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Published on: October 26, 2018
Optimized CDK19 PET Tracers: Spirocyclic-Driven Design and Prostate Cancer Imaging.
Jiang Yu1, Zhao Yang2,3, Feifei Xu1
1State Key Laboratory of Advanced Medical Materials and Devices, Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Tianjin Institutes of Health Science, Institute of Radiation Medicine, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin 300192, China.
A novel imaging tracer, 68Ga-IRM-8c, targets Cyclin-dependent kinase 19 (CDK19) for improved prostate cancer (PCa) detection. This tracer successfully identified lesions in advanced PCa patients, showing promising diagnostic potential.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Prostate cancer (PCa) exhibits high expression of Cyclin-dependent kinase 19 (CDK19).
- CDK19 is a potential therapeutic and diagnostic target in PCa.
- Optimizing imaging tracers for CDK19 is crucial for enhanced PCa detection.
Purpose of the Study:
- To optimize the structure of CDK19-targeted imaging tracers for improved PCa detection.
- To evaluate the efficacy and safety of a novel tracer, 68Ga-IRM-8c, in preclinical and clinical settings.
Main Methods:
- Structure-activity relationship studies and cyclization strategies were employed to optimize the lead compound's linker.
- Incorporation of a spirocyclic structure to enhance ligand binding affinity.
- Preclinical imaging in mice and clinical imaging in advanced castration-resistant prostate cancer (CRPC) patients using 68Ga-IRM-8c.
Main Results:
- Spirocyclic structure optimization improved ligand binding conformation and affinity (increased IC50).
- Mice imaging demonstrated clear tumor visualization and acceptable tissue safety.
- 68Ga-IRM-8c successfully identified three distinct lesions in two CRPC patients with favorable tumor-to-nontumor ratios.
Conclusions:
- 68Ga-IRM-8c effectively detects lesions in PCa patients.
- The tracer shows preliminary tissue safety, highlighting CDK19's potential in PCa diagnosis.
- Optimized CDK19-targeted tracers offer a promising avenue for advanced PCa imaging.
