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[177Lu]Lu-PEG-Tz
- Development stage
- Preclinical
- Lead developer
- Huazhong University of Science and Technology
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
[177Lu]Lu-PEG-Tz is a Lutetium-177-labeled, polyethylene glycol (PEG)-conjugated tetrazine (Tz) probe designed for pretargeted radionuclide therapy (PRRT). Developed by researchers at Tongji Hospital and Huazhong University of Science and Technology, the radiopharmaceutical is utilized in a pre-targeting strategy for triple-negative breast cancer (TNBC). In this approach, tumor microenvironment-responsive nanoparticles (SiO₂-TCO@CaP) are administered first, accumulating in the tumor and exposing trans-cyclooctene (TCO) groups upon pH-dependent degradation of their calcium phosphate shell. Subsequently administered [177Lu]Lu-PEG-Tz selectively binds to the tumor-localized TCO groups via a rapid, bioorthogonal inverse electron-demand Diels-Alder (iEDDA) click reaction. The localized beta-radiation from Lutetium-177 then induces DNA damage and tumor cell death, offering a highly specific therapeutic effect with minimized systemic toxicity.
- Other names
- 177Lu-PEG-Tz177Lu-PEG-tetrazineLutetium-177 PEG-tetrazineLutetium177 PEG-tetrazineLutetium 177 PEG-tetrazine[177Lu]Lu-PEG-tetrazine
02
Targets
TCO (trans-Cyclooctene)
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