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[Esophageal cancer: outcome according to therapeutic strategy].

PURPOSE: To assess the outcome of esophageal cancer according to therapeutic strategy. PATIENTS AND METHODS: One-hundred and twenty patients with esophageal cancer treated by an association of radiotherapy and chemotherapy and possibly surgery, between 2004 and 2010, were retrospectively studied. The first site of relapse was classified as follows: local (tumour), locoregional (tumour and/or nodal: celiac, mediastinal, sus-clavicular) or metastatic. RESULTS: With a 15.7-months (1.4-62) median follow-up, there were 89 deaths and 79 recurrences. Three types of treatments were performed: 50Gy e

High-dose chemotherapy in relapsed or refractory Hodgkin lymphoma patients: a reappraisal of prognostic factors.

High-dose chemotherapy (HDCT) has a consolidated role in the treatment of patients with refractory or relapsed Hodgkin lymphoma (HL). We report clinical results of 97 HL patients who underwent HDCT for refractory (62 patients) or relapsed (35 patients) diseases in Istituto Europeo di Oncologia, from 1995 to 2009. Treatment included high-dose carmustine, etoposide, cytarabine and melphalan in 84 patients and high-dose idarubicin and melphalan in 13 patients with subsequent peripheral hemopoietic stem cells transplant. Outcomes were evaluated in terms of progression-free survival (PFS) and overa

Sustainable release of vancomycin, gentamicin and lidocaine from novel electrospun sandwich-structured PLGA/collagen nanofibrous membranes.

This study investigated the in vitro release of vancomycin, gentamicin, and lidocaine from novel electrospun sandwich-structured polylactide-polyglycolide (PLGA)/collagen nanofibrous membranes. For the electrospinning of biodegradable membranes, PLGA/collagen and PLGA/vancomycin/gentamicin/lidocaine were separately dissolved in 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP). They were then electrospun into sandwich structured membranes, with PLGA/collagen for the surface layers and PLGA/drugs for the core layer. After electrospinning, an elution method and HPLC assay were employed to characterize th

Meeting abstracts from the 21st European Symposium on Radiopharmacy and Radiopharmaceuticals

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Extramedullary Soft Tissue Involvement and Discrepant Osseous Uptake on Tc-99m MDP and Ga-67 Citrate Scintigraphy in a Patient With Multiple Myeloma: A Case Report and Literature Review.

Multiple myeloma (MM) is a plasma cell neoplasm with skeletal destruction which could also spread to extramedullary regions. Common diagnostic imaging modalities include skeletal radiography, computed tomography (CT), magnetic resonance imaging (MRI). Recently, PET/CT is proposed as an ideal tomographic tool for diagnosis and follow-up, but impending factors includes high cost, limited availability of cameras and radiotracers. Bone scan and gallium scan are usually considered of limited clinical value. Herein, we present a 66-year-old Taiwanese man with MM, who was hospitalized to our hospital

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… Extramedullary involvement is a poor prognostic indicator, 3 , 4 which could be detected by gallium scintigraphy. 5 – 7 Recently, PET/CT with 2-deoxy-2-[fluorine-18]fluoro- d -glucose ( 18 F-FDG) is proposed as an ideal tomographic tool for diagnosis and follow-up, but impending factors includes high … Footnotes Abbreviations: 18 F-FDG = 2-deoxy-2-[fluorine-18]fluoro- d -glucose, CT = computed tomography, LDH = lactate dehydrogenase, MM = multiple myeloma, MRI = magnetic resonance imaging, PET = positron emission tomography. The authors have no funding or conflicts of interest to disclose. …

New PET Radiotracers for the Imaging of Neuroendocrine Neoplasms.

Opinion statementNeuroendocrine neoplasms (NEN) are a heterogeneous group of tumours derived from cells of neuroendocrine origin and can potentially arise everywhere in the human body. The diagnostic assessment of NEN can be performed using a variety of PET radiopharmaceuticals. Well-differentiated NEN (NET) present a high expression of SSTR (somatostatin receptors) and can therefore be studied with 68Ga-DOTA-peptides ([68Ga]Ga-DOTANOC, [68Ga]Ga-DOTATOC, [68Ga]Ga-DOTATATE). Current guidelines recommend the use of SSTR imaging to assess disease extension at staging/restaging, follow-up, assessm

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… Recently, a novel SSTR agonist labelled with fluorine was synthesised: [18F]F-AlF-NOTA-octreotide, produced with the Al18F-method, with the advantages of a chelator-based radiolabelling method and the advantages of fluorine-18 in imaging and logistical field [ 25 ]. … [18F]F-MFBG [18F]F-meta-fluorobenzylguanidine ([18F]F-MFBG) is a fluorinated analogue of [123I]I-MIBG, labelled with 18F (half life of 110 min), which is accumulated in cells through the same norepinephrine transporter uptake mechanism of [123I]I-MIBG. …

Toxic role of K+ channel oxidation in mammalian brain.

