Synthesis and Radiation Dosimetry of [⁶⁸Ga]-Ga-Lys¹, Lys³-DOTA-Bombesin (1,14) Antagonist for PET-Imaging, as a Potential Theragnostic Tracer in Oncology  

作　　者：Juan C. Manrique-Arias Quetzali Pitalua-Cortes Roberto Pedrero-Piedras Géiser Rodríguez-Mena Tessy López Cristian Cabezas-Ortiz Osvaldo García-Pérez Juan C. Manrique-Arias;Quetzali Pitalua-Cortes;Roberto Pedrero-Piedras;Géiser Rodríguez-Mena;Tessy López;Cristian Cabezas-Ortiz;Osvaldo García-Pérez(Departamento de Medicina Nuclear, Ciclotrón y Radiofarmacia Instituto Nacional de Cancerología, México City, México;Cancer Center Cyclotron Department, Doctors Hospital, Monterrey, México;Departamento de Atención a la Salud, Universidad Autónoma Metropolitana-Xochimilco, México City, México)

机构地区：[1]Departamento de Medicina Nuclear, Ciclotrón y Radiofarmacia Instituto Nacional de Cancerología, México City, México [2]Cancer Center Cyclotron Department, Doctors Hospital, Monterrey, México [3]Departamento de Atención a la Salud, Universidad Autónoma Metropolitana-Xochimilco, México City, México

出　　处：《Journal of Encapsulation and Adsorption Sciences》2020年第2期29-41,共13页封装与吸附期刊（英文）

摘　　要：This Bombesin (BBN), a tetradecapeptide analog of human gastrin-releasing peptide (GRP) with a high binding affinity for GRP receptors (GRPR), is over- expressed in early stages of androgen-dependent prostate carcinomas, but not in advanced stages. Therefore, there is a need to develop effective tracers for the accurate and specific detection of this disease. The objective of this study was to evaluate Lys¹, Lys³-DOTA-BBN (1,14) analog with the radiolabeled positron emitter [⁶⁸Ga]-Ga-BBN for receptor imaging with PET, and to determine its biodistribution and radiation dosimetry using whole-body (WB) PET scans in healthy volunteers. The highest uptake was in the pancreas, followed by urinary bladder. The critical organ was pancreas with a mean absorbed dose of 206 ± 0.7, 210 ± 0.7, 120 ± 0.9, 390.23 ± 0.6 μGy/MBq and the effective doses were estimated as 73.2 ± 0.6, 49.8 ± 0.3 μGy/MBq (women and men, respectively).This Bombesin (BBN), a tetradecapeptide analog of human gastrin-releasing peptide (GRP) with a high binding affinity for GRP receptors (GRPR), is over- expressed in early stages of androgen-dependent prostate carcinomas, but not in advanced stages. Therefore, there is a need to develop effective tracers for the accurate and specific detection of this disease. The objective of this study was to evaluate Lys¹, Lys³-DOTA-BBN (1,14) analog with the radiolabeled positron emitter [⁶⁸Ga]-Ga-BBN for receptor imaging with PET, and to determine its biodistribution and radiation dosimetry using whole-body (WB) PET scans in healthy volunteers. The highest uptake was in the pancreas, followed by urinary bladder. The critical organ was pancreas with a mean absorbed dose of 206 ± 0.7, 210 ± 0.7, 120 ± 0.9, 390.23 ± 0.6 μGy/MBq and the effective doses were estimated as 73.2 ± 0.6, 49.8 ± 0.3 μGy/MBq (women and men, respectively).

关 键 词：Radiation Dosimetry Biodistribution PET Imaging Radiopharmaceutical Lys¹ Lys³-DOTA-BBN (1 14) Bombesin Analogs 

分 类 号：R73[医药卫生—肿瘤]