Drug intelligence / Profile preview

artemisinin-copper

Development stage
Preclinical
Lead developer
Anhui Medical University
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intratumoral, Intravenous
01

Overview

Artemisinin-copper (including formulations such as NP@ARTCu and AHCu) is a novel combination nanotherapeutic system designed for cancer therapy. It combines artemisinin or its derivatives (such as artesunate) with copper ions or copper complexes (such as a dinitrogen-diphosphine chelated copper(I) complex) within a single nanoparticle or nanoprodrug delivery system. This combination leverages the synergistic effects of both components: the artemisinin component generates cytotoxic reactive oxygen species (ROS) and induces ferroptosis, while the copper component triggers cuproptosis—a copper-dependent form of programmed cell death characterized by mitochondrial dysfunction and aggregation of lipoylated proteins. Additionally, the copper ions can participate in Fenton-like reactions to further amplify ROS generation in the tumor microenvironment. This dual-action approach has shown promising antitumor efficacy and the ability to stimulate a robust systemic antitumor immune response in preclinical models of prostate cancer and other solid tumors.

Other names
artesunate-coppercopper-artemisinin
02

Targets

DLAT (Dihydrolipoamide S-acetyltransferase)GPX4 (Glutathione peroxidase 4)

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