Potassium (K(+)) channels are essential to neuronal signaling and survival. Here we show that these proteins are targets of reactive oxygen species in mammalian brain and that their oxidation contributes to neuropathy. Thus, the KCNB1 (Kv2.1) channel, which is abundantly expressed in cortex and hippocampus, formed oligomers upon exposure to oxidizing agents. These oligomers were ∼10-fold more abundant in the brain of old than young mice. Oxidant-induced oligomerization of wild-type KCNB1 enhanced apoptosis in neuronal cells subject to oxidative insults. Consequently, a KCNB1 variant resistant

Regulation of hepatic fatty acid elongase 5 by LXRalpha-SREBP-1c.

Dietary essential fatty acids linoleic acid and alpha-linolenic acid are converted to arachidonic-, eicosapentaenoic-, and docosahexaenoic acid under tight regulation by nutritional status and hormones. Hepatic fatty acid elongase 5 (Elovl5) elongates C18-20 polyunsaturated fatty acids (PUFAs) and is important for biosynthesis of C20-22 PUFAs. We demonstrate that Liver X Receptor alpha (LXRalpha) and sterol regulatory binding protein-1c (SREBP-1c) regulate hepatic Elovl5 expression. LXRalpha and LXRbeta play different roles in maintenance of basal expression of Elovl5. LXRalpha is necessary fo

The value of FDG positron emission tomography/computerised tomography (PET/CT) in pre-operative staging of colorectal cancer: a systematic review and economic evaluation.

OBJECTIVES: In the UK, colorectal cancer (CRC) is the third most common malignancy (behind lung and breast cancer) with 37,514 cases registe … ' scan). The research objectives are: to evaluate the diagnostic accuracy and therapeutic impact of fluorine-18-deoxyglucose (FDG) PET/CT for the pre-operative staging of primary, recurrent and metastatic cancer using systematic review methods; undertake probabilistic decision-analytic modelling (using Monte Carlo simulation); and conduct a value of inform …

FDA-Approved Drugs Containing Amide Functionality in the Last Five Years (2021-2025): Pharmaceutical Use, Trends and Synthetic Approaches.

The amide functional group remains a cornerstone of medicinal chemistry, serving as an indispensable scaffold in the design of modern therapeutics. This review presents an analysis of FDA-approved drugs (small molecules and peptides with MW ®), amides form the structural backbone of peptidomimetics, enabling high-affinity binding to a viral protease. In precision oncology, as seen with adagrasib (Krazati®), the amide acts as a critical, metabolically stable linker that positions a covalent warhead for selective inhibition of a mutant kinase. This analysis underscores that amide's unique combin

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… The fluorinated aromatic ring and CF 3 /difluoro substituents on the right enhance lipophilicity, metabolic stability, and binding affinity. … Moreover, N -aromatic heterocycles and fluorine atoms are present in two-thirds of all the small molecules approved in the year [ 28 ]. 2.4.1. …

Advanced Technologies for Large Scale Supply of Marine Drugs.

Marine organisms represent a source of unique chemical entities with valuable biomedical potentialities, broad diversity, and complexity. It is essential to ensure a reliable and sustainable supply of marine natural products (MNPs) for their translation into commercial drugs and other valuable products. From a structural point of view and with few exceptions, MNPs of pharmaceutical importance derive from the so-called secondary metabolism of marine organisms. When production strategies rely on marine macroorganisms, harvesting or culturing coupled with extraction procedures frequently remain t

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… In order to avoid adenosine deaminase mediated deactivation, Vidarabine ( 8 ) was initially replaced by Fludarabine ( 9 ) which carries, in addition, a fluorine at 2-position of the adenine ( Figure 1 ) [ 75 ]. 3.1.4. … The Balz–Schiemann reaction selectively obtained the purine derivative fluorinated at carbon 2 which, after deprotection of the hydroxyl groups, gives rise to Fludarabine ( 9 ) ( Scheme 5 ) [ 79 ]. …

CD70-targeted platform for diagnosing and treating multiple myeloma.

