Synthesis, preclinical evaluation and radiation dosimetry of a dual targeting PET tracer [⁶⁸Ga]Ga-FAPI-RGD.

ABSTRACT: To enhance tumor uptake and retention, we designed and developed bi-specific heterodimeric radiotracers targeting both FAP and αvβ3, [⁶⁸Ga]Ga-FAPI-RGD. The present study aimed to evaluate the specificity, pharmacokinetics, and dosimetry of [⁶⁸Ga]Ga-FAPI-RGD by preclinical and preliminary clinical studies. Methods: FAPI-RGD was designed and synthesized with the quinoline-based FAPI-02 and the cyclic RGDfK peptide. Preclinical pharmacokinetics were determined in Panc02 xenograft model using microPET and biodistribution experiments. The safety and effective dosimetry of [⁶⁸Ga]Ga-FAPI-RGD was evaluated in 6 cancer patients, and compared with 2-[¹⁸F]FDG imaging. Results: The [⁶⁸Ga]Ga-FAPI-RGD had good stability in saline for a

SUBMITTER: Zang J 

PROVIDER: S-EPMC9576616 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature