Search results for "pharmaceuticals"
showing 10 items of 202 documents
Clinical Translation and First In-Human Use of [44Sc]Sc-PSMA-617 for PET Imaging of Metastasized Castrate-Resistant Prostate Cancer
2017
Background: Various trivalent radiometals are well suited for labeling of DOTA-conjugated variants of Glu-ureido-based prostate-specific membrane antigen (PSMA) inhibitors. The DOTA-conjugate PSMA-617 has proven high potential in PSMA radioligand therapy (PSMA-RLT) of prostate cancer as well as PET imaging when labeled with lutetium-177 and gallium-68 respectively. Considering the relatively short physical half-life of gallium-68 this positron emitter precludes prolonged acquisition periods, as required for pre-therapeutic dosimetry or intraoperative applications. In this context, the positron emitter scandium-44 is an attractive alternative for PET imaging. We report the synthesis of [44Sc…
[18F]FDG-PET predicts complete pathological response of breast cancer to neoadjuvant chemotherapy
2007
To evaluate, in breast cancer patients treated by neoadjuvant chemotherapy, the predictive value of reduction in FDG uptake with regard to complete pathological response (pCR).Forty-seven women with non-metastatic, non-inflammatory, large or locally advanced breast cancer were included. Tumour uptake of FDG was evaluated before and after the first course of neoadjuvant chemotherapy. Four indices were used: maximal and average SUV without or with correction by body surface area and glycaemia (SUV(max), SUV(avg), SUV(max-BSA-G) and SUV(avg-BSA-G), respectively). The predictive value of reduction in FDG uptake with respect to pCR was studied by logistic regression analysis. Relationships betwe…
Radiation protection evaluations about a radiopharmaceutical production center based on a cyclotron
2012
Positron Emission Tomography (PET) has became a worldwide used functional and molecular imaging technique. Most of PET (or PET/CT- Computed Tomography) diagnostic facilities are installed within large population cities as well as dimensions of modern medical cyclotrons allow to install them inside hospitals or other health centers. Therefore, special radiation protection evaluations to assure safety operational conditions to operators and population are required. This work is focused on training activities oriented to evaluate PET/Cyclotron radiation protection procedures or to study special safety systems. The students are particularly oriented to determine shielding thickness according to…
In Vitro Evaluation of the Squaramide-Conjugated Fibroblast Activation Protein Inhibitor-Based Agents AAZTA5.SA.FAPi and DOTA.SA.FAPi
2021
Recently, the first squaramide-(SA) containing FAP inhibitor-derived radiotracers were introduced. DATA5m.SA.FAPi and DOTA.SA.FAPi with their non-radioactive complexes showed high affinity and selectivity for FAP. After a successful preclinical study with [68Ga]Ga-DOTA.SA.FAPi, the first patient studies were realized for both compounds. Here, we present a new squaramide-containing compound targeting FAP, based on the AAZTA5 chelator 1,4-bis-(carboxylmethyl)-6-[bis-(carboxymethyl)-amino-6-pentanoic-acid]-perhydro-1,4-diazepine. For this molecule (AAZTA5.SA.FAPi), complexation with radionuclides such as gallium-68, scandium-44, and lutetium-177 was investigated, and the in vitro properties of…
Castleman's disease presenting as fever of unknown origin: diagnostic value of fluorodeoxyglucose-positron emission tomography/computed tomography.
2009
Abstract: Castleman's disease is an uncommon lymphoproliferative disorder that can present in both nodal and extranodal sites. The cause is unknown, but a disordered immunoregulation, which results in the excessive proliferation of B lymphocytes and plasma cells in lymphoid organs, plays a central role in the development of the condition. Three distinct histologic types (hyaline vascular, plasma cell, and mixed), and 2 anatomical variants (localized and multicentric) have been described. Clinical presentation generally consists of enlargement of lymph nodes or other tissues, fever, asthenia, weight loss, and other general symptoms, associated with nonspecific blood analysis abnormalities, s…
Copper radiopharmaceuticals for theranostic applications
2018
The growing advancement in nuclear medicine challenges researchers from several different fields to integrate imaging and therapeutic modalities in a theranostic radiopharmaceutical, which can be defined as a molecular entity with readily replaceable radioisotope to provide easy switch between diagnostic and therapeutic applications for efficient and patient-friendly treatment of diseases. For such a reason, the diagnostic and therapeutic potential of all five medical radionuclides of copper have thoroughly been investigated as they boost the hope for development of successful radiotheranostics. To facilitate the mutual understanding between all different specialists working on this multidi…
Approaching ‘kit-type’ labelling with 68Ga : the DATA chelators.
2015
The DATA chelators are a novel class of tri-anionic ligands based on 6-amino-1,4-diazepine-triacetic acid, which have been introduced recently for the chelation of (68)Ga. Compared with macrocyclic chelators based on the cyclen scaffold (i.e., DOTA, DO3A, and DO2A derivatives), DATA chelators undergo quantitative radiolabelling more rapidly and under milder conditions. In this study, a systematic evaluation of the labelling of four DATA chelators--DATA(M), DATA(P), DATA(Ph), and DATA(PPh)--with (68)Ga is presented. The results highlight the extraordinary potential of this new class of chelators for application in molecular imaging using (68)Ga positron emission tomography (PET).
Phantom size in brachytherapy source dosimetric studies
2004
An important point to consider in a brachytherapy dosimetry study is the phantom size involved in calculations or experimental measurements. As pointed out by Williamson [Med. Phys. 18, 776-786 (1991)] this topic has a relevant influence on final dosimetric results. Presently, one-dimensional (1-D) algorithms and newly-developed 3-D correction algorithms are based on physics data that are obtained under full scatter conditions, i.e., assumed infinite phantom size. One can then assume that reference dose distributions in source dosimetry for photon brachytherapy should use an unbounded phantom size rather than phantom-like dimensions. Our aim in this paper is to study the effect of phantom s…
Image-Guided Synthesis Reveals Potent Blood-Brain Barrier Permeable Histone Deacetylase Inhibitors
2014
Recent studies have revealed that several histone deacetylase (HDAC) inhibitors, which are used to study/treat brain diseases, show low blood-brain barrier (BBB) penetration. In addition to low HDAC potency and selectivity observed, poor brain penetrance may account for the high doses needed to achieve therapeutic efficacy. Here we report the development and evaluation of highly potent and blood-brain barrier permeable HDAC inhibitors for CNS applications based on an image-guided approach involving the parallel synthesis and radiolabeling of a series of compounds based on the benzamide HDAC inhibitor, MS-275 as a template. BBB penetration was optimized by rapid carbon-11 labeling and PET im…
Evaluation of [11C]Metergoline as a PET Radiotracer for 5HTR in Nonhuman Primates
2010
Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [{sup 11}C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [{sup 11}C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.