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Clinical Translation of a Dual Integrin-and GRPR-targeting PET Radiotracer 68 Ga-DOTA-RGD-RM26 in Glioma
Rongxi Wang1,2,3, Ziyang Li4, Li'ao Wang4,5
1State Key Laboratory of Complex Severe and Rare Diseases, Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Department of Nuclear Medicine, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing, China.
Purpose:
Radiopharmaceuticals targeting integrin α V β 3 and gastrin-releasing peptide receptor (GRPR) are widely applied for imaging of patients with gliomas. This study aims to evaluate an integrin α V β 3 and GRPR dual-targeting PET radiotracer, 68 Ga-labeled DOTA-RGD-RM26 ( 68 Ga-DOTA-RGD-RM26) in patients with glioma and other brain tumors.
Patients And Methods:
The radiotracer 68 Ga-DOTA-RGD-RM26 was synthesized based on the previously reported peptide RGD-RM26-03 (LNC1015). Preclinical evaluation was assessed in the U87 xenograft model using Micro-PET/CT. Clinical applicability was evaluated in 34 patients with brain tumors (36 lesions), with head-to-head comparisons to single-targeting tracers 68 Ga-RM26 and 68 Ga-RGD in 7 and 11 glioma patients, respectively.
Results:
68 Ga-DOTA-RGD-RM26 demonstrated high affinity and specificity for integrin α V β 3 -positive and GRPR-positive U87 tumors. Tumor uptake of 68 Ga-DOTA-RGD-RM26 was higher than that of 68 Ga-RM26 and 68 Ga-RGD, with longer tumor retention. The radiotracer was well tolerated by all patients, with no reported side effects. The detection rate for gliomas was 84.6% (22/26) on 68 Ga-DOTA-RGD-RM26 PET/CT, with 95% (19/20) sensitivity for high-grade gliomas (HGGs). HGGs exhibited higher SUV max , SUV mean , and tumor-to-background (T/B) ratio compared with low-grade gliomas (LGGs) ( P <0.001). T/B ratios based on the SUV mean were higher for 68 Ga-DOTA-RGD-RM26 than for 68 Ga-RM26 (28.4±11.2 vs. 16.8±5.8, P =0.009) and 68 Ga-RGD (20.2±8.3 vs. 11.2±4.5, P =0.004). Spearman analysis revealed significant correlations between 68 Ga-DOTA-RGD-RM26 uptake parameters (SUV max , SUV mean and T/B ratio) and WHO grading and Ki-67% in 26 glioma lesions ( P =0.01). The radiotracer also performed well in other types of brain tumors.
Conclusions:
68 Ga-DOTA-RGD-RM26 exhibits superior tumor uptake and retention compared with single-targeting tracers, making it a promising tracer for the diagnosis and staging of gliomas and other brain tumors with integrin α V β 3 and GRPR expression.
Insights
A new dual-targeting PET radiotracer, 68Ga-DOTA-RGD-RM26, shows improved tumor uptake and retention for imaging brain tumors. This advanced tracer offers superior diagnostic potential for gliomas and other brain cancers expressing specific receptors.
Area of Science:
- Nuclear Medicine
- Oncology
- Radiopharmaceutical Chemistry
Background:
- Integrin αVβ3 and gastrin-releasing peptide receptor (GRPR) are key targets for glioma imaging.
- Current single-targeting radiotracers have limitations in sensitivity and specificity.
Purpose of the Study:
- To evaluate the dual-targeting PET radiotracer 68Ga-DOTA-RGD-RM26 for imaging brain tumors.
- To compare its performance against single-targeting tracers.
Main Methods:
- Synthesis and preclinical evaluation of 68Ga-DOTA-RGD-RM26 in U87 xenografts.
- Clinical assessment in 34 patients with brain tumors.
- Head-to-head comparison with 68Ga-RM26 and 68Ga-RGD in glioma patients.
Main Results:
- 68Ga-DOTA-RGD-RM26 showed high affinity and specificity, with superior tumor uptake and retention compared to single-targeting tracers.
- Detection rate for gliomas was 84.6%, with 95% sensitivity for high-grade gliomas.
- Significant correlations were found between tracer uptake and tumor grade/Ki-67.
- Well-tolerated with no reported side effects.
Conclusions:
- 68Ga-DOTA-RGD-RM26 is a promising dual-targeting tracer for diagnosing and staging gliomas and other brain tumors.
- Its superior performance enhances imaging capabilities for tumors expressing integrin αVβ3 and GRPR.
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