BackgroundCD70, overexpressed in multiple myeloma (MM), is a promising target for theranostics. This study developed a CD70-targeted theranostic pair: the immuno-positron emission tomography tracer [89Zr]Zr-DFO-ABDB6 and the therapeutic agent [177Lu]Lu-DOTA-ABDB6, aiming to combine imaging and radiotherapy for MM.MethodsCD70 expression was confirmed in patients with MM samples (positivity rate, 66.7%) and RPMI-8226 xenografts. The nanobody derivative ABDB6 was conjugated to DFO or DOTA and radiolabeled with 89Zr or 177Lu. Pharmacokinetics, biodistribution, and toxicity were evaluated in NCG an

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… Preclinical and clinical studies have demonstrated that [ 68 Ga]Ga-NOTA-RCCB6 and [ 18 F]RCCB6 outperform traditional tracers, such as fluorine-18 fluorodeoxyglucose ( 18 F-FDG), in diagnostic specificity and sensitivity, enabling precise lesion localization and longitudinal monitoring of therapeutic … **p<0.01, ***p<0.001. 18 F-FDG, fluorine-18 fluorodeoxyglucose; MIP, maximum-intensity projection; MM, multiple myeloma; PET, positron emission tomography; SUVmax, maximum standardized uptake value;TBR, tumor/bone ratio; TMR, tumor/muscle ratio. …

Clinicopathological characteristics of primary central nervous system lymphoma with low 18F-fludeoxyglucose uptake on brain positron emission tomography.

Primary central nervous system lymphoma (PCNSL) typically shows a strong uptake of F-fludeoxyglucose (FDG) imaged by positron emission tomography (PET). Uncommonly, PCNSL demonstrates a low uptake on FDG PET. We investigated the clinicopathological characteristics of the unusual cases of PCNSL with low FDG uptake.We retrospectively enrolled 104 consecutive patients with newly diagnosed PCNSL who underwent baseline brain FDG PET. The degree of FDG uptake of PCNSL was visually scored by 4 grades (0, ≤contralateral white matter; 1, >contralateral white matter and contralateral gray matter). Grade

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… AJR Am J Roentgenol 2008 ; 190 : W365 – 9 . 18492879 10.2214/AJR.07.2660 [10] Rosenfeld SS Hoffman JM Coleman RE Studies of primary central nervous system lymphoma with fluorine-18-fluorodeoxyglucose positron emission tomography . … Invest Ophthalmol Vis Sci 2005 ; 46 : 3957 – 64 . 16249468 10.1167/iovs.05-0318 [26] Roelcke U Blasberg RG von Ammon K Dexamethasone treatment and plasma glucose levels: relevance for fluorine-18-fluorodeoxyglucose uptake measurements in gliomas . …

Radiocopper in BCMA-targeted immunotheranostics of myeloma.

BACKGROUND: The theranostic potential of copper-64 (PET imaging) and copper-67 (SPECT imaging and therapy) is increasingly recognized. This work investigates the performance of this 'true' matched pair in a preclinical radioimmunotheranostic setting that utilizes experimental monoclonal antibodies (mAbs) directed against B cell maturation antigen (BCMA), a transmembrane glycoprotein that has emerged as a critical target for the treatment of multiple myeloma (MM). METHODS: The commercially available BCMA-directed mAbs MAB193 and Vicky-1 were modified with the bispidine N2py4 enabling chelation

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… Besides mAb-based approaches, other BCMA-specific vector molecules have been converted into gallium-68- and fluorine-18-containing PET radiotracers, including peptides 29 and sdAbs 27 , 32 , 33 . … However, in one recent study, a fluorine-18-labeled BCMA-specific sdAb has shown comparable uptake in both subcutaneous and disseminated myeloma xenografts 32 . …

Targeting Selectins and Their Ligands in Cancer.

Aberrant glycosylation is a hallmark of cancer cells with increased evidence pointing to a role in tumor progression. In particular, aberrant sialylation of glycoproteins and glycolipids has been linked to increased immune cell evasion, drug evasion, drug resistance, tumor invasiveness, and vascular dissemination, leading to metastases. Hypersialylation of cancer cells is largely the result of overexpression of sialyltransferases (STs). Differentially, humans express twenty different STs in a tissue-specific manner, each of which catalyzes the attachment of sialic acids via different glycosidi

India's Growing Nuclear Medicine Infrastructure and Emergence of Radiotheranostics in Cancer Care: Associated Challenges and the Opportunities to Collaborate.

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… Being a dedicated Neuro Institute, NIMHANS has developed radiotracers such as fluorine-18-[ 18 F] flumazenil for imaging benzodiazepine receptors, [ 18 F]-AVT-011 for assessing p-glycoprotein expression, and also started carbon-11-PBR28 TSPO PET imaging in amyotrophic lateral sclerosis.[ 18 , 19 ] Institute … Synthesis, characterization, and radiosynthesis of fluorine-18-AVT-011 as a Pgp chemoresistance imaging marker. Sci Rep. 2022;12:18584. doi: 10.1038/s41598-022-22930-6. 20. Das S, Sakhare N, Kumar D, Mathur A, Mirapurkar S, Sheela M, et al. …

Innovative Peptide Therapeutics in the Pipeline: Transforming Cancer Detection and Treatment.

