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[177Lu]Lu-DOTA-PEG7-Tz
- Development stage
- Preclinical
- Lead developer
- Hunter College
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
[177Lu]Lu-DOTA-PEG7-Tz is a radiolabeled tetrazine-bearing radioligand designed for pretargeted radioimmunotherapy (PRIT) or pretargeted radionuclide therapy (TRT). It consists of the beta-emitting radionuclide lutetium-177 (177Lu) chelated by DOTA, which is conjugated via a polyethylene glycol 7 (PEG7) linker to a tetrazine (Tz) moiety. In a pretargeting strategy, a trans-cyclooctene (TCO)-functionalized targeting agent (such as a monoclonal antibody, antibody fragment, or single-domain antibody/sdAb) is administered first and allowed to accumulate in the tumor and clear from healthy tissues. Subsequently, [177Lu]Lu-DOTA-PEG7-Tz is administered, which rapidly and selectively reacts with the TCO-bearing targeting agent in vivo via an inverse electron-demand Diels-Alder (IEDDA) click reaction. This approach allows for high tumor-to-background ratios and reduces off-target radiation doses, particularly to the kidneys and bone marrow, compared to directly labeled radioimmunoconjugates.
- Other names
- 177Lu-DOTA-PEG7-Tz177Lu-Tz-PEG7-DOTA[177Lu]Lu-DOTA-PEG7-Tz
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