First Experience of ¹⁸F-Alfatide in Lung Cancer Patients Using a New Lyophilized Kit for Rapid Radiofluorination

Abstract

18F-FPPRGD2, which was approved for clinical study recently, has favorable properties for integrin targeting and showed potential for antiangiogenic therapy and early response monitoring. However, the time-consuming multiple-step synthesis may limit its widespread applications in the clinic. In this study, we developed a simple lyophilized kit for labeling PRGD2 peptide (18F-AlF-NOTA-PRGD2, denoted as 18F-alfatide) using a fluo-ride–aluminum complex that significantly simplified the labeling procedure. Methods Nine patients with a primary diagnosis of lung cancer were examined by both static and dynamic PET imaging with 18F-alfatide, and 1 tuberculosis patient was investigated using both 18F-alfatide and 18F-FDG imaging. Standardized uptake values were measured in tumors and other main organs at 30 min and 1 h after injection. Kinetic parameters were calculated by Logan graphical analysis. Immunohisto-chemistry and staining intensity quantification were performed to confirm the expression of integrin αvβ3. Results Under the optimal conditions, the whole radiosynthesis including purifica-tion was accomplished within 20 min with a decay-corrected yield of 42.1% ± 2.0% and radiochemical purity of more than 95%. 18F-alfatide PET imaging identified all tumors, with mean standardized uptake values of 2.90 ± 0.10. Tumor-to-muscle and tumor-to-blood ratios were 5.87 ± 2.02 and 2.71 ± 0.92, respectively. Conclusion 18F-alfatide can be produced with excellent radiochemical yield and purity via a simple, 1-step, lyophilized kit. PET scanning with 18F-alfatide allows specific imaging of αvβ3 expression with good contrast in lung cancer patients. This technique might be used for the assessment of angiogene-sis and for planning and response evaluation of cancer therapies that would affect angiogenesis status and integrin expression levels.

In Vivo Evaluation of 18F-SiFAlin–Modified TATE: A Potential Challenge for 68Ga-DOTATATE, the Clinical Gold Standard for Somatostatin Receptor Imaging with PET

“…However, only a few clinical PET imaging sites routinely offer 18 F-radiolabeled peptides as a result of the typically difficult radiochemistry involved in peptide labeling with 18 F (10,11). Therefore, new labeling approaches have been developed, especially over the last decade (12)(13)(14)(15)(16). One of these approaches takes advantage of the thermodynamically favored formation of silicon-18 F bonds (silicon-fluoride acceptor [SiFA] chemistry, Fig.…”

Role of Fluorodeoxyglucose Positron Emission Tomography/Computed Tomography Imaging in Diagnosis and Staging of Lung Cancer

“…Tümör anjiogenezi ile ilişkili olarak aktifleşen endotel hücrelerinde integrin adı verilen moleküllerin ekspresyonu artar. İntegrinlerin görüntülenmesine yönelik F-18 ve Ga-68 ile işaretli çeşitli PET ajanları geliştirilmiş, bu ajanlar kullanılarak akciğer kanserinde anjiogenezin PET ile görüntülenmesine yönelik çalışmalar yapılmıştır (87,88,89). CXCR4 çeşitli solid kanseri türlerinde artmış ekspresyon gösteren, tümörün metastaz yapma potansiyeli ile ilişkili bir kemokin reseptörüdür (90,91).…”

Advancement in treatment and diagnosis of pancreatic cancer with radiopharmaceuticals

“…Angiogenesis is necessary for tumor growth and metastasis, and the integrin αvβ3 receptor plays an important role in promoting, sustaining, and regulating the angiogenesis [62] . In vitro analysis demonstrated that integrin αvβ3 receptor was expressed in 60% of invasive pancreatic ductal carcinomas and would be an excellent target for the early detection of malignant PC [63] .…”