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Current Radiopharmaceuticals

William Sun, Cheryl Falzon, Ebrahim Naimi, Ali Akbari, Leonard I Wiebe, Manju Tandon, Piyush Kumar
BACKGROUND: 1-α-D-(5-Deoxy-5-[18F]fluoroarabinofuranosyl)-2-nitroimidazole ([18F]FAZA) is manufactured by nucleophilic radiofluorination of 1-&alpha;-D-(2',3'-di-O-acetyl-5'-O-toluenesulfonylarabinofuranosyl)-2-nitroimidazole (DiAcTosAZA) and alkaline deprotection to afford [18F]FAZA. High yields (>60%) under optimized conditions frequently revert to low yields (<20%) in large scale, automated syntheses. Competing side reactions and concomitant complex reaction mixtures contribute to substantial loss of product during HPLC clean-up...
October 18, 2018: Current Radiopharmaceuticals
Afrouz Asgari, Mansour Ashoor, Leila Sarkhosh, Abdollah Khorshidi, Parvaneh Shokrani
OBJECTIVE: The characterization of cancerous tissue and bone metastasis can be distinguished by the accurate assessment of accumulated uptake and activity from different radioisotopes. The various parameters and phenomena such as calibration factor, Compton scattering, attenuation and penetration are influenced intrinsic this quantity, and the qualification of images as well. METHODS: The camera calibration factor (CF) translates reconstructed count map into absolute activity map, is determined by both planar and tomographic scans using different phantom geometries...
September 13, 2018: Current Radiopharmaceuticals
Sedighe Kolivand, Peyman Amini, Hana Saffar, Saeed Rezapoor, Elahe Motevaseli, Masoud Najafi, Farzad Nouruzi, Dheyauldeen Shabeeb, Ahmed Eleojo Musa
BACKGROUND: Heart injury is one of the most important concerns after exposure to a high dose of radiation in chest cancer radiotherapy or whole body exposure to a radiation disaster. Studies have proposed that increased level of inflammatory and pro-fibrotic cytokines following radiotherapy or radiation events play a key role in the development of several side effects such as cardiovascular disorders. In current study, we aimed to evaluate the expression of IL-4 and IL-13 cytokines as well as signaling pathways such as IL4Ra1, IL13Ra2, Duox1 and Duox2...
August 30, 2018: Current Radiopharmaceuticals
I Kreimerman, E Mora-Ramirez, A L Reyes, M Bardies, E Savio, H Engler
Background The SR101 N-(3-[18F]Fluoropropyl) sulfonamide ([18F]SRF101) is a Sulforhodamine 101 derivative that was previously synthesised by our group. The fluorescent dye SR101 has been reported as a marker of astroglia in the neocortex of rodents in vivo. Objective The aim of this study was to perform a toxicological evaluation of [18F]SRF101 and to estimate human radiation dosimetry based on preclinical studies. Methods Radiation dosimetry studies were conducted based on biokinetic data obtained from a mouse model...
August 30, 2018: Current Radiopharmaceuticals
Pierpaolo Alongi, Ignazio Gaspare Vetrano, Elisa Fiasconaro, Valerio Alaimo, Riccardo Laudicella, Marina Bellavia, Francesca Rubino, Sergio Bagnato, Giuseppe Galardi
OBJECTIVE: Glioblastoma multiforme (GBM) represents the most common and malignant glioma, accounting for 45%-50% of all gliomas . The median survival time for patients with glioblastoma is only 12-15 months after surgical, chemioterapic and radiotherapic treatment; a correct diagnosis is naturally fundamental to establish a rapid and correct therapy. Non-invasive imaging plays a pivotal role in each phase of the diagnostic workup of patients with suspected for diagnosis. The aim of this case report was to describe the potential clinical impact of 18F-fluorocholine (FCH) PET/CT in the assessment of a cystic GBM mimicking a spontaneous hemorrhage...
August 17, 2018: Current Radiopharmaceuticals
Valery Radchenko, Paul Schaffer, F F Russ Knapp
No abstract text is available yet for this article.
2018: Current Radiopharmaceuticals
F Hallouard, W Sauze, S Emery, A Skanjeti, C Rioufol, M Fraysse
OBJECTIVE: The present study had determine the impact of prolonged storage in a cartridge or syringe on the quality of the [18F]-radiopharmaceuticals used in our center [18F]fludeoxyglucose and [18F]fluorocholine). [18F]-radiopharmaceuticals registered as ready-to-use drugs are prepared in multidose flasks. When the change of packaging must be made extemporaneously for the preparation of patient unit doses in a syringe or cartridge, this is under the responsibility of radiopharmacists...
