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[177Lu]Lu-DOTA-(2P-PEG4)2
- Development stage
- Preclinical
- Lead developer
- Peking University
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
[177Lu]Lu-DOTA-(2P-PEG4)2 is a multivalent radiopharmaceutical developed for the targeted radionuclide therapy of prostate cancer. It consists of a lutetium-177 radioisotope chelated by DOTA, which is conjugated to a multimeric (specifically dimeric) prostate-specific membrane antigen (PSMA) targeting moiety via PEG4 (polyethylene glycol) linkers. The design leverages the multivalent effect to enhance binding affinity to PSMA-expressing cells and utilizes PEGylation to optimize pharmacokinetics by increasing tumor accumulation and accelerating renal clearance. Preclinical studies have demonstrated that this specific configuration provides prolonged tumor retention and high tumor-to-background ratios, making it a promising candidate for theranostic applications in prostate cancer management.
- Other names
- 177Lu-DOTA-(2P-PEG4)2177Lu-labeled PEGylated PSMA dimer
02
Targets
PSMA (Prostate-specific membrane antigen)
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