Drug intelligence / Profile preview

doxorubicin + copper(II)

Development stage
Preclinical
Lead developer
Farmitalia
Modality
Hydrogel Systems → Drug Delivery Systems, Small Molecules
Administration
Intratumoral
01

Overview

Doxorubicin + copper(II) is a coordination complex prodrug designed for synergistic multi-modal cancer therapy. In this system, the anthracycline antibiotic doxorubicin is coordinated with copper(II) ions, often encapsulated within a delivery vehicle such as a hydrogel (e.g., oxidized hyaluronic acid/carboxymethyl chitosan) alongside other agents like glucose oxidase. Upon reaching the acidic tumor microenvironment, the complex dissociates, releasing doxorubicin to exert its cytotoxic effects by intercalating into DNA and inhibiting topoisomerase II. Simultaneously, the released copper(II) ions are reduced to copper(I) by intracellular glutathione (GSH). The resulting copper(I) then catalyzes a Fenton-like reaction with endogenous or exogenous hydrogen peroxide to generate highly reactive hydroxyl radicals, a process known as chemodynamic therapy (CDT). This combination aims to overcome drug resistance and reduce systemic toxicity by providing localized, environment-responsive drug release and dual-action cytotoxicity.

Other names
doxorubicin-Cu2+ prodrugDOX-Cu2+doxorubicin-copper(II) complex
02

Targets

TOP2A (DNA topoisomerase II)DNA

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