Imaging apoptosis with positron emission tomography: 'bench to bedside' development of the caspase-3/7 specific radiotracer [(18)F]ICMT-11

Eur J Cancer. 2012 Mar;48(4):432-40. doi: 10.1016/j.ejca.2011.11.033. Epub 2012 Jan 5.


The capacity to evade apoptosis has been defined as one of the hallmarks of cancer and, thus, effective anti-cancer therapy often induces apoptosis. A biomarker for imaging apoptosis could assist in monitoring the efficacy of a wide range of current and future therapeutics. Despite the potential, there are limited clinical examples of the use of positron emission tomography for imaging of apoptosis. [(18)F]ICMT-11 is a novel reagent designed to non-invasively image caspase-3 activation and, hence, drug-induced apoptosis. Radiochemistry development of [(18)F]ICMT-11 has been undertaken to improve specific radioactivity, reduce content of stable impurities, reduce synthesis time and enable automation for manufacture of multi-patient dose. Due to the promising mechanistic and safety profile of [(18)F]ICMT-11, the radiotracer is transitioning to clinical development and has been selected as a candidate radiotracer by the QuIC-ConCePT consortium for further evaluation in preclinical models and humans. A successful outcome will allow use of the radiotracer as qualified method for evaluating the pharmaceutical industry's next generation therapeutics.

Publication types

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

MeSH terms

  • Apoptosis* / physiology
  • Azides* / chemistry
  • Azides* / pharmacokinetics
  • Caspase 3 / analysis
  • Caspase 3 / metabolism
  • Caspase 7 / analysis
  • Caspase 7 / metabolism
  • Diagnostic Imaging / methods*
  • Fluorine Radioisotopes* / pharmacokinetics
  • Humans
  • Indoles* / chemistry
  • Indoles* / pharmacokinetics
  • Isatin / analogs & derivatives
  • Isatin / chemistry
  • Models, Biological
  • Neoplasms / diagnostic imaging*
  • Neoplasms / therapy
  • Point-of-Care Systems*
  • Positron-Emission Tomography* / methods
  • Radioactive Tracers
  • Substrate Specificity
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacokinetics
  • Translational Research, Biomedical / methods


  • (18)F-ICMT11
  • Azides
  • Fluorine Radioisotopes
  • Indoles
  • Radioactive Tracers
  • Sulfonamides
  • Isatin
  • CASP3 protein, human
  • CASP7 protein, human
  • Caspase 3
  • Caspase 7