2018: Current Radiopharmaceuticals
Kalevi Kairemo, Denai R Milton, Elba Etchebehere, Eric M Rohren, Homer A Macapinlac
BACKGROUND: 223Ra was the first therapeutic alpha-emitting radionuclide registered for clinical practice. This radionuclide is targeting actively bone-forming cells, and it is approved for treating metastatic skeletal disease in prostate cancer. 18F-PET is used to detect skeletal metastatic disease based on osteoblastic activity. The aim of this study was to analyze, if 18F-PET can be used assessing the results of 223Ra therapy, and to report final median overall survival in a total of 773 therapy cycles...
2018: Current Radiopharmaceuticals
Nina Pfannkuchen, Nicole Bausbacher, Stefanie Pektor, Matthias Miederer, Frank Rosch
BACKGROUND: Conjugates of bisphosphonates with macrocyclic chelators possess high potential in bone targeted radionuclide imaging and therapy. DOTAZOL, zoledronic acid conjugated to DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), demonstrated promising results in vivo in small animals as well as in first patient applications using 68Ga for diagnosis via PET and the lowenergy β-emitter 177Lu for therapy of painful bone metastases. In consideration of the fact that targeted α-therapy probably offers various advantages over the use of β--emitters, the 225Ac-labelled derivative [225Ac]Ac-DOTAZOL was synthesized and evaluated in vivo...
2018: Current Radiopharmaceuticals
Evren Gundogdu, Meliha Ekinci, Emre Ozgenc, Derya I Ozdemir, Makbule Asikoglu
OBJECTIVE: The purpose of this study was to develop lipid-water based drug delivery system of Alendronate Sodium (ALD) in liquid and solid form obtained by using spray drying method and compare these two forms with radioactive cell culture studies. METHODS: This study included the development of liquid and solid form obtained by spray drying method, radiolabelling of ALD with 99mTc, preparation of formulations containing 99mTc -ALD and evaluation of their permeability with Caco-2 cell...
2018: Current Radiopharmaceuticals
Zohreh Zal, Arash Ghasemi, Shima Azizi, Hossein Asgarian-Omran, Azadeh Montazeri, Seyed Jalal Hosseinimehr
BACKGROUND: Ionizing radiation induces DNA damage on normal cell results in apoptosis and cell deaths. OBJECTIVES: The radioprotective effects of cerium oxide nanoparticles (CNPs) on genotoxicity, apoptosis and necrosis induced by Ionizing Radiation (IR) in human healthy lymphocytes as highly radiosensitive cells were investigated. MATERIALS AND METHODS: Lymphocytes were prepared from three volunteers and then treated with CNPs at different concentrations and exposed to IR at dose 1...
2018: Current Radiopharmaceuticals
Pierpaolo Alongi, Leonardo Iaccarino, Marco Losa, Antonella Del Vecchio, Simonetta Gerevini, Valentina Plebani, Nadia Di Muzio, Pietro Mortini, Luigi Gianolli, Daniela Perani
BACKGROUND AND OBJECTIVE: Even though the benefits of radiation therapy are well established, it is important to recognize the broad spectrum of radiation-induced changes, particularly in the central nervous system. The possible damage to the brain parenchyma may have clinical consequences and in particular cognitive impairment might be one of the major complications of radiotherapy. To date, no studies have investigated the effects of focal radiation therapy on brain structure and function together with the assessment of their clinical outcomes at a long follow-up...
2018: Current Radiopharmaceuticals
Joseph G Jurcic
OBJECTIVES: Due to the shorter range and higher linear energy transfer of α-particles compared to β-particles, targeted α-particle therapy may produce more efficient tumor killing while sparing neighboring healthy cells. We will review the clinical studies using α-particle therapy for Acute Myeloid Leukemia (AML). METHODS: A series of clinical trials were conducted to assess the safety, feasibility, and anti-leukemic effects of lintuzumab, an anti-CD33 humanized monoclonal antibody, labeled with the α-emitters bismuth- 213 (213Bi) and actinium-225 (225Ac)...
2018: Current Radiopharmaceuticals
James T Harvey
OBJECTIVE: Actinium-225, and its daughter Bismuth-213, have great promise in Alpha Immuno Therapy (AIT) for treatment of various disease modalities. Unfortunately, current production levels of actinium-225 do not support broad use of either actinium-225 or bismuth-213 in development or use for disease treatment. Further, the current cost per millicurie is much too high to be sustainable long term. Resolution of both supply and cost issues allows clinical research to proceed through clinical trials and potentially produce one or more effective therapies for cancer or infectious diseases that could benefit the public...
