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FAPI-74 PET/CT Using Either (18)F-AlF or Cold-Kit (68)Ga Labeling: Biodistribution, Radiation Dosimetry, and Tumor Delineation in Lung Cancer Patients
(68)Ga-fibroblast activation protein inhibitors (FAPIs) 2, 4, and 46 have already been proposed as promising PET tracers. However, the short half-life of (68)Ga (68 min) creates problems with manufacture and delivery. (18)F (half-life, 110 min) labeling would result in a more practical large-scale p...
Autores principales: | , , , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Society of Nuclear Medicine
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8679591/ https://www.ncbi.nlm.nih.gov/pubmed/32591493 http://dx.doi.org/10.2967/jnumed.120.245084 |
Sumario: | (68)Ga-fibroblast activation protein inhibitors (FAPIs) 2, 4, and 46 have already been proposed as promising PET tracers. However, the short half-life of (68)Ga (68 min) creates problems with manufacture and delivery. (18)F (half-life, 110 min) labeling would result in a more practical large-scale production, and a cold-kit formulation would improve the spontaneous availability. The NOTA chelator ligand FAPI-74 can be labeled with both (18)F-AlF and (68)Ga. Here, we describe the in vivo evaluation of (18)F-FAPI-74 and a proof of mechanism for (68)Ga-FAPI-74 labeled at ambient temperature. Methods: In 10 patients with lung cancer, PET scans were acquired at 10 min, 1 h, and 3 h after administration of 259 ± 26 MBq of (18)F-FAPI-74. Physiologic biodistribution and tumor uptake were semiquantitatively evaluated on the basis of SUV at each time point. Absorbed doses were evaluated using OLINDA/EXM, version 1.1, and QDOSE dosimetry software with the dose calculator IDAC-Dose, version 2.1. Identical methods were used to evaluate one examination after injection of 263 MBq of (68)Ga-FAPI-74. Results: The highest contrast was achieved in primary tumors, lymph nodes, and distant metastases at 1 h after injection, with an SUV(max) of more than 10. The effective dose per a 100-MBq administered activity of (18)F-FAPI-74 was 1.4 ± 0.2 mSv, and for (68)Ga-FAPI-74 it was 1.6 mSv. Thus, the radiation burden of a diagnostic (18)F-FAPI-74 PET scan is even lower than that of PET scans with (18)F-FDG and other (18)F tracers; (68)Ga-FAPI-74 is comparable to other (68)Ga ligands. FAPI PET/CT supported target volume definition for guiding radiotherapy. Conclusion: The high contrast and low radiation burden of FAPI-74 PET/CT favor multiple clinical applications. Centralized large-scale production of (18)F-FAPI-74 or decentralized cold-kit labeling of (68)Ga-FAPI-74 allows flexible routine use. |
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