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

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Abstract

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. [18F]ICMT-11 is a novel reagent designed to non-invasively image caspase-3 activation and, hence, drug-induced apoptosis. Radiochemistry development of [18F]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 [18F]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. © 2011 Elsevier Ltd. All rights reserved.

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Nguyen, Q. D., Challapalli, A., Smith, G., Fortt, R., & Aboagye, E. O. (2012). Imaging apoptosis with positron emission tomography: “Bench to bedside” development of the caspase-3/7 specific radiotracer [18F]ICMT-11. European Journal of Cancer, 48(4), 432–440. https://doi.org/10.1016/j.ejca.2011.11.033

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