Victoria López-Rodríguez1, Carlos Galindo-Sarco2, Francisco O García-Pérez3, Guillermina Ferro-Flores4, Oscar Arrieta5, Miguel A Ávila-Rodríguez6. 1. Unidad Radiofarmacia-Ciclotrón, Facultad de Medicina, Universidad Nacional Autónoma de México, Mexico City, Mexico. 2. Departamento de Radiología, Instituto Nacional de Cancerología, Mexico City, Mexico. 3. Departamento de Medicina Nuclear, Instituto Nacional de Cancerología, Mexico City, Mexico. 4. Gerencia de Aplicaciones Nucleares en la Salud, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac, Mexico; and. 5. Departamento de Oncología Médica, Instituto Nacional de Cancerología, Mexico City, Mexico. 6. Unidad Radiofarmacia-Ciclotrón, Facultad de Medicina, Universidad Nacional Autónoma de México, Mexico City, Mexico avilarod@uwalumni.com.
Abstract
UNLABELLED: Peptides containing the Arg-Gly-Asp (RGD) sequence have high affinity for αvβ3 integrin receptors overexpressed in tumor cells. The objective of this research was to determine the biodistribution and estimate the radiation dose from (68)Ga-DOTA-E-[c(RGDfK)]2 using whole-body PET scans in humans. METHODS: Five healthy volunteers (2 women, 3 men; mean age ± SD, 37.2 ± 15.6 y; range, 28-65 y; mean weight, 79.2 ± 21.0 kg; range, 64-115 kg) were included. After intravenous injection of the tracer (198.3 ± 3.3 MBq), 3 successive whole-body (vertex to mid thigh) PET/CT scans at 3 time points (30, 60, and 120 min) were obtained on a 16-slice PET/CT scanner. The subjects did not void the bladder until the entire series of images was completed. Low-dose CT without contrast agent was used for anatomic localization and attenuation correction. OLINDA/EXM software was applied to calculate human radiation doses using the reference adult model. RESULTS: The highest uptake was in the urinary bladder, followed by the liver, kidneys, and spleen, in descending order. The critical organ was the urinary bladder wall. The mean effective doses (all subjects, men and women) were 34.1 ± 4.9, 31.0 ± 2.4, and 20.9 ± 5.2 μSv/MBq for the no-voiding, 2.5-h-voiding, and 1-h-voiding models, respectively. CONCLUSION: Of particular interest in this research was the visualization of the choroid plexus and ventricular system, which seems to be a characteristic of RGD-dimeric peptides. Measured absorbed doses and effective doses are comparable to other previously reported RGD-based radiopharmaceuticals labeled with (68)Ga and (18)F. Therefore, (68)Ga-DOTA-E-[c(RGDfK)]2 can safely be used for imaging integrin αVβ3 expression.
UNLABELLED: Peptides containing the Arg-Gly-Asp (RGD) sequence have high affinity for αvβ3 integrin receptors overexpressed in tumor cells. The objective of this research was to determine the biodistribution and estimate the radiation dose from (68)Ga-DOTA-E-[c(RGDfK)]2 using whole-body PET scans in humans. METHODS: Five healthy volunteers (2 women, 3 men; mean age ± SD, 37.2 ± 15.6 y; range, 28-65 y; mean weight, 79.2 ± 21.0 kg; range, 64-115 kg) were included. After intravenous injection of the tracer (198.3 ± 3.3 MBq), 3 successive whole-body (vertex to mid thigh) PET/CT scans at 3 time points (30, 60, and 120 min) were obtained on a 16-slice PET/CT scanner. The subjects did not void the bladder until the entire series of images was completed. Low-dose CT without contrast agent was used for anatomic localization and attenuation correction. OLINDA/EXM software was applied to calculate human radiation doses using the reference adult model. RESULTS: The highest uptake was in the urinary bladder, followed by the liver, kidneys, and spleen, in descending order. The critical organ was the urinary bladder wall. The mean effective doses (all subjects, men and women) were 34.1 ± 4.9, 31.0 ± 2.4, and 20.9 ± 5.2 μSv/MBq for the no-voiding, 2.5-h-voiding, and 1-h-voiding models, respectively. CONCLUSION: Of particular interest in this research was the visualization of the choroid plexus and ventricular system, which seems to be a characteristic of RGD-dimeric peptides. Measured absorbed doses and effective doses are comparable to other previously reported RGD-based radiopharmaceuticals labeled with (68)Ga and (18)F. Therefore, (68)Ga-DOTA-E-[c(RGDfK)]2 can safely be used for imaging integrin αVβ3 expression.
Authors: Philipp M Kazmierczak; Andrei Todica; Franz-Josef Gildehaus; Heidrun Hirner-Eppeneder; Matthias Brendel; Ralf S Eschbach; Magdalena Hellmann; Konstantin Nikolaou; Maximilian F Reiser; Hans-Jürgen Wester; Saskia Kropf; Axel Rominger; Clemens C Cyran Journal: PLoS One Date: 2016-12-19 Impact factor: 3.240
Authors: Silvano Gnesin; Periklis Mitsakis; Francesco Cicone; Emmanuel Deshayes; Vincent Dunet; Augusto F Gallino; Marek Kosinski; Sébastien Baechler; Franz Buchegger; David Viertl; John O Prior Journal: EJNMMI Res Date: 2017-05-18 Impact factor: 3.138
Authors: D Lobeek; M Rijpkema; S Y A Terry; J D M Molkenboer-Kuenen; L Joosten; E A J van Genugten; A C H van Engen-van Grunsven; J H A M Kaanders; S A H Pegge; O C Boerman; W L J Weijs; M A W Merkx; C M L van Herpen; R P Takes; E H J G Aarntzen; W J G Oyen Journal: Eur J Nucl Med Mol Imaging Date: 2020-03-20 Impact factor: 9.236