No abstract

To enhance tumor uptake and retention, we designed and developed bi-specific heterodimeric radiotracers targeting both FAP and αvβ3, [ 68 Ga]Ga-FAPI-RGD. The present study aimed to evaluate the specificity, pharmacokinetics, and dosimetry of [ 68 Ga]Ga-FAPI-RGD by preclinical and preliminary clinical studies. Methods: FAPI-RGD was designed and synthesized with the quinoline-based FAPI-02 and the cyclic RGDfK peptide. Preclinical pharmacokinetics were determined in Panc02 xenograft model using microPET and biodistribution experiments. The safety and effective dosimetry of [ 68 Ga]Ga-FAPI-RGD was evaluated in 6 cancer patients, and compared with 2-[ 18 F]FDG imaging. Results: The [ 68 Ga]Ga-FAPI-RGD had good stability in saline for at least 4 h, and showed favorable binding affinity and specificity in vitro and in vivo . Compared to [ 68 Ga]Ga-FAPI-02 and [ 68 Ga]Ga-RGDfK, the tumor uptake and retention of [ 68 Ga]Ga-FAPI-RGD were very much enhanced than its monomeric counterparts at all the time points examined by microPET imaging. A total of 6 patients with various malignant tumors were prospectively enrolled. The effective dose of [ 68 Ga]Ga-FAPI-RGD was 1.94E-02 mSv/MBq. The biodistribution of [ 68 Ga]Ga-FAPI-RGD from 0 to 2 h after injection demonstrated rapid and high tumor uptake, prolonged tumor retention, and high tumor-to-background ratios (TBRs) which further increased over time. No significant difference in mean SUVmax of [ 68 Ga]Ga-FAPI-RGD and 2-[ 18 F]FDG was present in primary tumors (8.9±3.2 vs. 10.3 ± 6.9; p = 0.459). Conclusion: The dual targeting PET tracer [ 68 Ga]Ga-FAPI-RGD showed significantly improved tumor uptake and retention, as well as cleaner background over 68 Ga-labeled FAPI and RGD monospecific tracers. The first-in-human biodistribution study showed high TBRs over time, suggesting high diagnostic performance and favorable tracer kinetics for potential therapeutic applications.

A 78-year-old man with a newly diagnosed gastric adenocarcinoma underwent 18F-FDG and 68Ga-FAPI-04 PET/CT before treatment. Both 18F-FDG and 68Ga-FAPI-04 PET/CT demonstrated intense radioactivity in the gastric cancer. However, the benign Schmorl node in the inferior endplate of the T5 vertebrae showed increased uptake of 68Ga-FAPI-04, which was not FDG avid. Two months after radical gastrectomy of the gastric cancer (pT1aN0M0, IA), a follow-up CT showed that the Schmorl node in T5 vertebrae remained unchanged.

Purpose To evaluate the efficacy and safety of methylprednisolone in treating the coronavirus disease 2019 (COVID-19) patients. Methods A retrospective cohort study was conducted, and all COVID-19 patients were recruited who were admitted to the Yichang Third People’s Hospital from February 1st to March 31st, 2020. One-to-one propensity score matching (PSM) was used for minimizing confounding effects. The primary outcome was hospital mortality, with the secondary outcomes being the time needed for a positive SARS-CoV-2 nucleic acid test to turn negative and the length of hospital stay. Results Totaling 367 patients with COVID-19 hospitalized at the Yichang Third People’s Hospital were identified, of whom 276 were mild or stable COVID-19, and 67 were serious or critically ill. Among them, 255 patients were treated using methylprednisolone, and 188 did not receive any corticosteroid-related treatment. After PSM, no statistically significant difference was found in the baseline characteristics between the two groups. Regarding the outcomes, there also were no statistically significant difference between the two groups. Patients without the use of methylprednisolone were more quickly to obtain negative results of their nasopharyngeal swab tests of SARS-CoV-2 nucleic acid after treatment, compared to those receiving methylprednisolone. Conclusion Methylprednisolone could not improve the prognosis of patients with COVID-19, and the efficacy and safety of the use of methylprednisolone in patients with COVID-19 still remain uncertain, thus the use of corticosteroids clinically in patients with COVID-19 should be with cautions.