Cancer remains a leading global health burden, profoundly affecting patient survival and quality of life. Current treatments-including chemotherapy, radiotherapy, immunotherapy, and surgery-are often limited by toxicity or insufficient specificity. Conventional chemotherapy, for instance, indiscriminately attacks rapidly dividing cells, causing severe side effects. In contrast, peptide-based therapeutics offer a paradigm shift, combining high tumour-targeting precision with minimal off-target effects. Their low immunogenicity, multi-pathway modulation capabilities, and adaptability for diagnos

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… to the positron-emitting isotope fluorine-18 ( 18 F) ( Figure 9 ) [ 112 ]. … Radiosynthesis of high affinity fluorine-18 labeled GnRH peptide analogues: In vitro studies and in vivo assessment of brain uptake in rats. MedChemComm. 2015;6:708–714. doi: 10.1039/C4MD00486H. 79. Gründker C., Emons G. …

Detection Rate and Clinical Impact of PET/CT with 18F-FACBC in Patients with Biochemical Recurrence of Prostate Cancer: A Retrospective Bicentric Study.

Our aim was to assess the detection rate (DR) of positron emission computed tomography (PET/CT) with anti-1-amino-3-[18F]-flurocyclobutane-1-carboxylic acid (18F-FACBC) in patients with biochemical recurrence (BCR) from prostate cancer (PC). As a secondary endpoint, we evaluated 18F-FACBC PET/CT's impact on patients management. Clinical records of 81 patients submitted to 18F-FACBC PET/CT due to PC BCR in two Italian Nuclear Medicine Units were retrospectively assessed. DR was gauged in the whole cohort and stratifying patients by discrete intervals of PSA levels. PET/CT's impact on clinical m

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… In this scenario, positron emission computed tomography (PET/CT) has been successfully applied for the detection of metabolically active tumor tissue through the radiopharmaceutical choline, labeled with 18-fluorine ( 18 F) or 11-carbon ( 11 C) radionuclide. … Fluorine-18-Labeled Fluciclovine PET/CT in Primary and Biochemical Recurrent Prostate Cancer Management Am. J. Roentgenol. 2020 215 267 276 10.2214/AJR.19.22404 32551903 24. Parent E.E. …

Multimodal imaging of bone metastases: From preclinical to clinical applications.

Metastases to the skeletal system are commonly observed in cancer patients, highly affecting the patients' quality of life. Imaging plays a major role in detection, follow-up, and molecular characterisation of metastatic disease. Thus, imaging techniques have been optimised and combined in a multimodal and multiparametric manner for assessment of complementary aspects in osseous metastases. This review summarises both application of the most relevant imaging techniques for bone metastasis in preclinical models and the clinical setting.

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… Accuracy of whole-body fluorine-18-FDG PET for the detection of recurrent or metastatic breast carcinoma. J Nucl Med. 1998;39:431–435. 83. Sugawara Y., Fisher S.J., Zasadny K.R., Kison P.V., Baker L.H., Wahl R.L. … Preclinical and clinical studies of bone marrow uptake of fluorine-1-fluorodeoxyglucose with or without granulocyte colony-stimulating factor during chemotherapy. J Clin Oncol. 1998;16:173–180. doi: 10.1200/JCO.1998.16.1.173. 84. …

Targeted treatments of bone metastases in patients with lung cancer.

Until now ~30-40% of patients with advanced lung cancer develop bone metastases, but as the newer therapies are extending survival, the chance of developing bone metastases increases. Bone metastases cause skeletal-related events (SREs) such as pathologic fractures, spinal cord compression, radiation therapy or surgery to bone, or hypercalcemia, which can have debilitating consequences affecting patients' health-related quality of life (HR-QOL) and performance status (PS). Poor PS then prevents the patients to receive further lines of treatments, which are available today. SREs are associated

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… Fluorine-18 deoxyglucose (FDG)-PET scans for the detection of bone metastases in NSCLC have been shown to have a higher specificity compared with bone scans (~90 versus 70%, respectively) ( 13 , 14 ) and a much lower rate of false negatives (6 versus 39%, respectively) ( 15 ). … Available from: http://www.nccn.org/professionals/physician_gls/PDF/nsclc.pdf 13 Bury T Barreto A Daenen F Barthelemy N Ghaye B Rigo P Fluorine-18 deoxyglucose positron emission tomography for the detection of bone metastases in patients with non-small cell lung cancer . …