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Updated: Apr 25, 2026

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging
Published on: February 3, 2015
Pretargeted imaging using bioorthogonal chemistry in mice
Raffaella Rossin1, Marc S Robillard1
1Tagworks Pharmaceuticals, High Tech Campus 11, 5656AE Eindhoven, The Netherlands.
In vivo chemistry enables non-invasive molecular imaging and therapy. Pretargeted radioimmuno-imaging and -therapy uses tagged antibodies and radiolabeled probes for tumor targeting in animals and humans.
Area of Science:
- Chemical biology
- Molecular imaging
- Medical therapy
Background:
- In vivo chemistry applications are expanding from chemical biology to non-invasive imaging and therapy.
- Pretargeted radioimmuno-imaging and -therapy involves antibody-based tumor targeting followed by a radiolabeled probe.
- There is growing interest in applying these techniques in living animals and humans.
Purpose of the Study:
- To review the requirements for advancing in vivo chemistry to non-invasive applications in animals.
- To summarize recent achievements in non-invasive molecular imaging and therapy.
- To provide a perspective on future developments in the field.
Main Methods:
- Review of current literature on in vivo chemistry and pretargeted radioimmuno-imaging/-therapy.
- Analysis of requirements for non-invasive applications in animal models.
- Synthesis of recent advancements and future outlook.
Main Results:
- Successful application of in vivo chemistry in chemical biology.
- Growing interest in extending applications to non-invasive molecular imaging and therapy.
- Development of pretargeted radioimmuno-imaging and -therapy strategies.
Conclusions:
- The field is progressing towards non-invasive applications in animals.
- Further research is needed to meet the requirements for clinical translation.
- Future developments hold promise for improved molecular imaging and therapy.
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