Portal de Periódicos da CAPES

Clinical Evaluation of 68 Ga-FAPI-RGD for Imaging of Fibroblast Activation Protein and Integrin α v β 3 in Various Cancer Types

2023; Society of Nuclear Medicine and Molecular Imaging; Volume: 64; Issue: 8 Linguagem: Inglês

10.2967/jnumed.122.265383

1535-5667

Liang Zhao, Xuejun Wen, Weizhi Xu, Yizhen Pang, Long Sun, Xiaoming Wu, Peng‐Fei Xu, Jingjing Zhang, Zhide Guo, Qin Lin, Xiaohong Chen, Haojun Chen,

Neuropeptides and Animal Physiology

Radiolabeled fibroblast activation protein (FAP) inhibitors (FAPIs) and Arg-Gly-Asp (RGD) peptides have been extensively investigated for imaging of FAP- and integrin α v β 3 –positive tumors. In this study, a FAPI-RGD heterodimer was radiolabeled with 68 Ga and evaluated in patients with cancer. We hypothesized that the heterodimer, recognizing both FAP and integrin α v β 3 , would be advantageous because of its dual-receptor–targeting property. Methods: The effective dose of 68 Ga-FAPI-RGD was evaluated in 3 healthy volunteers. The clinical feasibility of 68 Ga-FAPI-RGD PET/CT was evaluated in 22 patients with various types of cancer, and the results were compared with those of 18 F-FDG and 68 Ga-FAPI-46. Results: 68 Ga-FAPI-RGD was tolerated well, with no adverse events in any of the healthy volunteers or patients. The effective dose from 68 Ga-FAPI-RGD PET/CT was 1.01 × 10 −2 mSv/MBq. In clinical investigations with different types of cancer, the radiotracer uptake and tumor-to-background ratio (TBR) of primary and metastatic lesions in 68 Ga-FAPI-RGD PET/CT were significantly higher than those in 18 F-FDG PET/CT (primary tumors: SUV max , 18.0 vs. 9.1 [ P < 0.001], and TBR, 15.2 vs. 5.5 [ P < 0.001]; lymph node metastases: SUV max , 12.1 vs. 6.1 [ P < 0.001], and TBR, 13.3 vs. 4.1 [ P < 0.001]), resulting in an improved lesion detection rate and tumor delineation, particularly for the diagnosis of lymph node (99% vs. 91%) and bone (100% vs. 80%) metastases. 68 Ga-FAPI-RGD PET/CT also yielded a higher radiotracer uptake and TBR than 68 Ga-FAPI-46 PET/CT did. Conclusion: 68 Ga-FAPI-RGD exhibited improved tumor uptake and TBR compared with 18 F-FDG and 68 Ga-FAPI PET/CT. This study demonstrated the safety and clinical feasibility of 68 Ga-FAPI-RGD PET/CT for imaging of various types of cancer.