Drug intelligence / Profile preview

89Zr-DFOsq-bisPSMA

Development stage
Preclinical
Lead developer
Telix Pharmaceuticals
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

89Zr-DFOsq-bisPSMA (also known as [89Zr]Zr-DFOSq-bisPhPSMA) is a bivalent, small-molecule positron emission tomography (PET) imaging tracer designed for the diagnostic detection of prostate-specific membrane antigen (PSMA)-expressing prostate cancer. It consists of a bivalent lysine-ureido-glutamate PSMA-targeting motif conjugated to a squaramide ester derivative of desferrioxamine B (DFOSq) chelator, which is radiolabeled with the positron-emitting radionuclide zirconium-89 (89Zr). The bivalent design enhances binding affinity and tumor retention compared to monovalent analogs, while the use of zirconium-89, with its physical half-life of 78.4 hours, allows for delayed PET imaging time points to optimize tumor-to-background contrast. The tracer was developed by the University of Melbourne in collaboration with Telix Pharmaceuticals, Peter MacCallum Cancer Centre, Austin Health, and Cyclotek.

Other names
89Zr-DFOSq-bisPSMA89Zr-DFOSq-bisPhPSMA[89Zr]Zr-DFOSq-bisPSMA[89Zr]Zr-DFOSq-bisPhPSMA[89Zr]ZrDFOSq-bisPhPSMA
02

Targets

PSMA (Prostate-specific membrane antigen)

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