RT Journal Article
SR Electronic
T1 Clinical Evaluation of <sup>68</sup>Ga-FAPI-RGD for Imaging of Fibroblast Activation Protein and Integrin α<sub>v</sub>β<sub>3</sub> in Various Cancer Types
JF Journal of Nuclear Medicine
JO J Nucl Med
FD Society of Nuclear Medicine
SP jnumed.122.265383
DO 10.2967/jnumed.122.265383
A1 Zhao, Liang
A1 Wen, Xuejun
A1 Xu, Weizhi
A1 Pang, Yizhen
A1 Sun, Long
A1 Wu, Xiaoming
A1 Xu, Pengfei
A1 Zhang, Jingjing
A1 Guo, Zhide
A1 Lin, Qin
A1 Chen, Xiaoyuan
A1 Chen, Haojun
YR 2023
UL http://jnm.snmjournals.org/content/early/2023/05/04/jnumed.122.265383.abstract
AB Radiolabeled fibroblast activation protein (FAP) inhibitors (FAPIs) and Arg-Gly-Asp (RGD) peptides have been extensively investigated for imaging of FAP- and integrin αvβ3–positive tumors. In this study, a FAPI-RGD heterodimer was radiolabeled with 68Ga and evaluated in patients with cancer. We hypothesized that the heterodimer, recognizing both FAP and integrin αvβ3, would be advantageous because of its dual-receptor–targeting property. Methods: The effective dose of 68Ga-FAPI-RGD was evaluated in 3 healthy volunteers. The clinical feasibility of 68Ga-FAPI-RGD PET/CT was evaluated in 22 patients with various types of cancer, and the results were compared with those of 18F-FDG and 68Ga-FAPI-46. Results: 68Ga-FAPI-RGD was tolerated well, with no adverse events in any of the healthy volunteers or patients. The effective dose from 68Ga-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 68Ga-FAPI-RGD PET/CT were significantly higher than those in 18F-FDG PET/CT (primary tumors: SUVmax, 18.0 vs. 9.1 [P &lt; 0.001], and TBR, 15.2 vs. 5.5 [P &lt; 0.001]; lymph node metastases: SUVmax, 12.1 vs. 6.1 [P &lt; 0.001], and TBR, 13.3 vs. 4.1 [P &lt; 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. 68Ga-FAPI-RGD PET/CT also yielded a higher radiotracer uptake and TBR than 68Ga-FAPI-46 PET/CT did. Conclusion: 68Ga-FAPI-RGD exhibited improved tumor uptake and TBR compared with 18F-FDG and 68Ga-FAPI PET/CT. This study demonstrated the safety and clinical feasibility of 68Ga-FAPI-RGD PET/CT for imaging of various types of cancer.