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Clinical Translation of a Dual-Integrin αvβ3- and CD13-Targeting PET Tracer
Xiao Zhang, Biao Yang, Chunxia Qin
1Hexin (Suzhou) Pharmaceutical Technology Co, Ltd, Taicang, China.
Clinical Nuclear Medicine
|January 23, 2025
Summary
The novel PET radiotracer 68 Ga-HX01 is safe and effective for visualizing tumor neovascularization by targeting integrin αvβ3 and CD13. This dual-targeting agent shows promise in cancer diagnosis and patient selection for antiangiogenic therapy.
Area of Science:
- Nuclear Medicine
- Oncology
- Radiochemistry
Background:
- Tumor angiogenesis is critical for cancer growth and metastasis.
- Integrin αvβ3 and CD13 are key markers of tumor neovascularization.
Purpose of the Study:
- To evaluate the clinical safety and efficacy of 68 Ga-labeled heterodimeric peptide (68 Ga-HX01) for imaging tumor neovascularization.
- To assess the diagnostic potential of 68 Ga-HX01 in patients with various malignancies.
Main Methods:
- Biodistribution, pharmacokinetics, and radiation dosimetry of 68 Ga-HX01 were studied in healthy volunteers.
- Positron emission tomography (PET) imaging with 68 Ga-HX01 was performed in patients with malignancies.
- Tumor integrin αvβ3 and CD13 expression was confirmed using immunohistochemistry.
Main Results:
- 68 Ga-HX01 demonstrated favorable safety and tolerability with a low effective radiation dose in healthy volunteers.
- PET imaging clearly visualized malignant lesions, with significantly higher tumor uptake compared to surrounding tissues (P < 0.05).
- A positive correlation was observed between tumor uptake and semiquantitative expression of integrin αvβ3 and CD13 (P < 0.05).
Conclusions:
- 68 Ga-HX01 is a safe PET radiotracer with low radiation exposure for clinical use.
- The dual integrin αvβ3 and CD13-targeting tracer is effective for tumor diagnosis.
- 68 Ga-HX01 may aid in patient prognosis and selection for antiangiogenic therapies.

