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PSMA-1-DOTA
- Development stage
- Unknown
- Lead developer
- Peking University
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
PSMA-1-DOTA is a small-molecule radioligand therapy (RLT) agent designed for the treatment of prostate cancer. It consists of a high-affinity ligand targeting the prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II, conjugated to a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) chelator. This chelator allows for the complexation of therapeutic radionuclides, such as Lutetium-177 (^177Lu) or Actinium-225 (^225Ac). PSMA-1-DOTA was specifically developed to optimize binding characteristics and biodistribution to improve the therapeutic index compared to existing agents like PSMA-617. A key objective of its design is to reduce off-target uptake in the salivary glands, thereby mitigating salivary gland toxicity (xerostomia), which is a common and significant dose-limiting side effect of alpha- and beta-emitting PSMA-targeted therapies.
- Other names
- DOTA-PSMA-1DOTA-PSMA1DOTA-PSMA 1
02
Targets
PSMA (Prostate-specific membrane antigen)
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