][10]. Additionally, it inhibits various forms of regulated cell death including ferroptosis and gasdermin B-mediated pyroptosis[3][6]. Recent studies show that it can suppress chemokine production and eosinophil development in airway inflammation models[7], and selectively induce ferroptotic death in drug-resistant retinoblastoma cells in vivo[6]. It also modulates type I interferon responses via inhibition of STING signaling by alkylating specific cysteine residues on STING[10].

Other names
Monooctyl itaconate
02

Targets

KEAP1 (Kelch-like ECH-associated protein 1)

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