Related Experiment Video
Updated: Aug 11, 2026
Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging
Published on: February 3, 2015
Design, Synthesis, and Evaluation of a Novel 99mTc-Labeled Small Molecule Inhibitor (Lapatinib)-Based SPECT Tracer
Zuojie Li1,2, Lina Diao1, Peiwen Han1
1Key Laboratory of Radiopharmaceuticals of the Ministry of Education, College of Chemistry, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), Beijing Normal University, Beijing 100875, P. R. China.
Abstract:
Radiolabeled human epidermal growth factor receptor 2 (HER2) tracers are important tools for the accurate clinical diagnosis and treatment of HER2-positive tumors. The aim of this study was to investigate the potential of small molecule inhibitors (lapatinib) as target groups for novel radiotracers targeting HER2. Twelve stable radiotracers were prepared by chelation with different coligands. The relationships between the linker and the combination of coligands with pharmacodynamics were systematically evaluated. [99mTc]Tc-Lapa-HYNIC-TPPTS exhibits the most favorable pharmacokinetic properties, as it can stably bind to the active pocket of the HER2 protein. Both in vitro and in vivo studies demonstrated its high targeting specificity toward HER2. SPECT images of [99mTc]Tc-Lapa-HYNIC-TPPTS in HER2-positive model mice revealed that it can effectively locate tumors. This study is the first attempt at a 99mTc-labeled small-molecule inhibitor tracer targeting HER2, showing great potential for applications in the diagnosis of HER2-positive cancers.
