Drug intelligence / Profile preview

[61Cu]Cu-DOTAGA-PSMA-I&T

Development stage
Preclinical
Lead developer
Nuclidium
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

[61Cu]Cu-DOTAGA-PSMA-I&T is a radiopharmaceutical diagnostic agent designed for positron emission tomography (PET) imaging of prostate cancer. It consists of the positron-emitting radionuclide copper-61 ($^{61}$Cu) chelated by DOTAGA (1,4,7,10-tetraazacyclododececane,1-(glutaric acid)-4,7,10-triacetic acid) and conjugated to the PSMA-I&T (Imaging & Therapy) ligand. The ligand specifically targets the prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II, which is highly overexpressed in prostate cancer cells. While $^{61}$Cu offers advantageous physical decay properties compared to $^{68}$Ga, such as a longer half-life (3.33 h) and lower positron energy, preclinical studies have shown that the DOTAGA-chelated version of this tracer exhibits poor kinetic stability in vivo compared to its NODAGA-chelated counterpart. This instability leads to suboptimal biodistribution and higher background signal, potentially limiting its clinical utility in favor of more stable chelator-ligand combinations.

Other names
61Cu-DOTAGA-PSMA-I&TCopper-61-DOTAGA-PSMA-I&T
02

Targets

PSMA (Prostate-specific membrane antigen)

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