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Updated: Jun 20, 2026
Development of a 68Gallium-Labeled D-Peptide PET Tracer for Imaging Programmed Death-Ligand 1 Expression
Published on: February 3, 2023
Advances in PD-L1 Targeted Molecular Imaging Radiotracers Research: From Preclinical Exploration to Clinical
Chang Yu1,2,3, Ya Liu1,2,3, Haojie Chen4
1Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, 646000, Sichuan, People's Republic of China.
Abstract:
Programmed death-ligand 1 (PD-L1) is highly expressed in tumour cells and the tumour microenvironment, mediates tumour immune evasion, and is a key target for cancer immunotherapy. Immunohistochemistry (IHC), as a conventional method for PD-L1 detection, has limitations such as invasiveness, temporal and spatial heterogeneity, and an inability to provide dynamic monitoring. In contrast, PD-L1-targeted molecular imaging enables non-invasive, quantitative, and whole-body visual assessment of PD-L1 expression, offering a precise tool for patient selection, treatment response prediction and dynamic monitoring in immunotherapy, and has thus become a focal point in precision oncology research. This paper systematically reviews the development trajectory of PD-L1-targeting radiotracers, including monoclonal antibodies, peptides, nanobodies, aptamers and small molecules. It summarises the targeting performance, pharmacokinetics, imaging efficacy and safety in preclinical and clinical studies; compares the advantages and suitable applications of different types of tracers; analyses the challenges currently facing the field, such as the lack of evaluation standards, tumour heterogeneity, insufficient clinical translation and a scarcity of multicentre data; and offers a prospect on the standardisation of PD-L1-targeted molecular imaging, the integration of diagnosis and treatment, multimodal imaging and its promotion and application in primary care settings. To date, more than 40 PD-L1-targeting tracers have undergone preclinical or clinical validation, with non-invasive imaging demonstrated to be feasible in over 100 cancer patients; early data support further in-depth research and clinical translation in this field.
Insights
Molecular imaging targeting programmed death-ligand 1 (PD-L1) offers a non-invasive alternative to traditional methods for assessing cancer immunotherapy targets. This review explores PD-L1 tracers for improved patient selection and treatment monitoring.
Area of Science:
- Oncology
- Molecular Imaging
- Immunotherapy
Background:
- Programmed death-ligand 1 (PD-L1) is crucial for tumor immune evasion and a key immunotherapy target.
- Conventional immunohistochemistry (IHC) for PD-L1 detection has limitations including invasiveness and heterogeneity.
- PD-L1-targeted molecular imaging provides non-invasive, quantitative, and dynamic assessment of PD-L1 expression.
Purpose of the Study:
- To systematically review the development of PD-L1-targeting radiotracers.
- To summarize tracer performance, efficacy, and safety in preclinical and clinical studies.
- To analyze current challenges and future prospects for PD-L1 imaging in precision oncology.
Main Methods:
- Review of PD-L1-targeting radiotracers including antibodies, peptides, nanobodies, aptamers, and small molecules.
- Summary of targeting performance, pharmacokinetics, imaging efficacy, and safety data.
- Analysis of challenges like standardization, heterogeneity, and clinical translation.
Main Results:
- Over 40 PD-L1 tracers have undergone validation, with non-invasive imaging feasible in over 100 cancer patients.
- Various tracers show promise for patient selection, treatment prediction, and dynamic monitoring.
- Early data indicate the potential for PD-L1 molecular imaging in clinical oncology.
Conclusions:
- PD-L1-targeted molecular imaging is a promising tool for precision oncology, complementing or potentially replacing IHC.
- Further research and standardization are needed for widespread clinical translation.
- Integration with diagnosis, treatment, and multimodal imaging strategies is a future direction.
