Comparison of Different Organometallics Towards Electrophilic Aromatic At-Astatinations of Highly Reactive Tetrazines.

Organometallics can be used as precursors for electrophilic At-statinations. In this report, we compared the potential of aryl trimethylsilanes, -germanes, or -stannanes to be used as precursors to At-label highly reactive tetrazines. Tetrazines can be used for pretargeted radioligand therapies or be applied as synthons to radiolabel rapidly and orthogonally a broad set of precursors such as peptides, mAbs or nanomedicines.

[Ga]Ga-DOTAGA-Glu(FAPi) Shows Enhanced Tumor Uptake and Theranostic Potential in Preclinical PET Imaging.

The use of fibroblast activation protein inhibitors (FAPis) for positron emission tomography (PET) imaging in cancer has garnered significant interest in recent years, yielding promising results in preclinical and clinical settings. FAP is predominantly expressed in pathological conditions such as fibrosis and cancer, making it a compelling target. An optimized approach involves using FAPi homodimers as PET tracers, which enhance tumor uptake and retention, making them more effective candidates for therapy.