[68Ga]Ga-AV01017

[68Ga]Ga-AV01017 is a bispecific radiopharmaceutical imaging agent designed for positron emission tomography (PET) of prostate cancer. Developed by researchers at the BC Cancer Research Institute and the University of British Columbia, the tracer is engineered to target both prostate-specific membrane antigen (PSMA) and fibroblast activation protein (FAP). This dual-targeting approach aims to address the heterogeneous expression of PSMA in prostate cancer lesions, which can limit the sensitivity of monospecific PSMA-targeted imaging. Chemically, [68Ga]Ga-AV01017 consists of a PSMA-targeting pharmacophore and a FAP-targeting quinoline-based pharmacophore connected via a linker and conjugated to a DOTA chelator for labeling with gallium-68 (68Ga). In preclinical studies, [68Ga]Ga-AV01017 demonstrated binding affinity to both PSMA and FAP, though it exhibited lower tumor uptake and prolonged blood retention compared to monospecific counterparts, suggesting a need for further linker optimization.

Other names

Ga-AV01017Ga-AV-01017Ga-AV 01017[68Ga]Ga-AV01017