[68Ga]Ga-R54

[68Ga]Ga-R54 is a radiopharmaceutical consisting of the positron-emitting isotope Gallium-68 complexed with the R54 ligand, a small molecule inhibitor of Fibroblast Activation Protein alpha (FAP). FAP is a cell-surface serine protease that is highly expressed on cancer-associated fibroblasts (CAFs) within the stroma of most epithelial tumors, while being nearly absent in healthy adult tissues. Developed by the IRCCS Istituto Nazionale Tumori Fondazione Pascale, [68Ga]Ga-R54 is utilized as a diagnostic tracer for Positron Emission Tomography (PET) imaging. It is currently in Phase 2 clinical development for the detection, staging, and monitoring of various solid tumors, including breast, lung, colorectal, ovarian, and pancreatic cancers. By targeting the tumor microenvironment rather than the tumor cells themselves, [68Ga]Ga-R54 provides a high tumor-to-background ratio and may offer diagnostic advantages over [18F]FDG, particularly in cancers with low glucose metabolism or in regions with high physiological FDG uptake.

Other names

Gallium-68 R54Gallium68 R54Gallium 68 R5468Ga-labeled FAP inhibitor R54