Related Experiment Video
Updated: Jun 21, 2025

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging
Published on: February 3, 2015
Recent Advances in Pretargeted Strategy for Cancer Theranostics
Yuyang Tian1, Zheng Huang1, Jiewei Luo2
1State Key Laboratory of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Chemistry and Biomedicine Innovation Center (ChemBIC), Nanjing University, Nanjing, 210023, China.
The pretargeted strategy improves cancer theranostics by separately delivering tumor-targeting vectors and radionuclides, optimizing their in vivo behavior for better imaging and therapy.
Area of Science:
- Nuclear Medicine
- Oncology
- Radiochemistry
Background:
- Theranostic probes combine imaging and therapy for cancer, but face challenges with radionuclide and probe accumulation times.
- Discrepancies in probe accumulation and radionuclide half-lives limit current theranostic probe development.
- Long-lived radionuclides can cause suboptimal effects and high toxicity in cancer theranostics.
Purpose of the Study:
- To introduce and discuss the pretargeted strategy for overcoming limitations in cancer theranostics.
- To explore various tumor-targeting vectors used in pretargeted theranostics.
- To review current challenges and future perspectives for clinical applications of pretargeted cancer theranostics.
Main Methods:
- Discusses the principle of the pretargeted strategy in nuclear medicine.
- Reviews different tumor-targeting vectors: antibody-mediated, nanoparticle-mediated, metabolic glycan labeling, and enzyme-triggered in situ self-assembly.
- Analyzes the independent optimization of pharmacokinetics for improved in vivo performance.
Main Results:
- The pretargeted strategy allows separate optimization of vector and radionuclide delivery, improving in vivo pharmacokinetics.
- This approach addresses the limitations of probe accumulation time and radionuclide half-life.
- Enables enhanced nuclear imaging and/or therapeutic effects in tumors.
Conclusions:
- Pretargeted strategy offers a promising solution for developing effective cancer theranostic probes.
- Various targeting vectors show potential for efficient radionuclide delivery and retention in tumors.
- Further research and clinical translation are needed to overcome current challenges in pretargeted cancer theranostics.
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against...
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Tumor Immunotherapy
Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
Cancer Vaccines
Cancer vaccines come in two categories: preventive (prophylactic) and treatment (active). Preventive vaccines, such as the Human Papillomavirus (HPV) vaccine, protect against viruses that cause certain...

