Human Biodistribution and Radiation Dosimetry of the Targeting Fibroblast Growth Factor Receptor 1-Positive Tumors Tracer [ 68 Ga]Ga-DOTA-FGFR1-Peptide.

Autor: Yuan H; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Chen X; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Zhao M; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Zhao X; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China.; Hebei Provincial Key Laboratory of Tumor Microenvironment and Drug Resistance, Shijiazhuang, China., Chen X; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Han J; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Zhang Z; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Zhang J; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Wang J; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Dai M; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China., Liu Y; Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang, China.
Jazyk: angličtina
Zdroj: Cancer biotherapy & radiopharmaceuticals [Cancer Biother Radiopharm] 2024 Dec; Vol. 39 (10), pp. 712-720. Date of Electronic Publication: 2024 Jul 18.
DOI: 10.1089/cbr.2024.0073
Abstrakt: Objective: [ 68 Ga]Ga-DOTA-FGFR1-peptide is a novel positron emission tomography (PET) radiotracer targeting fibroblast growth factor receptor 1 (FGFR1). This study evaluated the safety, biodistribution, radiation dosimetry, and imaging potential of [ 68 Ga]Ga-DOTA-FGFR1-peptide. Methods: The FGFR1-targeting peptide DOTA-(PEG2)-KAEWKSLGEEAWHSK was synthesized by manual solid-phase peptide synthesis with high-performance liquid chromatography purification, and labeled with 68 Ga with DOTA as chelating agent. We recruited 14 participants and calculated the radiation dose of 4 of these pathologically confirmed nontumor subjects using OLINDA/EXM 2.2.0 software. At the same time, the imaging potential in 10 of these lung cancer patients was evaluated. Results: The biodistribution of [ 68 Ga]Ga-DOTA-FGFR1-peptide in 4 subjects showed the highest uptake in the bladder and kidney. Dosimetry analysis indicated that the bladder wall received the highest effective dose (3.73E-02 mSv/MBq), followed by the lungs (2.36E-03 mSv/MBq) and red bone marrow (2.09E-03 mSv/MBq). No normal organs were found to have excess specific absorbed doses. The average systemic effective dose was 4.97E-02 mSv/MBq. The primary and metastatic tumor lesions were clearly visible on PET/computed tomography (CT) images in 10 patients. Conclusion: Our results indicate that [ 68 Ga]Ga-DOTA-FGFR1-peptide has a good dosimetry profile and can be used safely in humans, and it has significant potential value for clinical PET/CT imaging.
Databáze: MEDLINE