[⁶⁸Ga]Ga-DOTAGA-Glu(FAPi)₂ Shows Enhanced Tumor Uptake and Theranostic Potential in Preclinical PET Imaging.

ABSTRACT: 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. Here, a UAMC-1110 inhibitor-based homodimer, DOTAGA-Glu(FAPi)₂, was synthesized and radiolabeled with gallium-68, and its efficacy was evaluated in vivo for PET imaging in an endogenously FAP-expressing xenografted mouse model, U87MG. Notably, 45 min post-injection, the mean

SUBMITTER: Mortensen JVK 

PROVIDER: S-EPMC11431137 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature