Emerging chelators for nuclear imaging

Curr Opin Chem Biol. 2021 Aug:63:152-162. doi: 10.1016/j.cbpa.2021.03.001. Epub 2021 May 26.

Abstract

Chelators are necessary in nuclear medicine imaging to direct an inorganic radionuclide, a radiometal, to a desired target; unfortunately, there is no 'one-size-fits-all' chelator. As the toolbox of radiometals is expanding, new chelators are required to prevent off-target side effects. 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is the current gold standard chelator for several radiometals, but typically, chelation requires harsh conditions, making it unsuitable to label biological vectors. The ideal chelator would allow labelling under mild conditions (near-neutral pH and low temperatures [∼37 °C]) and be both thermodynamically and kinetically stable. Over the past 2-3 years, several exciting chelators have been developed that have superior properties to make them worth investigating for future clinical applications.

Keywords: Lutetium-177 radiopharmaceutical; PET; Scandium-44; Zirconium-89.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Chelating Agents / chemistry*
  • Coordination Complexes / chemistry*
  • Coordination Complexes / pharmacokinetics
  • Heterocyclic Compounds, 1-Ring / chemistry
  • Humans
  • Hydrogen-Ion Concentration
  • Kinetics
  • Metals / chemistry*
  • Molecular Structure
  • Positron-Emission Tomography
  • Radioisotopes / chemistry*
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / pharmacokinetics
  • Staining and Labeling
  • Structure-Activity Relationship
  • Temperature
  • Thermodynamics
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Chelating Agents
  • Coordination Complexes
  • Heterocyclic Compounds, 1-Ring
  • Metals
  • Radioisotopes
  • Radiopharmaceuticals
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid