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Drug intelligence / Profile preview
177Lu-D0301
- Development stage
- Preclinical
- Lead developer
- TRIMT
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
177Lu-D0301 (also known as RAD-302 or 177Lu-DOTPI-Tyr2 tetramer) is a peptide-based radiotherapeutic agent targeting αvβ6-integrin, an epithelial-specific integrin highly expressed in various solid tumors, including pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), and head-and-neck squamous cell carcinoma (HNSCC). Developed by Radiopharm Theranostics in collaboration with TRIMT and the Technical University of Munich, the drug consists of a tetrameric formulation of the αvβ6-integrin-targeting cyclic peptide Tyr2 conjugated to the chelator DOTPI and labeled with the beta-emitting radioisotope lutetium-177 (177Lu). Upon binding to αvβ6-integrin on tumor cells, the radiopharmaceutical is internalized, delivering localized, cytotoxic beta radiation that induces DNA damage and cell death. 177Lu-D0301 is currently in preclinical development for the treatment of αvβ6-integrin-expressing carcinomas.
- Other names
- 177Lu-DOTPI(Tyr2)4177Lu-DOTPI-Tyr2177Lu-DOTPI-Tyr2 tetramerlutetium Lu 177 DOTPI-Tyr2 tetramer
02
Targets
αVβ6 (Integrin αVβ6)
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