Drug intelligence / Profile preview

levistolide A

Development stage
Preclinical
Lead developer
Jeju National University
Modality
Small Molecules
Administration
Oral
01

Overview

Levistolide A is a natural phthalide derivative isolated from the traditional Chinese medicinal herb *Ligusticum chuanxiong* Hort. It is being investigated for its anti-cancer properties, specifically in the treatment of bladder cancer. The compound's mechanism of action involves the induction of ferroptosis, a form of regulated cell death characterized by iron-dependent lipid peroxidation. Levistolide A achieves this by suppressing the expression of glutathione peroxidase 4 (GPX4) and up-regulating prostaglandin-endoperoxide synthase 2 (PTGS2), which leads to the accumulation of lipid peroxides and the disruption of intracellular iron homeostasis. Preclinical studies in bladder cancer cell lines and xenograft models have demonstrated its efficacy in inhibiting tumor progression, both as a monotherapy and in combination with other ferroptosis inducers like RSL3.

Other names
LA
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)GPX4 (Glutathione peroxidase 4)

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