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Drug intelligence / Profile preview
astatine-211 labeled tetrazine-poly(L)lysine
- Development stage
- Preclinical
- Lead developer
- University of Gothenburg
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptides, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
astatine-211 labeled tetrazine-poly(L)lysine is a preclinical radiopharmaceutical designed for pretargeted alpha therapy (TAT) of disseminated cancer. It consists of a poly(L)lysine (PL) scaffold conjugated with tetrazine (either H-tetrazine or methyltetrazine) and labeled with the alpha-emitting radionuclide astatine-211 ($^{211}\text{At}$). This effector molecule is designed to react via inverse electron-demand Diels-Alder (IEDDA) click chemistry with a pretargeted trans-cyclooctene (TCO)-modified monoclonal antibody bound to tumor antigens. This pretargeting strategy aims to deliver highly localized, cytotoxic alpha radiation to disseminated tumor cells while minimizing systemic toxicity and optimizing pharmacokinetics.
- Other names
- 211At-labeled tetrazine-poly(L)lysineastatine-211 labeled H-tetrazine-poly(L)lysineastatine-211 labeled methyltetrazine-poly(L)lysineastatine-211 tetrazine-poly(L)lysine
02
Targets
TCO (trans-Cyclooctene)
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