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Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
Published on: April 25, 2025
Design, Preclinical Evaluation, and Clinical Translation of [68Ga]Ga/[177Lu]Lu-JH120061, a Novel Radiopharmaceutical
Guochang Wang1,2, Tianrui Kang1,2, Yumeng Peng1,2
1Department of Nuclear Medicine, National Regional Medical Center, Binhai Campus of the First Affiliated Hospital, Fujian Medical University, Fuzhou, China.
Purpose:
We designed and synthesized a novel compound targeting C-X-C motif chemokine receptor 4 (CXCR4), JH120061. Using clinically established Pentixafor and Pentixather as references, we evaluated the potential of [68Ga]Ga/[177Lu]Lu-JH120061 in a series of preclinical and clinical studies.
Patients And Methods:
Preclinical studies of [68Ga]Ga/[177Lu]Lu-JH120061 were conducted on CXCR4-expressing cell lines (HT1080-hCXCR4) and HT1080-hCXCR4 tumor-bearing mice. A head-to-head comparison of [68Ga]Ga-JH120061 with [68Ga]Ga-Pentixafor for PET/CT was conducted in patients with multiple myeloma (n = 5) and renal masses (n = 5). An expanded cohort of 53 patients with renal masses underwent [68Ga]Ga-JH120061 PET/CT to assess its performance in identifying renal malignancy.
Results:
Preclinical studies revealed that JH120061 demonstrated high binding affinity for CXCR4, promising cellular uptake and retention. In a clinical study, [68Ga]Ga-JH120061 PET/CT detected more malignant lesions than [68Ga]Ga-Pentixafor (94 vs. 81, P = 0.031) and showed significantly higher tumor uptake [maximum standardized uptake value (SUVmax) 22.3 ± 12.9 vs. 9.4 ± 6.5, P < 0.001, at 60 minutes]. Furthermore, [68Ga]Ga-JH120061 PET/CT exhibited excellent detectability for clear-cell renal cell carcinoma (ccRCC); its tumor uptake was significantly higher than that in non-ccRCC (SUVmax 28.9 ± 11.7 vs. 7.3 ± 2.4, P < 0.001).
Conclusions:
This study demonstrated that JH120061 may have excellent affinity for CXCR4. Notably, [68Ga]Ga-JH120061 PET/CT demonstrated a remarkable capability for detecting ccRCC. Future studies should further explore the potential of [68Ga]Ga/[177Lu]Lu-JH120061 in precision theranostics of CXCR4-positive tumors.
