99mTc-CN7DG: A Highly Expected SPECT Imaging Agent of Cancer with Satisfactory Tumor Uptake and Tumor-to-Nontarget Ratios

Mol Pharm. 2021 Mar 1;18(3):1356-1363. doi: 10.1021/acs.molpharmaceut.0c01177. Epub 2021 Feb 15.

Abstract

A novel glucose derivative (CN7DG) possessing an isonitrile as a coordinating group was synthesized, and 99mTc-CN7DG, which was expected to be a powerful tumor imaging agent for SPECT, was prepared in a kit by the reaction of CN7DG with SnCl2·2H2O and 99mTcO4-. 99mTc-CN7DG exhibited good stability and was transported via glucose transporters. Biodistribution results in mice bearing A549 tumor models showed that 99mTc-CN7DG had a higher uptake at the tumor sites and better tumor/blood and tumor/muscle ratios than did [18F]FDG and 99mTc-CN5DG. SPECT/CT imaging studies showed obvious accumulation in tumor sites, suggesting that 99mTc-CN7DG is a promising candidate for tumor imaging. Because 99mTc and 188Re stand for a "theranostic pair", 188Re-CN7DG is expected to be prepared as a promising agent for tumor therapy.

Keywords: 99mTc; cancer; glucose derivatives; imaging agents; isocyanide ligands.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Animals
  • Biological Transport / physiology
  • Fluorodeoxyglucose F18 / metabolism
  • Humans
  • Mice
  • Neoplasms / diagnostic imaging*
  • Neoplasms / metabolism
  • Organotechnetium Compounds / metabolism*
  • Radiopharmaceuticals / metabolism*
  • Single Photon Emission Computed Tomography Computed Tomography / methods*
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon / methods*

Substances

  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • Fluorodeoxyglucose F18