Kit preparation and biokinetics in women of 99mTc-EDDA/HYNIC-E-[c(RGDfK)]2 for breast cancer imaging

Ortiz-Arzate, Z.; Santos-Cuevas, Clara; Ocampo‐García, Blanca; Ferro-Flores, Guillermina; Garcı́a-Becerra, Rocı́o; Estrada, G.; Gómez-Argumosa, Edgar; Izquierdo-Sánchez, Vanessa

doi:10.1097/mnm.0000000000000065

Cited by 22 publications

(22 citation statements)

References 29 publications

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“…In this system, the retention time for free 99mTc, 99mTc-coligand and 99m Tc-HYNIC-TMTP1 were 1.6, 2.2 and 13.0-13.6 min, respectively. [20]. A reverse-phase Sep-Pak C-18 cartridge was preconditioned with 5 mL of ethanol followed by 5 mL of 0.9% NaCl solution and 5 mL of air.…”

Section: Radiochemistrymentioning

confidence: 99%

Evaluation of 99mTc-HYNIC-TMTP1 as a tumor-homing imaging agent targeting metastasis with SPECT

Cheng

Dong

et al. 2015

Nuclear Medicine and Biology

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Section: Radiochemistrymentioning

confidence: 99%

Evaluation of 99mTc-HYNIC-TMTP1 as a tumor-homing imaging agent targeting metastasis with SPECT

Cheng

Dong

et al. 2015

Nuclear Medicine and Biology

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“…Additionally, detailed biodistribution and measured radiation dosimetry in humans have been reported for 18 F-galactoRGD (26), 18 F-RGD-K5 (27), 68 Ga-NOTA-RGD (28), and 18 F-FPPRGD2 (29). Given the proven higher affinity of RGDdimeric conjugates for a V b 3 integrin receptors (17)(18)(19)(20), RGDdimeric derivatives labeled with 99m Tc (30,31) for SPECT and with 18 F (29,32) for PET have been evaluated in humans.…”

mentioning

confidence: 99%

PET-Based Human Dosimetry of the Dimeric α_vβ₃ Integrin Ligand ⁶⁸Ga-DOTA-E-[c(RGDfK)]₂, a Potential Tracer for Imaging Tumor Angiogenesis

et al. 2015

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Peptides containing the Arg-Gly-Asp (RGD) sequence have high affinity for α v β 3 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 α V β 3 expression. The last few years have witnessed the development of a virtual revolution in PET molecular imaging, and radiolabeled receptor-binding peptides are emerging as powerful tools for imaging and therapy applications of tumors expressing peptide binding receptors (1-3). Somatostatin analogs have been in use the longest, have led to the accumulation of a vast amount of data, and have proven useful for the management of patients with neuroendocrine tumors (4-8). Several other peptide receptorbinding compounds have been synthesized within the past few years and are currently in various research stages-in vitro, in vivo, and preclinical studies-but have not yet been approved for clinical use (9-11). These new and rapidly expanding peptide-based radiopharmaceuticals deserve close attention.It has been shown that peptides based on the RGD amino acid sequence have a high affinity and selectivity for a V b 3 integrin receptors (12). The a V b 3 integrins are transmembrane proteins that are preferentially expressed on proliferating endothelial cells but absent from quiescent endothelial cells (13). Integrins are overexpressed on newly formed blood vessels of actively growing tumors and are therefore potential targets for receptor-mediated tumor imaging and therapy when labeled with the proper radionuclide. Angiogenesis, the formation of n...

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“…Moreover, (18)F-glyco-RGD peptides are used in PET imaging of integrin expression, modulation, and biodistribution. Recently integrins have become increasingly attractive targets for molecular imaging of angiogenesis with positron emission tomography or single-photon emission computed tomography, but the reliable production of radiopharmaceuticals remains challenging [87]. …”

Section: Cns Protectionmentioning

confidence: 99%

Drug Delivery Systems, CNS Protection, and the Blood Brain Barrier

Upadhyay

2014

BioMed Research International

350

222

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Present review highlights various drug delivery systems used for delivery of pharmaceutical agents mainly antibiotics, antineoplastic agents, neuropeptides, and other therapeutic substances through the endothelial capillaries (BBB) for CNS therapeutics. In addition, the use of ultrasound in delivery of therapeutic agents/biomolecules such as proline rich peptides, prodrugs, radiopharmaceuticals, proteins, immunoglobulins, and chimeric peptides to the target sites in deep tissue locations inside tumor sites of brain has been explained. In addition, therapeutic applications of various types of nanoparticles such as chitosan based nanomers, dendrimers, carbon nanotubes, niosomes, beta cyclodextrin carriers, cholesterol mediated cationic solid lipid nanoparticles, colloidal drug carriers, liposomes, and micelles have been discussed with their recent advancements. Emphasis has been given on the need of physiological and therapeutic optimization of existing drug delivery methods and their carriers to deliver therapeutic amount of drug into the brain for treatment of various neurological diseases and disorders. Further, strong recommendations are being made to develop nanosized drug carriers/vehicles and noninvasive therapeutic alternatives of conventional methods for better therapeutics of CNS related diseases. Hence, there is an urgent need to design nontoxic biocompatible drugs and develop noninvasive delivery methods to check posttreatment clinical fatalities in neuropatients which occur due to existing highly toxic invasive drugs and treatment methods.

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Kit preparation and biokinetics in women of 99mTc-EDDA/HYNIC-E-[c(RGDfK)]2 for breast cancer imaging

Cited by 22 publications

References 29 publications

Evaluation of 99mTc-HYNIC-TMTP1 as a tumor-homing imaging agent targeting metastasis with SPECT

Evaluation of 99mTc-HYNIC-TMTP1 as a tumor-homing imaging agent targeting metastasis with SPECT

PET-Based Human Dosimetry of the Dimeric α_vβ₃ Integrin Ligand ⁶⁸Ga-DOTA-E-[c(RGDfK)]₂, a Potential Tracer for Imaging Tumor Angiogenesis

Drug Delivery Systems, CNS Protection, and the Blood Brain Barrier

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Kit preparation and biokinetics in women of 99mTc-EDDA/HYNIC-E-[c(RGDfK)]2 for breast cancer imaging

Cited by 22 publications

References 29 publications

Evaluation of 99mTc-HYNIC-TMTP1 as a tumor-homing imaging agent targeting metastasis with SPECT

Evaluation of 99mTc-HYNIC-TMTP1 as a tumor-homing imaging agent targeting metastasis with SPECT

PET-Based Human Dosimetry of the Dimeric αvβ3 Integrin Ligand 68Ga-DOTA-E-[c(RGDfK)]2, a Potential Tracer for Imaging Tumor Angiogenesis

Drug Delivery Systems, CNS Protection, and the Blood Brain Barrier

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PET-Based Human Dosimetry of the Dimeric α_vβ₃ Integrin Ligand ⁶⁸Ga-DOTA-E-[c(RGDfK)]₂, a Potential Tracer for Imaging Tumor Angiogenesis