Preclinical Assessment of a 68Ga-DOTA-Functionalized Depsipeptide as a Radiodiagnostic Infection Imaging Agent

Molecules. 2017 Aug 24;22(9):1403. doi: 10.3390/molecules22091403.

Abstract

The study assessed a radiolabeled depsipeptide conjugate (68Ga-DOTA-TBIA101) for its potential as an imaging agent targeting infection or infection-associated inflammation. 68Ga-labeled DOTA-TBIA101 imaging was performed in (NZR1) healthy rabbits; (NZR2) rabbits bearing muscular sterile inflammation and Staphylococcus aureus (SA) infection; and (NZR3) rabbits infected with Mycobacterium tuberculosis (MTB) combined with a subcutaneous scruff infection of SA in the same animal. All animals were imaged using a PET/CT scanner at 5 and 60 min post injection. Images showed elevated accumulation of 68Ga-DOTA-TBIA101 in the sterile muscular inflammation site (T/NT ratio = 2.6 ± 0.37 (5 min) and 2.8 ± 2.3 (60 min)) and muscles infected with MTB (T/NT ratio = 2.6 ± 0.35 (5 min) and 2.8 ± 0.16 (60 min)). The findings suggest that 68Ga-DOTA-TBIA101-PET/CT may detect MTB-associated inflammation, although more foundational studies need to be performed to rationalize the diagnostic value of this technique.

Keywords: 68Ga/68Ge generator; DOTA-TBIA101; PET/CT imaging; depsipeptides; infection; inflammation; tuberculosis.

MeSH terms

  • Animals
  • Depsipeptides* / chemistry
  • Depsipeptides* / pharmacology
  • Gallium Radioisotopes* / chemistry
  • Infections / diagnostic imaging*
  • Infections / etiology
  • Infections / pathology
  • Male
  • Molecular Structure
  • Mycobacterium Infections / diagnostic imaging
  • Mycobacterium Infections / microbiology
  • Mycobacterium Infections / pathology
  • Organometallic Compounds* / chemistry
  • Positron Emission Tomography Computed Tomography / methods
  • Rabbits
  • Radiopharmaceuticals*
  • Tissue Distribution

Substances

  • Depsipeptides
  • Gallium Radioisotopes
  • Organometallic Compounds
  • Radiopharmaceuticals