FAP-targeted
radiopharmaceuticals represent a breakthrough in
cancer imaging and a viable option for therapeutic applications. OncoFAP is an ultra-high-affinity
ligand of FAP with a dissociation constant of 680 pM. OncoFAP has been recently discovered and clinically validated for PET imaging procedures in patients with solid
malignancies. While more and more clinical validation is becoming available, the need for scalable and robust procedures for the preparation of this new class of
radiopharmaceuticals continues to increase. In this article, we present the development of automated radiolabeling procedures for the preparation of OncoFAP-based
radiopharmaceuticals for
cancer imaging and
therapy. A new series of [68Ga]Ga-OncoFAP, [177Lu]Lu-OncoFAP and [18F]AlF-OncoFAP was produced with high radiochemical yields. Chemical and biochemical characterization after radiolabeling confirmed its excellent stability, retention of high affinity for FAP and absence of radiolysis by-products. The in vivo biodistribution of [18F]AlF-
NOTA-OncoFAP, a candidate for PET imaging procedures in patients, was assessed in mice bearing FAP-positive solid
tumors. The product showed rapid accumulation in solid
tumors, with an average of 6.6% ID/g one hour after systemic administration and excellent
tumor-to-healthy organs ratio. We have developed simple, quick, safe and robust synthetic procedures for the preparation of
theranostic OncoFAP-compounds based on
Gallium-68,
Lutetium-177 and
Fluorine-18 using the commercially available FASTlab synthesis module.