2018: Current Radiopharmaceuticals
Licia Uccelli, Alessandra Boschi, Corrado Cittanti, Petra Martini, Luca Lodi, Elisa Zappaterra, Simona Romani, Samanta Zaccaria, Davide Cecconi, Ilaria Rambaldi, Ivan Santi, Stefano Panareo, Melchiore Giganti, Mirco Bartolomei
BACKGROUND AND OBJECTIVE: Gallium-68 is a PET isotope available in each nuclear medicine departments, even those not equipped with a cyclotron, since it is easily obtained by eluting compact and transportable generator system. The preparation of Ga-68 DOTA-labeled compounds is performed by remotely controlled automated systems developed in order to ensure production efficiency, reproducibility of the results, fast reaction time, to facilitate the synthesis and minimize the radiation exposure...
2018: Current Radiopharmaceuticals
Alfred Morgenstern, Christos Apostolidis, Clemens Kratochwil, Mike Sathekge, Leszek Krolicki, Frank Bruchertseifer
Background: Recent reports of the remarkable therapeutic efficacy of 225Ac-labeled PSMA- 617 for therapy of metastatic castration-resistant prostate cancer have underlined the clinical potential of targeted alpha therapy. Objective and Conclusion: This review describes methods for the production of 225Ac and its daughter nuclide 213Bi and summarizes the current clinical experience with both alpha emitters with particular focus on recent studies of targeted alpha therapy of bladder cancer, brain tumors, neuroendocrine tumors and prostate cancer...
2018: Current Radiopharmaceuticals
George Sgouros, Robert Hobbs, Anders Josefsson
BACKGROUND: Radiopharmaceutical therapy is a cancer treatment modality by which radiation is delivered directly to targeted tumor cells or to their microenvironment. This makes it possible to deliver highly potent alpha-particle radiation. The short-range and highly potent nature of alpha-particles require a dosimetry methodology that considers microscale distributions of the alpha-emitting agent. The high energy deposition density along an alpha-particle track causes a spectrum of DNA lesions...
2018: Current Radiopharmaceuticals
Zewei Jiang, Ekaterina Revskaya, Darrell R Fisher, Ekaterina Dadachova
BACKGROUND AND OBJECTIVE: The demand for the alpha-emitting radionuclide Actinium-225 (225Ac) for use in radionuclide therapy is growing. Producing 225Ac using high energy linear accelerators, cyclotrons or photoinduction could increase its supply. One potential problem with accelerator produced 225Ac using Thorium-232 targets is the presence in final product of 0.1-0.3% by activity of the long-lived 227Ac impurity at the end of irradiation. It is important to comprehensively evaluate the behavior of accelerator-produced 225Ac in vivo before using it in pre-clinical and clinical applications...
2018: Current Radiopharmaceuticals
Elena De Ponti, Sabrina Morzenti, Cinzia Crivellaro, Federica Elisei, Andrea Crespi, Luca Guerra
BACKGROUND AND OBJECTIVE: Motion due to patient's breathing can introduce heavy bias in PET/CT, both in image quality and quantitation. This paper is a review of the main technical solutions available to manage movement in PET/CT studies: a) Respiratory Gated (RG), b) Motion Free (MF), c) End Expiration (EE), d) Banana Artefact Management (BAM) and e) Data Driven Gating (DDG). METHODS: The most diffused solutions (RG, MF and EE) are based on LIST mode acquisition of a PET Field of View (4D FOV), centered on the anatomical region of interest; to link PET data not only to time and to spatial position but also to the corresponding breathing phase, the synchronized acquisition of the patient's breathing curve is performed by an external tracking device...
2018: Current Radiopharmaceuticals
Jonathan W Engle
BACKGROUND: The radionuclide 225Ac and its daughter 213Bi are among the most interesting alpha emitters being evaluated for incorporation into targeted therapeutic vectors. Global supply of 225Ac is presently insufficient to meet anticipated clinical demand, but the deficiency has been targeted by many research and development efforts, privately and publicly funded. From more than a decade of these endeavors, no single production technology has emerged as a complete solution. In the foreseeable future, global supply of 225Ac will continue to be sourced from a patchwork of production methods and laboratories with a range of radioisotopic purities and achievable yields...
2018: Current Radiopharmaceuticals
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