L-05：Application of PET Imaging to Theranostics

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＜L-05＞：Life Science, Pharmaceutical Sciences sdgs-03 sdgs-09
 

Application of PET Imaging to Theranostics
― From Non-Invasive “Seeing” Cancer to Truly “Diagnosing” It ―

Tsuyoshi Tahara Associate Professor
Division of Bio-imaging, Advanced Research Promotion Center
Keywords PET, cancer imaging, theranostics drug discovery
Laboratory URL http://www.tbis2013.net/
Research Overview
● More Than 50% Lifetime Cancer Risk in Japan: Understanding Cancer Characteristics Is Essential for Overcoming Cancer
In an era in which more than one in two people will develop cancer during their lifetime, not only basic research related to anticancer drug development but also technologies for early detection and for understanding the biological characteristics of cancer are essential. Such technologies contribute to early treatment and enable prediction of therapeutic efficacy, playing a crucial role in overcoming cancer.
Conventional positron emission tomography (PET) (Fig. 1) has primarily focused on “seeing” cancer, while technologies for truly “diagnosing” cancer remain largely undeveloped, representing an urgent challenge. To address this issue, we aim to establish PET imaging technologies that enable cancer diagnosis, not merely visualization.

● Probe Development of Cancer-Type-Specific Antibody and Peptide Therapeutics to Visualize Cancer Characteristics
By converting antibody therapeutics and peptide therapeutics into PET probes, it becomes possible to non-invasively detect cancer while simultaneously characterizing cancer cell properties and predicting therapeutic responses. First, antibodies and peptides are labeled with chelators, followed by coordination of metallic radionuclides such as ^64Cu and ^89Zr to the chelators, successfully achieving positron labeling (Fig. 2). The biodistribution of ^64Cu-labeled antibodies and ^64Cu-labeled peptides is evaluated using cancer PET imaging in tumor-bearing mouse models.
 
Potential Applications and Commercialization Prospects

● Translation to Theranostics Drug DiscoveryThis technology can initially be translated into clinical applications as cancer PET probes. In recent years, next-generation precision medical systems known as theranostics (therapy + diagnostics), which enable both diagnosis and treatment using a single agent, have attracted considerable attention. PET probe development based on antibody and peptide therapeutics represents a true form of theranostics.
Furthermore, in the future, by labeling antibodies or peptides with astatine-211, it will be possible to achieve cancer-specific alpha-particle radiotherapy, further expanding the therapeutic potential of this platform.

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Fig. 1. Theranostics using PET
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Fig. 2. PET probe development of antibodies		 L-05-3.png

Fig. 3. Representative example of antibody-based PET imaging
● Diagram explanation
Principle of PET
 In positron emission tomography (PET), the position of a positron-emitting radionuclide is determined by detecting two annihilation gamma rays emitted in opposite directions (180°) following positron–electron annihilation. The detected signals are then computationally processed to reconstruct an image.		    
Publications ● Tsuyoshi Tahara et. al., Characteristic evaluation of 11C-labeled leucine analog, L-a-[5-11C]MeLeu, as an agent for tumor imaging by positron emission tomography. Mol. Pharmaceutics, Volume 20, Pages 1842-1849, 2023. DOI: 10.1021/acs.molpharmaceut.2c01069
● Tsuyoshi Tahara et. al., A novel 11C-labeled thymidine analog, [11C]AZT, for tumor imaging by positron emission tomography, EJNMMI Research, Volume 5, Pages e45, 2015. DOI: 10.1186/s13550-015-0124-0

Last updated date：October 15, 2026

 

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