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ES-64Cu@LR
- Development stage
- Preclinical
- Lead developer
- Union Hospital
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Positron Emitters → Radiopharmaceuticals, Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
ES-64Cu@LR (also known as ES-64Cu(II)@Liposome-RGD) is an investigational, tumor-targeted theranostic liposomal system developed by researchers at Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, and the University of Wisconsin-Madison. It co-encapsulates the beta+/beta- bifunctional radionuclide copper-64 (64Cu) and the cuproptosis inducer elesclomol (ES). The liposome is functionalized with an RGD peptide to target integrin alpha-V/beta-3 receptors, which are highly expressed on tumor cells and neovasculature. ES-64Cu@LR is designed to achieve three concurrent objectives: positron-emission tomography (PET) imaging of elesclomol biodistribution via 64Cu beta+ emission, local internal radiation therapy via 64Cu beta- emission, and elesclomol-mediated cuproptosis. This dual-action approach produces a synergistic antitumor effect by combining the biological effects of cuproptosis with the physical effects of internal radiotherapy, showing promising preclinical efficacy in glioblastoma models.
- Other names
- ES-64Cu(II)@Liposome-RGDES-Cu@LR
02
Targets
αVβ3 (Integrin αVβ3)
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