Radiosynthesis and First Preclinical Evaluation of the Novel ¹¹C-Labeled FAP Inhibitor ¹¹C-FAPI: A Comparative Study of ¹¹C-FAPIs and (⁶⁸Ga) Ga-DOTA-FAPI-04 in a High-FAP-Expression Mouse Model.

ABSTRACT:

Purpose

⁶⁸Ga-labeled fibroblast activation protein inhibitors, such as [⁶⁸Ga]Ga-DOTA-FAPI-04 and [⁶⁸Ga]Ga-DOTA-FAPI-46, have been successfully applied in positron emission tomography imaging of various tumor types. To broaden the PET tracers of different positron nuclides for imaging studies of FAP-dependent diseases, we herein report the radiosynthesis and preclinical evaluation of two ¹¹C-labeled FAP inhibitors, ¹¹C-RJ1101 and ¹¹C-RJ1102.

Methods

Two phenolic hydroxyl precursors based on a quinoline amide core coupled with a 2-cyanopyrrolidine moiety were coupled with [¹¹C]CH₃I to synthesize ¹¹C-RJ1101 and ¹¹C-RJ1102. In vivo small-animal PET and biological

SUBMITTER: Wang C 

PROVIDER: S-EPMC9388731 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature